Modulateurs d'enzymes

6-Thioguanine is a purine analog used in the therapy for leukemia and for remission consolidation in patients with acute nonlymphocytic anemia. This drug also has antimetabolite action. It replaces guanine during DNA replication. This substitution disrupts the accurate pairing of DNA bases, leading to errors in DNA replication and hinders cell division. 6-Thioguanine is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Selective inhibitor of the interaction between the UNC119 chaperone and its cargo. Squarunkin A inhibits activation of Src kinase by interrupting the interaction between the myristoylated peptide at the N-terminus of the Src kinase and UNC119A chaperone (IC50 = 10 nM). Squarunkin A impairs the UNC119-mediated enrichment of plasma membrane with non-receptor protein tyrosine kinase Src, resulting in the decrease in Src autophosphorylation and decreased oncogenic Src signalling.

Apixaban is an anticoagulant agent used for the prophylaxis of stroke and deep vein thrombosis leading to pulmonary embolism. This drug is an inhibitor of factor Xa and prothrominase. As a result, this prevents the formation of a thrombus. Apixaban is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

p38 MAP kinase antagonist

Inhibits phorbol ester TPA/PMA; immunosuppressant

Inhibitor of carbonic anhydrase; muscle relaxant

Hydroxychloroquine is a drug that is used to treat multiple types of autoimmune diseases, including rheumatoid arthritis, systemic lupus erythematosus and discoid lupus. It is a prodrug, which is activated in the liver to hydroxychloroquine. It inhibits the production of inflammatory cytokines and nitric oxide by binding to the toll-like receptor 4 (TLR4) and inhibiting signaling pathways downstream of TLR4 activation. Additionally, Hydroxychloroquine is used to prevent and treat malaria caused by parasitic protozoan from the Plasmodium genus. Furthermore, recent studies revealed that hydroxychloroquine has beneficial effects on COVID-19 patients, as the current evidence shows that hydroxychloroquine inhibits SARS CoV-2 entry in host cells by interfering with endocytosis and affecting the glycoprofile on the spike glycoprotein. Hydroxychloroquine sulfate is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Inhibitor of the histone methyltransferase SETD8 that supresses methylation of the K20 residue in histone 4. UNC 0379 treatment of human glioma reduced recruitment of 53BP1 protein to double strand breaks and sensitised cells to radiotherapy without altering cell cycle kinetics.

Inhibits JAK1 and JAK2 kinases

Potent and irreversible inhibitor of phosphoinositide-3-kinase (PtdIns-3-kinase) with IC50 of 0.1 nM. PX 866 inhibited cell motility and growth of 3D spheroids of glioblastoma, breast, prostate and colon cancer cell lines at low nanomolar concentrations. PX 866 also exhibited anti-tumoral activity in vivo in xenograft models for ovarian and lung cancer.

Reversible inhibitor of trypsin

The peptide IRW, characterised from egg protein, exhibits inhibitory properties against the angiotensin converting enzyme (ACE2) and could be used to prevent cardiovascular disease with further research. Treatment of hypertensive mice with IRW induced endothelium-dependent vasorelaxation and reduced vascular inflammation. The IRW tripeptide acts as anti-hypertensive by upregulating ACE2 activity via the Mas receptor (MasR) and upregulating Akt/eNOS signalling in the aorta. IRW also induces superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPx) activity. These may play a factor in IRW's role as an anti-inflammatory. IRW shows promise as a nutraceutical for inflammatory conditions and a tool for drug development in cardiovascular disease.

Pritelivir mesylate is an antiviral compound, which is derived from thiazolylamide class molecules, with a targeted mechanism of action against the herpes simplex virus (HSV). It functions by inhibiting the viral helicase-primase complex, which is essential for the replication of viral DNA. This distinct mode of action differentiates it from traditional treatments like acyclovir, which targets viral DNA polymerase. Pritelivir mesylate is primarily used in the treatment and suppression of HSV infections, including HSV-1 and HSV-2. By targeting the helicase-primase, it effectively reduces the replication of the virus, leading to decreased viral shedding and lesion formation. Its unique pathway offers an alternative for cases where resistance to standard antivirals occurs. Given its potential, Pritelivir mesylate is under extensive study to better understand its efficacy and safety profile. Its promising results in early clinical trials may provide a significant advancement in antiviral therapies, offering new hope for managing and controlling HSV infections.

