Enzyme Modulators

Carmofur is an antineoplastic agent that is used to treat various cancers such as breast and colorectal cancer. This drug is a derivative of fluorouracil. Carmofur is an inhibitor of the human acid ceramidase, a lysosomal amidase involved in the development of cancer cells. Carmofur 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.

HMG-CoA reductase inhibitor

Inhibitor of Abl and Src kinases; anti-proliferative; antineoplasticÂ

Toceranib phosphate is a receptor tyrosine kinase inhibitor. Toceranib phosphate has been shown to be effective in the treatment of skin cancer and other types of cancer, including lung cancer and breast cancer. It is approved in the US as a treatment for canine mastocytoma (mast cell tumours).  Toceranib phosphate 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.

LRRKtide (also called moesin) is a peptide substrate for leucine-rich repeat kinase 2 (LRRK2). The sequence of LRRKtide has been derived from the ERM proteins: Ezrin (amino acids 561-573), radixin (amino acids 558-570) and moesin (amino acids 539-553). These proteins influence cytoskeletal dynamics by anchoring the cytoskeleton to the plasma membrane. LRRK2 phosphorylates LRRKtide at its Thr558 site. This peptide contains the phosphorylated threonine residue.LRRK2 is a large, ubiquitous protein of unknown function. LRRK2 has GTPase and kinase activity, and is located in multiple areas of the cell, associated with intracellular membranes and vesicular structures- suggesting LRRK2 may be involved in several cellular pathways. LRRK2 is also found in most organs and mutations in LRRK2 have been identified in Parkinson's disease.The threonine residue at position 9 of this peptide has been phosphorylated.

Potently inhibits PARP-1 and PARP-2 enzymes, orally bioavailable and crosses blood-brain barrier. Sensitises cancer cells to DNA-damaging chemotherapy and radiotherapy. Combination therapies investigated in clinical trials for solid and blood malignancies.

Selective, potent, competitive and reversible inhibitor of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) with IC50 of 2.3 nM and more than 10000-fold selectivity over the related 11β-HSD-2 isoform. BMS 823778 inhibits conversion of cortisone in cortisol and has applications in the treatment of diabetes type 2 since it can influence the occurrence of insulin resistance.

Atorvastatin is an HMG-CoA reductase inhibitor which is used to lower lipid levels and to reduce the risk of cardiovascular disease. This drug belongs to the class of medicines called statins. It lowers abnormal levels of cholesterol and lipids to reduce the risk of cardiovascular disease by inhibiting the enzyme HMG-CoA. Atorvastatin sodium 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.

mTOR serine/threonine kinase inhibitor

Selective c-Met kinase inhibitor

Cerivastatin is a drug that belongs to the class of drugs called statins. This drug is used to reduce the risk of cardiovascular events and lower lipid levels. Cerivastatin is an HMG-CoA reductase inhibitor and allows for a decrease in cholesterol in hepatic cells. Cerivastatin is cardioprotective and anti-atherosclerotic. Cerivastatin 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.

Leflunomide is a pyrimidine synthesis inhibitor drug that is used to treat rheumatoid arthritis. Although its mechanism of action is not fully determined, this drug has shown to interfere with cell cycle progression by inhibiting dihydroorotate dehydrogenase and has shown antiproliferative activity. As a result of this, it interferes with the expansion of activated autoimmune lymphocytes. Additionally, Leflunomide is a tyrosine kinase inhibitor. Leflunomide 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 EIF2AK3/PERK kinases

Specific inhibitor of glycogen synthase kinase 3 (GSK-3) with IC50 in low nanomolar range. Studies showed that BIO maintains self-renewal in embryonic stem cells (ESCs) as well as increases activity of β-catenin. In neonatal cardiomyocytes, BIO promotes cell cycle by stimulating cell entry into S phase as well as cytokinesis. In germline stem cells from female mice (FGSCs), BIO promoted proliferation and maintenance of FGSCs by activating β-catenin and up-regulating E-cadherin.

Perindopril t-butylamine salt inhibits the angiotensin converting enzyme (ACE) to prevent the conversion of angiotensin I to angiotensin II. When used in drug formulations, it has been shown to decrease blood pressure in patients with congestive heart failure. Perindopril also has an effect on the renin-angiotensin system, which regulates blood pressure and fluid homeostasis by promoting vasoconstriction and increasing salt and water retention. Perindopril t-butylamine 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.

