Modulateurs d'enzymes

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

Tirofiban is a platelet aggregation inhibitor drug that is used for the prevention of thrombotic events in acute coronary syndrome. This drug is an antagonist of fibrinogen and inhibits it from binding to the glycoprotein IIb/IIIa receptor. As a result of this, Tirofiban blocks the blood from clotting during a cardiovascular event. Tirofiban HCl 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.

Inhibitor of HMG-CoA reductase

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.

A potent ATP-competitive inhibitor of tropomyosin-related kinases (TRK1, TRK2 and TRK3), members of the receptor tyrosine kinase family of neurotrophin receptors. Tumors with oncogenic TRK fusions are sensitive to larotrectinib, leading to reduced proliferation and tumor growth in patients with soft tissue sarcoma, triple-negative breast cancer and lung cancer.

Sunitinib is a tyrosine kinase inhibitor drug. It is a drug that is used as a treatment for renal cell carcinoma, gastrointestinal stromal tumor, and other solid tumors. This drug inhibits tyrosine kinases such as VEGFRs, this prevents tumour growth and pathologic angiogenesis. Sunitinib base 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.

Sorafenib is a drug that belongs to the class of multikinase inhibitors. It inhibits a number of kinases, including the Mcl-1 protein, which is involved in apoptosis along with blocking picolinic acid (PA), an endogenous metabolite involved in apoptosis signal transduction. Sorafenib also binds to epidermal growth factor receptor (EGFR) on the surface of cancer cells, inhibiting the production of proteins that are required for angiogenesis, thus blocking the formation of new blood vessels. Sorafenib may also inhibit P-glycoprotein (Pgp) activity. Overall, these cytotoxic effects give Sorafenib anti-tumor properties, inhibiting angiogenesis and cellular transformation, which are the two main processes of tumor growth and metastasis. Sorafenib tosylate has been shown to be effective against a range of solid tumors such as breast, prostate and lung cancers and is also used for the treatment of metastatic colorectal cancer and renal cell carcinoma. A combination therapy group found that sorafenib was more effective when used with interferon alfa-2b for the treatment of advanced renal cell carcinoma. Sorafenib also has the potential for drug interactions with other drugs that are metabolized by cytochrome P450 enzymes.