Teniposide is a cytotoxic drug that is used in the treatment of refractory childhood acute lymphoblastic leukemia. It has antitumour activity. It is a type II topoisomerase inhibitor. This drug inhibits DNA synthesis by forming a complex with topoisomerase II and DNA. Teniposide is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Inhibits lysophosphatidylserine hydrolysis by the integral membrane serine hydrolase ABHD12 (IC50 = 1.3 µM). Raised levels of lysophosphatidylserine were observed in mouse brain in vivo and in primary human macrophages. DO 264 had proinflammatory effects, following infection with lymphocytic choriomeningitis virus (LCV) clone 13 in mice, resulting in severe inflammatory lung damage.

Inhibitor of VEGFR, PDGR, c-Kit and Ret; inhibitor of angiogenesis

SU 3327, originally introduced as a thiadiazole JNK inhibitor (De et al. 2009) has recently been identified as having antibiotic activity against a broad range of bacteria including drug-resistant gram positive and negative strains (Strokes et al. 2020). This molecule has been given the fictional name ‘Halicin’ inspired by the AI approach used to discover its novel biological activity.

Mirodenafil dihydrochloride is a potent phosphodiesterase-5 (PDE5) inhibitor, which is a synthetic compound with a primarily chemical origin. Its mode of action involves the inhibition of the enzyme PDE5, which predominantly resides in the smooth muscle cells lining blood vessels. By inhibiting PDE5, Mirodenafil dihydrochloride effectively increases the levels of cyclic guanosine monophosphate (cGMP), leading to the relaxation of smooth muscle tissues and vasodilation. This mechanism of action makes Mirodenafil dihydrochloride particularly effective in the treatment of erectile dysfunction (ED). By enhancing blood flow to specific areas of the body, primarily the corpus cavernosum of the penis, it facilitates the achievement and maintenance of an erection in response to sexual stimulation. The compound’s selectivity for PDE5 over other phosphodiesterases minimizes potential side effects and enhances its therapeutic efficacy. As such, Mirodenafil dihydrochloride serves as a valuable tool in clinical settings for managing erectile dysfunction, providing an alternative for patients who may not respond to or tolerate other PDE5 inhibitors.

Inhibitor of BACE1 protease

Anagrelide is a thrombocytopenic drug that is used to treat thrombocythemia and related conditions. This drug works by decreasing the platelet count by suppressing transcription factors that are necessary for the maturation of platelets. This drug is also a phosphodiesterase III inhibitor. Anagrelide HCl is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Selective inhibitor of the mutated RET variant RETV804M, which is the anticipated drug-resistant RET mutant that can occur in tumours treated with kinase inhibitors. The compound has a biochemical IC50 of 0.02 µM and selectivity for purified RETV804M over purified RET and KDR of 3.7 and 110, respectively. The efficacy of the compound was shown also in cell cultures with IC50 of 4.4 µM, and cell assay selectivity for RETV804M over RET and KDR of 0.89 and 2.3, respectively.

Proteosome inhibitor; pro-apoptotic; has anti-myeloma activity

Fluvastatin is a statin that lowers blood cholesterol and triglycerides by inhibiting HMG-CoA reductase, an enzyme that plays a critical role in the synthesis of cholesterol. Fluvastatin has also been shown to reduce the incidence of myocardial infarction, and to reduce atherosclerotic lesions in animal models, reducing the incidence of cardiovascular disease. Fluvastatin also has been shown to inhibit the activation of toll-like receptor 4 (TLR4) by lipopolysaccharide (LPS), which may be related to its anti-inflammatory effects. Furthermore, through lowering blood cholesterol, Fluvastatin also inhibits tubulointerstitial injury and prevents renal damage caused by high concentrations of the lipid.