Sildenafil is a pharmaceutical compound, which is a synthetic product derived from chemical processes. It functions as a selective inhibitor of the enzyme phosphodiesterase type 5 (PDE5). By inhibiting PDE5, sildenafil increases cyclic guanosine monophosphate (cGMP) levels within the smooth muscle cells of the corpus cavernosum. This leads to smooth muscle relaxation and vasodilation, allowing increased blood flow and facilitating penile erection in the presence of sexual stimulation. Primarily, sildenafil is used in the treatment of erectile dysfunction (ED) and is also prescribed for pulmonary arterial hypertension under different brand names. The compound's efficacy in treating ED arises from its ability to enhance the natural erectile response to sexual arousal by modulating the nitric oxide-cGMP pathway, crucial for vascular regulation. Published studies have demonstrated its effectiveness and safety profile, making it a widely utilized therapeutic option in clinical settings. The pharmacokineteics of sildenafil underscore its relevance by ensuring rapid absorption and a preferable half-life, which defines its dosage regimen and therapeutic window.

Brain-penetrant inhibitor of anaplastic lymphoma kinase (ALK) and proto-oncogene kinase ROS1. It is a reversible ATP-competitor, interacting with P-loop (L1122, G1123, V1130) and K1150 residue of ALK tyrosine kinase. It has major implications in the treatment of non-small cell lung cancer (NSCLC). The compound is used for resensitization of drug resistant, ALK-mutated cancers to crizotinib chemotherapy and was shown to trigger the regression of EML40ALK-driven brain metastases.

Inhibitor of beta-lactamase enzymes

Inhibitor of COX-2 and PDE4 enzymes; NSAID of coxib class

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.

Etodolac is a non-steroidal anti-inflammatory drug (NSAID) used to treat osteoarthritis and rheumatoid arthritis. It is also used to treat acute pain. This drug works by inhibiting prostaglandin synthesis from the inhibition of the enzyme cyclooxygenase. Etodolac 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 multiple protein kinases, such as PKC and FLT3

AKTide-2T is a 14-mer peptide which has the ability to bind to the substrate binding domain of Akt1 with a Ki of 12mM. AKt1 is part of the Akt kinase family which are serine/threonine kinase and it is ubiquitously expressed. AKt1 performs roles such as promoting endothelial neoplasms and through phosphorylating angiogenic substrates AKt1 plays a role in angiogenesis. AKT kinases as a whole perform functional roles in cell proliferation, cell growth, survival and intermediary metabolism.During peptide library screening, AKTide-2T was found to contain the optimal motif for successful binding to AKT. When phosphoamino acid analysis of AKTide-2T was carried out it was observed that although AKTide-2T contained two potential AKT phosphorylation sites: serine or threonine, AKT only phosphorylated the serine site. Furthermore it was found that AKTide-2T exhibits properties of being a competitive inhibitor for example it competitively inhibits histone H2B from being phosphorylated by AKT.

Inhibitor of cyclin-dependent kinases CDK4 and CDK6

Inhibitor of β-lactamase enzymes

HMG-CoA reductase inhibitor

Letrozole is an aromatase inhibitor drug that is used in the treatment of breast cancer in postmenopausal women. It is a non-steroidal type II inhibitor that blocks the active site and thus blocking the electron transfer chain of CYP19A1. As a result of this, the conversion of androgen to estrogen is inhibited. Letrozole 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.

Mevastatin is a drug that inhibits the synthesis of cholesterol and has been used to treat hypercholesterolemia. It binds to the hydroxyl group at position 3 on the mevalonate molecule, which prevents the formation of 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) and consequently reduces the production of cholesterol. Mevastatin has been shown to inhibit mitochondrial functions in wild-type strain yeast cells and myeloma cell lines, which may be due to receptor activity. Mevastatin 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.

Omeprazole is a proton pump inhibitor (PPI) that inhibits the production of gastric acid in the stomach. This is due to Omeprazole binding through a stable disulphide bond to the H+/K+ ATPase enzyme found on parietal cells, and preventing hydrogen ion transport. Consequently, gastric acid secretion is supressed. As a PPI, Omerprazole can be used to treat disorders where gastric acid is over-secreted. Examples of these disorders are gastroesophageal reflux disease (GERD) and peptic ulcer disease. Omeprazole sodium 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.

Potent, selective and cell-permeable tool for modulation of O-GlcNAcylation. Ac4GlcNAcF3 is a dual modulator of O-GlcNAc transferase (OGT) and O-GlcNAcase (OGA). Ac4GlcNAcF3 perturbates the GlcNAc cycling as OGT can incorporate GlcNAcF3 onto proteins but subsequently, it cannot be removed by OGA. In a mouse embryogenic fibroblast cell line, Ac4GlcNAcF3 increased the level of protein O-GlcNAcylation.

MK 886 is a leukotriene antagonist that has been studied for use in treating atherosclerosis. This drug inhibits the 5-lipoxygenase activating protein thus inhibiting 5-lipoxygenase. MK 886 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.

Autocamtide-3-related inhibitory peptide is a calmodulin-dependent protein kinase II (CaMKII) inhibitor. AC3-I is derived from Autocamtide-3, a substrate for CaMKII, with the Thr-9 phosphorylation site substituted with Ala.CAMK represents a class of Ca2+/calmodulin-dependent protein kinase enzymes. CAMKs are activated by increases in the concentration of intracellular calcium ions (Ca2+) and transfers phosphates from ATP to defined serine or threonine residues in other proteins. Activated CAMK is involved in the phosphorylation of transcription factors and therefore, in the regulation of expression of responding genes.

Inhibits VEGFR1, VEGFR2, VEGFR3, c-kit and PDGFR tyrosine kinases

Mitochondrial division inhibitor (mdivi-1) inhibits dynamin related protein-1 (drp1)-dependent mitochondrial fission. It is a therapeutic candidate for the treatment of stroke, myocardial infarction and neurodegenerative disease. The neuroprotective effects of mdivi-1 has been demonstrated in various models of brain ischemia and neurodegeneration.

EGFR tyrosine kinase inhibitor; pro-apoptotic; antiproliferative in cancer cells

Cis/trans-form of GK 563 [2351820-19-2]

Selective and potent inhibitor of 8-oxoguanine DNA glycosylase OGG1 with IC50 of 0.6 μM. OGG1 is a key enzyme in DNA repair mechanism called base excision repair (BER). The compound inhibits the hydrolysis of glycosidic bond required for the excision of 8-oxoguanine from double stranded DNA, which leads to accumulation of mutations. It has been proposed as monotherapy for certain types of cancers as well as adjuvant for cancer therapy with DNA damaging agents. It has potential to sensitize tumours for chemotherapy and inhibit development of drug resistance mechanisms.

Ibrutinib is a small-molecule inhibitor of Bruton’s tyrosine kinase, a crucial enzyme to the B-cell receptor pathway. Bruton’s tyrosine kinase becomes continuously activated in B-cell cancers and therefore promotes the survival of tumor cells. Ibrutinib binds irreversibly and covalently to a cysteine residue within the ATP-binding site of the enzyme, thus preventing ATP binding and downstream signal transduction. The ability of Ibrutinib to inhibit Bruton’s tyrosin kinase and hence the B-cell receptor pathway it can be used in the treatment of some B cell cancers such as diffuse large B-cell lymphoma (DLBCL) and chronic lymphocytic leukemia (CLL). Ibrutinib 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.

5-HT6 serotonin receptor antagonist; anti-convulsant

Angiotensin-converting enzyme inhibitor; anti-hypertensive

Lestaurtinib is a multitarget tyrosine kinase inhibitor of the JAK, FLT-3 and TrkA families of tyrosine kinases at nanomolar concentrations. It inhibits proliferation and induces apoptosis in vitro. Lestaurtinib is a FDA approved orphan drug for acute myeloid leukemia.

Cyclosporin A (CsA) is a cyclic undecapeptide that is extracted from the fungus Tolypocladium inflatum. CsA is used as an immunosuppressive drug to prevent rejection of transplanted organs and to treat autoimmune diseases such as rheumatoid arthritis and psoriasis. CsA works by binding to a protein called cyclophilin D, which is a component of the enzyme calcineurin. Calcineurin is an important enzyme involved in the activation of immune cells, and by binding to cyclophilin D, CsA inhibits its activity. This leads to the inhibition of T-cell activation and the suppression of the immune response. Cyclosporin A has has been rpeorted to exhibit some nephrotoxicity, hypertension and also increases the risk of infections and tumors when used in transplantation Cyclosporin 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.