Drotaverine is an antispasmodic drug that is used to alleviate gastrointestinal and genitourinary smooth muscle spasms. This drug works by inhibiting phosphodiesterase-4 and increasing levels of cAMP leading to smooth muscle relaxation. Drotaverine HCl is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Tacrolimus is a calcineurin inhibitor drug that is used for the prevention of rejection after an organ transplant. This drug can also be used in the treatment of severe atopic dermatitis. Tacrolimus’ mechanism of action is not well known however it is understood that this drug inhibits T-lymphocyte activation by binding to an intracellular protein called FKBP-12. This drug also has anti-inflammatory properties. Tacrolimus monohydrate is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

The sequence of this peptide has been derived from a highly conserved region of the T-cell phosphatase TC.PTP45 and is an excellent general substrate for protein tyrosine phosphatases.The protein tyrosine phosphatase (PTP) superfamily has 103 enzymes that catalyse substrate dephosphorylation at tyrosine residues through a covalent enzyme intermediate involving a thiophosphate linkage from the active site cysteine residue. All PTPs share a common signature motif (I/V)HCXAGXGR(S/T), named the P-loop, responsible for the enzyme activity. The PTP superfamily can be divided into four classes based on their cellular localization/catalytic domains: the receptor-like PTPs (rPTPs), the non-receptor PTPs (nrPTPs), the low molecular weight PTP (LMWPTP), and the VH-1 and CDC-25 groups.PTPs are involved in regulating a plethora of cellular activities, including proliferation and differentiation, survival, migration, metabolism, and the immune response. Abnormal protein tyrosine phosphorylation has been associated with the etiology of various human diseases, including cancer, diabetes, and autoimmune dysfunctions, therefore making PTPs novel therapeutic targets.

Ligand of plasminogen; used for bleeding control

Inhibitor of Aurora kinases A, B and C

Inhibits human and mouse diacylglycerol O-acyltransferase 1 (DGAT-1) with IC50 values of 9 and 22 nM, respectively. Selective for DGAT-1 over DGAT-2 (IC50 = 53 µM), acyl coenzyme A transferase (IC50 = 296 µM) and other acyltransferases. Reduces plasma and liver triglycerides, FFA, chylomicron secretion and increases HDL cholesterol in vivo.

Specific inhibitor of the phosphoinositide 3-kinase (PI3K) alpha subunit with IC50 of 32 nM. In heart muscle it negatively regulates hypertrophic growth, causes increase in late sodium current and leads to arrhythmias. In tumours it inhibits the p110α subunit of PI3K and blocks growth factor signalling resulting in reduced tumour growth.

Odevixibat is a pharmacological agent that functions as an ileal bile acid transport inhibitor, which is synthesized through complex organic chemistry methods to create a specific molecular structure targeting bile acid transport mechanisms. It works by inhibiting the apical sodium-dependent bile acid transporter (ASBT) in the terminal ileum. This action reduces the reabsorption of bile acids from the small intestine back into the liver, thereby reducing overall bile acid levels in the body. The primary application of Odevixibat is in managing progressive familial intrahepatic cholestasis (PFIC), a rare genetic disorder characterized by impaired bile flow and accumulation of bile acids, leading to liver injury. By lowering bile acid levels, Odevixibat can alleviate symptoms such as intense pruritus and slow the progression of liver damage. Its role in improving patient outcomes in cholestatic liver diseases makes it a key therapeutic option under investigation and application. Additionally, its unique mechanism of action provides a valuable approach to addressing unmet medical needs in rare hepatic conditions.

H-9 hydrochloride is a group P2 proton pump inhibitor that inhibits the H+/K+ ATPase enzyme. It is a prodrug that is metabolized to the active form, H-9, by esterases in the gut wall. The proton pump inhibitor blocks the conversion of K+ to H+, thereby reducing gastric acidity. H-9 hydrochloride has been shown to have antimicrobial activity and has been used in the treatment of infectious diseases such as bowel disease and inflammatory bowel disease. The drug also has kinetic energy which can be measured using laser ablation and X-ray diffraction data.

Inhibits Akt translocation by targeting the pleckstrin homology (PH) domain. Inhibits hepatitis C virus NS5B RNA-dependent RNA polymerase (IC50 = 79 µM). Attenuates cannabinoid agonist-mediated proliferation of neural stem/precursor cells.