Aldose reductase AKR1B10 inhibitor; hepatotoxic

γ-secretase inhibitor; inhibits notch signaling

Inhibitor of angiotensin-converting enzyme

Inhibitor of protein kinase CK1

Vildagliptin is an antihyperglycemic agent that is used for the management of type 2 diabetes mellitus. This drug is a dipeptidyl peptidase 4 inhibitor and prevents the degradation of glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). This leads to improved glycemic control. Vildagliptin 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.

Forskolin is a compound derived from the medicinal plant Coleus forskohlii. As an activator of adenylate cyclase, Forskolin causes increases cellular levels of cAMP, and can be used in cell physiology research. It also has antihypertensive, platelet aggregation inhibitory and smooth muscle relaxant effects. Forskolin 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 protein kinases; induces apoptosis; anti-cancer

Specific inhibitor of Rho-associated ROCK kinases which supresses tumour cell invasion and affects cell proliferation, differentiation and motility. The compound competes with ATP for binding to the kinase catalytic site and inhibits phosphorylation of ROCK substrates. This inhibitor was also shown to attenuate neuronal death after transient retinal ischemia and to possess protective effects on human embryonic stem cells.

IBMX is a competitive non-selective phosphodiesterase inhibitor that raises cAMP and activates PKA. It also inhibits TNFα and leukotriene synthesis. This chemical compound reduces inflammation and is an adenosine receptor antagonist. IBMX 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.

Nabumetone is a non-steroidal anti-inflammatory drug that is used in the treatment of osteoarthritis and rheumatoid arthritis. This drug is also a cyclooxygenase inhibitor and works by inhibiting this enzyme so that pain and inflammation is reduced. Nabumetone 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.

Azathioprine belongs to the group of immunosuppressant drugs that suppress the immune system by inhibiting the production of white blood cells (leukocytes). It is used to treat inflammatory diseases, such as rheumatoid arthritis, lupus, and Crohn's disease. Azathioprine is metabolized in the liver. Additionally, this drug inhibits DNA synthesis by binding to nuclear DNA, preventing RNA transcription and protein synthesis in susceptible cells. Azathioprine 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.

Rofecoxib is a non-steroidal anti-inflammatory drug that is used to treat osteoarthritis, acute pain and migraine attacks. This drug is also a COX-2 inhibitor. As a result, it reduces inflammation and pain. Rofecoxib 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.

Potent and specific inhibitor of checkpoint kinase CHK2 with IC50 of 3 nM. CCT 241533 binds to the ATP pocket of CHK2 and shows minimal cross-reactivity against related kinases. CCT 241533 blocked the activity of CHK2 and impaired DNA repair in response to DNA damage in human tumoral cell lines. The compound did not potentiate genotoxicity of several genotoxic compounds but it did potentiate the cytotoxicity of a PARP inhibitor olaparib.

Orlistat is a drug that has been approved for the treatment of obesity. It inhibits gastric and pancreatic lipases, which are enzymes that break down dietary fats into smaller molecules to facilitate absorption. Orlistat has been shown to reduce coronary heart disease in patients with type 2 diabetes. Orlistat has also been shown to have a significant upregulation of gene expression associated with disease activity when injected into the skin of patients with primary pulmonary hypertension. Orlistat 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.

MET tyrosine kinase inhibitor; anti-proliferative; pro-apoptotic

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.

Axltide-is a substrate peptide for use in kinase assays and is based on the mouse insulin receptor substrate 1 (IRS1) (amino acid 979-989).IRS1 is a membrane-proximal adaptor protein, which binds to, and is phosphorylated by, the insulin receptor (IR) at its tyrosine residue. IRS1 transmits the extracellular signal for insulin to serine/threonine kinases, such as Akt which then deliver the signal into the cell to mediate the various actions of insulin.