This peptide is phosphorylated by Janus kinase 1 (JAK1) and is an ideal substrate for use in kinase assays. The JAK family of kinases is essential for the signalling of a host of immune modulators in tumour, stromal, and immune cells where they are highly expressed. JAK family proteins mediate the signalling of the interferon (IFN), IL-6, and IL-2 families of cytokines.JAK kinases are associated with cytokine receptors. Cytokine binding to these receptors results in activation of JAK kinases and receptor phosphorylation. Phosphorylated cytokine receptors recruit STAT proteins, which are then phosphorylated by the activated JAK kinases. Phosphorylated STAT proteins form homo- and hetero-dimers that translocate into the nucleus and function as transcription factors.This JAK1 substrate peptide contains an N-terminal Glycine-residue and a phospho-tyrosine-residue.

Nimesulide is a non-steroidal anti-inflammatory drug that is used to treat acute pain and primary dysmenorrhea. This drug is also a cyclooxygenase inhibitor and works by targeting a range of key mediators of the inflammatory process such as histamines and free radicals to reduce pain and inflammation. Nimesulide is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Irinotecan hydrochloride trihydrate is a topoisomerase I inhibitor that is used as chemotherapy drug for colorectal cancer. By inhibiting topoisomerase I, Irinotecan hydrochloride trihydrate prevents the replication of DNA in cells, and stops the cancer cells from growing and dividing. When used for chemotherapy, Irinotecan hydrochloride trihydrate is usually part of combination therapy with other chemotherapy drugs, such as 5-fluorouracil (5-FU) and leucovorin for other cancers. Irinotecan hydrochloride trihydrate is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Cyclooxygenase inhibitor; anti-inflammatory; antipyretic; analgesic

Indirubin is a chemical compound that belongs to the indole family. It has been studied for its anti-inflammatory and antipyretic properties. Research suggests that Indirubin can inhibit certain kinases displaying antineoplastic properties. Indirubin is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Cyclosporin B is an antifungal and immunosuppressive cyclic peptide, which is derived from the fungus *Tolypocladium inflatum*. The compound is a member of the cyclosporin family, characterized by cyclic polypeptides with a unique arrangement of amino acids that enable its biological activity. Though its precise mode of action is not completely delineated, it is observed to influence cell growth and viability by potentially disrupting cellular communication or signal transduction pathways. Cyclosporin B is primarily used in scientific research due to its complex interactions with cellular processes, offering insights into fungal growth mechanisms and immune modulation. While it is not as commonly applied as Cyclosporin A in therapeutic contexts, its distinctive bioactivity makes it a subject of interest for studies in pharmacology and toxicology. Researchers explore its potential applications in discovering novel antifungal strategies and understanding immune response pathways.

An inhibitor of caspase-1 and active metabolite of VX-765. Blocks lipopolysaccharide-mediated release of cytokines. Suppresses release of interleukins IL-1β and IL-18. Reduced inflammatory cytokines, such as IL-1α, tumor necrosis factor-α, IL-6 and IL-8, observed in in vivo models of rheumatoid arthritis and skin inflammation.

Inhibitor of ataxia telangiectasia mutated (ATM) kinase and AKT kinase with anti-cancer activity. ATM is a nuclear protein kinase and a signal transducer sensing DNA damage as well as controlling double strand DNA break (DSB) repair. It is a radiotherapy and chemotherapy sensitizer, especially in tumors sensitive to DNA alkylating agents (such as temozolomide). Moreover, KU 55933 inhibits phosphorylation of cytoplasmic AKT kinase, downregulates synthesis of cyclin D1 and induces cell cycle arrest in G1 phase.

Substrate peptide for protein tyrosine phosphatase 1B (PTP1B)- an ubiquitously expressed non-receptor tyrosine phosphatase. PTP1B negatively regulates signalling pathways controlling metabolic homeostasis, cell proliferation and immunity (such as leptin and insulin receptor signalling), making PTP1B an interesting target for type 2 diabetes mellitus (T2DM) and obesity treatment. PTP1B also has important leptin-independent metabolic effects, playing a critical role in the regulation of inflammation, cell proliferation, differentiation and invasion. Therefore PTP1B is also interesting as a therapeutic target for inflammatory and autoimmune diseases and cancer.-For application data please see: Figure 2 supplement 1C.

Inhibitor of COX-1 and COX-2 cyclooxygenases

Inhibitor of protein kinase CK2

Inhibits RNAPII-mediated trasncription; immunosuppressant; anti-inflammatory

A potent selective inhibitor of cGMP-specific phosphodiesterase type 5 (PDE-5), thereby reducing the degradation rate of cGMP. Sildenafil is used to treat erectile dysfunction and pulmonary arterial hypertension. Sildenafil citrate is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Metformin is a widely used anti-hyperglycemic (anti-diabetic) agent for the treatment of type 2 diabetes mellitus. This is due to it decreasing blood glucose by decreasing hepatic glucose product by activation of the AMP-activated protein kinase AMPK. Studies have also demonstrated Metformin to have anti-cancer activity, attributed to several mechanisms such as inhibition of mammalian target of rapamycin (mTOR), cancer stem cells and inflammation. Metformin HCl is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

BRK tyrosine kinase (PTK6) inhibitor; anti-proliferative in breast cancer cells

DARKtide is a substrate peptide for death-associated protein kinase (DAPK) for use in kinases assays. DAPK is involved in several cellular pathways including: apoptosis, tumour suppression, stress response, anti-viral immunity and IL-1-associated inflammatory diseases. In C. elegans DAPK-1 regulates epidermal morphogenesis, innate immunity and wound repair.

Proteosome inhibitor; antineoplastic

Loxoprofen is a non-steroidal anti-inflammatory drug that belongs to the group of propionic acid derivatives. It can be used for the treatment of pain and inflammation associated with osteoarthritis, rheumatoid arthritis and other musculoskeletal disorders. Its therapeutic effects are attributed to inhibition of cyclooxygenases 1 and 2 (COX-1 and COX-2) enzymes. Loxoprofen sodium is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Inhibitor of CSF1R receptor

Inhibitor of Janus kinase JAK-1

GC 376 is an inhibitor of the main protease Mpro (3CLpro) in coronaviruses as well as picornaviruses. This broad-spectrum antiviral compound has been used as investigational veterinary drug for treatment of feline infectious peritonitis virus (FIPV) infections. Recent studies also showed that GC 376 inhibits the main protease Mpro (3CLpro) from SARS-CoV-2 with IC50 of 0.03 μM and EC50 of 3.37 μM.

Selective and potent inhibitor of lysine acetyltransferases KAT6A and KAT6B with IC50 values of 8 nM and 28 nM, respectively. The compound is a reversible competitor of acetyl coenzyme A domain of KAT6A/B enzymes. It inhibits MYST-catalysed histone acetylation and potentiates senescence in vitro and in zebrafish model of hepatocellular carcinoma. The compound opened the door to a new class of cancer therapeutics that could potentially direct the cancer cells in senescence or permanent dormancy.

Potent inhibitor of dual specificity tyrosine-phosphorylation-regulated kinase 3 (DYRK3) with IC50 value of 0.7 nM. Elevates hemoglobin and platelet levels in anemic mice.

Tacrolimus is a calcineurin inhibitor drug that is used for the prevention of rejection after an organ transplant. This drug can also be used in the treatment of severe atopic dermatitis. Tacrolimus’ mechanism of action is not well known however it is understood that this drug inhibits T-lymphocyte activation by binding to an intracellular protein called FKBP-12. This drug also has anti-inflammatory properties. Tacrolimus is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Diflunisal is a nonsteroidal anti-inflammatory drug (NSAID), which is a synthetic derivative of salicylic acid. It is primarily sourced through chemical synthesis rather than extraction from natural elements. Diflunisal functions by inhibiting the cyclooxygenase (COX) enzymes, specifically COX-1 and COX-2, which play a crucial role in the biosynthesis of prostaglandins. This inhibition results in reduced production of prostaglandins, compounds involved in inflammation and pain signaling pathways. The primary applications of Diflunisal are in the management of mild to moderate pain and inflammatory conditions. It is often utilized in the treatment of conditions such as osteoarthritis and rheumatoid arthritis. Its analgesic properties make it effective for addressing musculoskeletal pain and postoperative discomfort. Due to its mechanism of action, Diflunisal provides anti-inflammatory, analgesic, and antipyretic effects, which can be beneficial in clinical settings where inflammation and pain management are critical. However, its usage must be monitored due to potential side effects associated with NSAID use, such as gastrointestinal irritation and cardiovascular risks. Scientists continue to explore various applications and improve the therapeutic index of Diflunisal through modified formulations and targeted delivery approaches.