Inhibitor of TGF-α, CTGF, ERK1/2, NF-κB and FasL; anti-inflammatory

Cyclosporine U is a cyclic polypeptide immunosuppressant, which is a derivative of the natural product Cyclosporine A, produced by the fermentation process involving the filamentous fungus *Tolypocladium inflatum*. It primarily acts by inhibiting the activity of calcineurin, a phosphatase enzyme, which in turn blocks the transcription of interleukin-2 and other cytokines. This mechanism suppresses the activation of T-lymphocytes, a crucial component in the immune response. Cyclosporine U is employed extensively in clinical settings to prevent organ rejection in transplant patients by modulating the immune response. It is also utilized in the treatment of various autoimmune diseases such as psoriasis and rheumatoid arthritis, where the immune system mistakenly attacks the body’s own tissues. Despite its clinical significance, careful monitoring of blood concentrations is essential due to its narrow therapeutic index and the potential for nephrotoxicity and other adverse effects. The development and refinement of derivatives like Cyclosporine U continue to be an active area of research aimed at enhancing efficacy and reducing side effects.

RIPK2 protein kinase inhibitor; EGFR inhibitor

Autocamtide-2-related inhibitory peptide is a calmodulin-dependent protein kinase II (CaMKII) inhibitor.CAMK represents a class of Ca2+/calmodulin-dependent protein kinase enzymes. CAMKs are activated by increases in the concentration of intracellular calcium ions (Ca2+) and transfers phosphates from ATP to defined serine or threonine residues in other proteins. Activated CAMK is involved in the phosphorylation of transcription factors and therefore, in the regulation of expression of responding genes.

Topoisomerase II inhibitor; chemotherapeutic drug

COX-2 enzyme inhibitor; anti-inflammatory

Inhibitor of topoisomerase TOP2

TAS 6417 hydrochloride is a small-molecule inhibitor, which is synthesized via chemical processes in pharmaceutical research. It functions primarily as a potent and selective inhibitor of specific mutant forms of the epidermal growth factor receptor (EGFR). By targeting these EGFR mutations, TAS 6417 hydrochloride disrupts the signaling pathways that are crucial for the proliferation and survival of cancer cells. The compound is primarily utilized in the context of scientific research for understanding and developing targeted cancer therapies, particularly in relation to non-small cell lung cancer (NSCLC). Researchers employ TAS 6417 hydrochloride to investigate the biochemical pathways and to test its efficacy and safety in preclinical models. The inhibitor's ability to target specific mutations positions it as a valuable tool in elucidating the mechanisms of resistance and sensitivity in cancer treatment strategies.

Inhibitor of 3β-hydroxysteroid dehydrogenase in steroid biosynthesis

Cyclooxygenase inhibitor; NSAID; an opthalmic analgesic

Inhibits FGFR family of kinases; antineoplastic; anti-angiogenic

Inhibitor of monoamine oxidase; anti-bacterial agent

Inhibitor of metalloendopeptidase neprilysin

Inhibitor of acetylcholinesterase

Inhibits tankyrase (TNKS1 and TNKS2 with IC50 values of 11 and 4 nM respectively), by binding to the catalytic poly-ADP-ribose polymerase (PARP) domain. This stabilizes cytoplasmic protein Axin, mediating β-catenin depletion and thereby suppresses Wnt signalling pathway. XAV 939 has anti-proliferative and pro-apoptotic effects on neuroblastoma and colorectal cancer cells.

Potent and selective inhibitor of histone deacetylase 6 (HDAC6) with IC50 of 2.4 nM. Its anti-inflammatory activity was examined in a mouse model for acute colitis. The compound protected from intestinal inflammation by prevention of infiltration of CD19+ B-cells into the lamina propria of colonic epithelium and attenuated neutrophil activation. Its broad anti-inflammatory response involved decrease in 24 inflammatory chemokines and cytokines. Also, it is a potent inhibitor of cell proliferation in pancreatic cancer cell lines.

COX1 inhibitor; blocker of Ca2+-activated non-selective cation channels

Glucokinase activator

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.  Fluvastatin 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.

Casein kinase (CK1ε and CK1Ύ) inhibitor

p38α MAP kinase inhibitor; JNK2α2 protein kinase inhibitor

Celecoxib is a pyrazole derivative that acts as a selective COX-2 inhibitor. It has been shown to inhibit prostaglandin synthesis and promote apoptosis in human osteosarcoma cells. Celecoxib also inhibits tumor growth and inhibits angiogenesis in combination with paclitaxel, which is a chemotherapeutic agent. It is a nonsteroidal anti-inflammatory drug, thus a beneficial treatment in conditions such as rheumatoid arthritis, osteoarthritis, musculoskeletal pain, acute pain and juvenile rheumatoid arthritis. Furthermore it can be utilized in patients with familial adenomatous polyposis to reduce colon and rectal polyps. Celecoxib 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 COX1 cyclooxygenase