Inhibitor of chymotrypsin

Inhibitor of poly (ADP-ribose) polymerase enzyme; antineoplastic

Lisinopril is a drug that belongs to the group of angiotensin converting enzyme (ACE) inhibitors. It is used to treat hypertension, heart failure and myocardial infarction. Lisinopril binds to the active site of the ACE enzyme, preventing it from converting angiotensin I into angiotensin II. (S)-Lisinopril is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Sitagliptin is a drug that can be used to treat type 2 diabetes. This drug increases the production of an incretin hormone called glucagon-like peptide-1 (GLP-1) by stimulating the GLP-1 receptor. Sitagliptin is used in combination with metformin or a thiazolidinedione to improve glycemic control in patients with type 2 diabetes mellitus. Sitagliptin has been shown to improve postprandial blood glucose levels and reduce the risk of cardiovascular events. It also reduces the incidence of myocardial infarction and congestive heart failure in patients with type 2 diabetes who are already at high risk for these conditions. Sitagliptin phosphate monohydrate is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Seratrodast is a thromboxane receptor antagonist that is used to treat asthma. However, this drug does not affect thrombus formation as other thromboxane synthase inhibitors do such as ozagrel. Seratrodast is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Proprotein convertase subtilisin/kexin type 9 (PCSK9) is negative regulator of hepatic low-density lipoprotein (LDL) receptors by promoting their degradation. This leads to an increase in plasma levels of cholesterol-LDL (LDL-c). PCSK9 binds to the LDL receptor at the epidermal growth factor precursor homology domain A (EGF-A) which leads the receptor to be targeted for degradation. Natural loss of function mutations in PCSK9 have been linked to improved coronary health and lower cholesterol levels with reduced risk of coronary heart disease. This has led to further study to find inhibitors of PCSK9 with the hope that they may be clinically relevant in the future.As discussed, PCSK9 binds to EGF-A on the LDL receptor. A peptide named pep 2-8 is a mimic of EGF-A and binds PCSK9 in the same manner observed with the LDL receptor. Pep 2-8 is a potent selective competitive inhibitor of PCSK9. Pep 2-8 restores LDL receptor function and LDL uptake of PCSK9-treated HepG2 cells. This is still an active area of research to optimise inhibition of PCSK9 for cholesterol regulation.Pep 2-8 has also been utilised as an anchor peptide in phage-display experiments to bind an extension peptide library to the groove site.Peptide Ac-TVFTSWEEYLDWV-NH2 is a Research Peptide with significant interest within the field academic and medical research. This peptide is available for purchase at Cymit Quimica in multiple sizes and with a specification of your choice. Recent citations using Ac-TVFTSWEEYLDWV-NH2 include the following: LDL-R promoting activity of peptides derived from human PCSK9 catalytic domain (153-421): design, synthesis and biochemical evaluation RH Alghamdi, P O'Reilly, C Lu, J Gomes - European journal of , 2015 - Elsevierhttps://www.sciencedirect.com/science/article/pii/S0223523415000422 Biological characterization of computationally designed analogs of peptide TVFTSWEEYLDWV (Pep2-8) with increased PCSK9 antagonistic activity C Lammi, J Sgrignani , A Arnoldi , G Grazioso - Scientific reports, 2019 - nature.comhttps://www.nature.com/articles/s41598-018-35819-0 Computational design and biological evaluation of analogs of lupin peptide p5 endowed with dual pcsk9/hmg-coar inhibiting activity C Lammi, EMA Fassi, J Li , M Bartolomei, G Benigno - Pharmaceutics, 2022 - mdpi.comhttps://www.mdpi.com/1999-4923/14/3/665 Molecular dynamics insights on the role beta-augmentation of the peptide N-terminus with binding site beta-hairpin of proprotein convertase subtilisin/kexin 9 B Pasam, KM Medicherla , RS Rathore - Chemical Biology & , 2019 - Wiley Online Libraryhttps://onlinelibrary.wiley.com/doi/abs/10.1111/cbdd.13612

Simvastatin Na is the salt form of Simvastatin. It acts as HMG-CoA reductase inhibitor and suppresses TNF-mediated NF-kappaB activation.

Gastric proton pump inhibitor

Pemetrexed is a chemotherapy drug that belongs to the class of drugs called folate antimetabolites. It is used for the treatment of various cancers such as non-small cell lung cancer and pleural mesothelioma. Pemetrexed targets the enzymes thymidylate synthase, dihydrofolate reductase and glycinamide ribonucleotide formyltransferase. The drug works by inhibiting those enzymes so that the formation of DNA and RNA is prevented. Pemetrexed is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Aurora kinase inhibitor; antineoplastic

This peptide is phosphorylated by Janus kinase 1 (JAK1) and is an ideal substrate for use in kinase assays. The JAK family of kinases is essential for the signalling of a host of immune modulators in tumour, stromal, and immune cells where they are highly expressed. JAK family proteins mediate the signalling of the interferon (IFN), IL-6, and IL-2 families of cytokines.JAK kinases are associated with cytokine receptors. Cytokine binding to these receptors results in activation of JAK kinases and receptor phosphorylation. Phosphorylated cytokine receptors recruit STAT proteins, which are then phosphorylated by the activated JAK kinases. Phosphorylated STAT proteins form homo- and hetero-dimers that translocate into the nucleus and function as transcription factors.This JAK1 substrate peptide contains an N-terminal glycine-residue.

Sphingosine is a sphingolipid that can be found in human cells and plays an important role in signal transduction. Sphingosine is synthesized by the enzyme sphingosine kinase from sphinganine, which is a product of the breakdown of phospholipids. It also has a basic structure that can be used to inhibit the activity of protein kinases, such as PKC and Src, and tumor necrosis factor alpha. Sphingosine is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Inhibitor of caspases; broad spectrum

Inhibits interaction between small GTPase Rab27a and its effector JFC1 (synaptotagmin-like protein1, Slp1). These proteins regulate neutrophil exocytosis, decrease neutrophil infiltration in liver and kidneys and reduce extracellular ROS production by NAPDH oxidase. Thus, nexinhibib20 suppresses systemic inflammation.

Pentoxifylline is a methylxanthine derivative that is used to treat intermittent claudication that is caused by chronic occlusive arterial disease of the limbs. This drug also has antioxidant and anti-inflammatory properties. Pentoxifylline is a phosphodiesterase inhibitor aiding to increase levels of cAMP. Pentoxifylline is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

PD 168393 is a potent and selective irreversible inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It is synthesized through advanced chemical processes, designed to specifically target and covalently modify the ATP-binding site of EGFR. The mode of action involves the irreversible binding to the cysteine residue in the ATP-binding pocket, leading to the inhibition of EGFR autophosphorylation and subsequent downstream signaling pathways. PD 168393 is primarily utilized in cancer research to investigate the role of EGFR in tumor development and progression. By effectively inhibiting EGFR activity, it serves as a valuable tool in studying the biological processes regulated by EGFR, as well as in the development of therapeutic strategies targeting EGFR-driven malignancies. Researchers apply PD 168393 in both in vitro and in vivo models to elucidate the mechanisms of action, resistance, and potential combination therapies in oncology.

Potent and specific inhibitor of the tyrosine protein kinase Mer precursor (MERTK) with 38-fold selectivity over the FMS-like protein kinase FLT3. UNC 4203 inhibits MERTK with an IC50 value of 2.4 nM and shows favourable pharmacokinetic properties. In vivo experiments in mice showed that UNC 4203 dramatically decreased the phosphorylation of MERTK in bone marrow leukemia cells.

Arbutin or alpha-arbutin is a natural product. It is a hydroquinone glucoside with antioxidant properties. It is widely used in cosmetics as depigmenting agent, acting as an inhibitor of tyrosinase in melanocytes. Arbutin acts by supressing the enzymes that stimulate these melanocytes without killing or fully inhibiting them. As a consequence, melanin production is decreased to avoid hyperpigmentation that might be caused by an excess of UV radiation or a higher activity of tyrosinases.

Inhibitor of HIF prolyl hydroxylase

An inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase that reduces total cholesterol and low-density lipoprotein (LDL). Cerivastatin is cardioprotective and anti-atherosclerotic. Cerivastatin inhibits the expression of the atherosclerotic genes monocyte chemoattractant protein-1 (MCP-1) and C-C chemokine receptor type 2 (CCR2), whilst inducing the expression of Kruppel-like factor 2 (KLF2).

Pamidronic acid is a bisphosphate used in the treatment of Paget’s disease, osteolytic bone lesions and in the treatment of hypercalcemia of malignancy. This drug inhibits farnesyl diphosphate and induces apoptosis of hematopoietic tumor cells. Pamidronic acid sodium salt hydrate is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Inhibitor of CKD1, CDK2, and CDK4 serine/threonine kinases

N-alpha-Benzoyl-L-argininamide is a synthetic compound that is used as an enzyme inhibitor. It binds to the active site of proteases, thereby inhibiting their activity. This drug has been shown to inhibit the activities of phosphodiesterase and phosphatase enzymes in vitro. N-alpha-Benzoyl-L-argininamide also inhibits the proteolytic degradation of hippuric acid and casein in vitro. The binding affinity for this drug is due to its structural similarity with substrates such as glutamate and rhizosphere exudates.

Pemetrexed is an antifolate drug that is used to treat mesothelioma and non-small cell lung cancer. It is used during chemotherapy and sometimes used in conjunction with cisplatin. This drug disrupts folate-dependent metabolic activities essential for cell replication. In vitro studies have shown that Pemetrexed inhibits thymidylate synthase. Pemetrexed disodium salt is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Inhibitor of myosin?II?specific ATPase which blocks the myosin heads in an actin-detached state, disrupts contractility of myosin-actin filaments and stabilizes super-relaxed state of muscle fibres. It inhibits skeletal muscle myosin, non-muscle myosin II and heart muscle myosin.

This product is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Inhibitor of 8-oxoguanine DNA glycosylase OGG1 with IC50 of 0.059 μM and excellent specificity over other DNA repair enzymes. OGG1 and its substrate 8-oxoguanine are involved in mutagenesis, genotoxicity, inflammation and cancer. The compound can cause accumulation of 8-oxoguanine in DNA in vitro and is a potent tool for the study of OGG1 biology.

Dual COX/5-LO inhibitor; anti-inflammatory; analgesic

Inhibitor of LRRK2 kinase

Inhibits MET, VEGFR1, VEGFR2; VEGFR3 receptor tyrosine kinases; antineoplastic

Linagliptin is a dipeptidyl peptidase-4 inhibitor drug that is used to manage hyperglycaemia in patients with type 2 diabetes. This drug works by inhibiting the enzyme dipeptidyl peptidase-4 and allows for the breakdown of GLP-1 and glucose dependent insulinotropic polypeptide. As a result of this, breakdown of glycogen is reduced and release of insulin is increased. Linagliptin is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Masitinib is an orally bioavailable inhibitor of c-Kit, PDGFR and FGFR3 tyrosine. It is an antineoplastic which has been studied for applications in a range of human diseases including Alzheimers and cancer and is currently used to treat mast cell tumours in animals. As part of a screening study, Masitinib was shown to be highly effective in blocking SARs-CoV-2 replication.

ERKtide Substrate Peptide.

Inhibitor of activin receptor-like kinases (ALK4, ALK5 and ALK7), members of TGFβ type I receptor family. Blocks activin- and TGFβ-mediated signaling and phosphorylation of Smad2 downstream. Suppresses tumor-promoting and tumor-suppressing effects of TGFβ. Promotes differentiation of human embryonic stem cells (hESCs), whilst sustaining mouse ESCs in the undifferentiated state.

Competitive inhibitor of ceramide-glycosyltransferase used for substrate reduction therapy in lysosomal storage disorders. It inhibits glucosylceramide synthase, which catalyses the initial step in glycosphingolipid biosynthetic pathway. This compound delays the onset of symptoms in type 1 Gaucher disease, Sandhoff disease and Tay-Sachs disease. It also reduces brain abnormalities in mucolipidosis type IV.

Neuronal selective nitric oxide synthase inhibitor