Lifirafenib is a targeted anticancer therapy, which is a small molecule inhibitor sourced through pharmaceutical development processes. Its mode of action involves the selective inhibition of the RAF kinase family, including B-RAF, which plays a critical role in the MAPK/ERK signaling pathway. By targeting these kinases, Lifirafenib effectively disrupts the aberrant signaling that contributes to tumor growth and survival in certain cancers with mutations such as BRAF V600E. Lifirafenib is primarily used in the treatment of cancers with identified aberrations in the RAS/RAF/MEK/ERK pathway, including certain forms of melanoma and thyroid and colorectal cancers. This drug holds therapeutic potential due to its ability to target specific genetic alterations, thereby providing a more personalized approach to cancer treatment. As with other targeted therapies, Lifirafenib is subject to ongoing clinical trials to better understand its efficacy, tolerability, and broader applications across various oncological indications.

MAP kinase kinase (MEK) inhibitor. Binds to MEK-1, preventing phosphorylation and activation by Raf or MEK kinase. PD 098059 enhances self-renewal in stem cells. Has anti-growth and anti-proliferative effects on AML cells. Anti-apoptotic effect on AML cells observed in synergy with Nutlin-3a.

Lenvatinib is a tyrosine kinase inhibitor that is used to treat cancers such as solid tumours. This drug inhibits the activity of VEGR receptors. It also inhibits other receptors such as fibroblast growth factor. Lenvatinib 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.

Inhibitor of stearoyl-CoA desaturase SCD1 with IC50 of 6.3 nM, as measured in the SCD1-expressing human microsomes.  A 939572 exhibited anticancer activity as it reduced cell proliferation and triggered cell killing in human non-small cell lung carcinoma cells. A 939572 inhibited tumour growth in an in vivo model for gastric carcinoma and reduced the oleic acid:stearic acid ratio in mouse liver and plasma.

Inhibitor of ecto-ATPase which blocks the hydrolysis of nucleoside diphosphates and triphosphates in extracellular space. The compound inhibits NTPDase1, NTPDase 3, NTPDase 8 and NPP1and prolongs the effect of ATP on purinergic P2 receptors in environment with physiological concentrations of nucleotides. The compound has variable effectiveness as ecto-ATP inhibitor in mouse, rat, human and guineia pig tissues.

A potent Met kinase inhibitor (IC50 = 3.9 nM). Also inhibits Axl, Ron, and Tyro-3 (IC50 = 1.1, 1.8 and 4.3 nM, respectively). Anti-proliferative in Met-driven tumors in vitro and in vivo. Induces polyploidy in breast cancer cells and thereby chemoresistance.

Inhibitor of EGFR, HER2 and HER4 tyrosine kinases

Simvastatin is a lipid-lowering agent that belongs to the group of statins. It is prescribed for the treatment of hypercholesterolemia, coronary heart diseases, and other conditions related to high cholesterol levels. Simvastatin inhibits the production of 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) reductase, an enzyme involved in the synthesis of cholesterol. Simvastatin 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.

Rivastigmine is a cholinergic agent that is used in the treatment of dementia in Parkinson’s and Alzheimer’s disease. This drug is a carbamate derivative that binds to and inactivates cholinesterase such as acetylcholinesterase and butyrylcholinesterase. This leads to an increase concentration of acetylcholine at cholinergic synapse. Rivastigmine tartrate 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.

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.

VEGFR2 a tyrosine kinase receptor inhibitor; antineoplastic

Bestatin is a competitive protease inhibitor. It inhibits aminopeptidase N and is being studied for the use and treatment for acute myelocytic leukemia. Bestatin 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.

Etoricoxib is a cyclooxygenase-2 (COX-2) inhibitor, which is a type of nonsteroidal anti-inflammatory drug (NSAID). It works by blocking the enzyme COX-2 that is involved in the production of certain hormones called prostaglandins. These hormones are involved in the inflammation (swelling and heat) associated with conditions such as arthritis. By blocking the action of the COX-2 enzyme, Etoricoxib reduces the production of prostaglandins and thus, reduces the inflammation and pain. Etoricoxib 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.

Nilotinib is a kinase inhibitor that is used for the treatment of Chronic Myeloid Leukemia (CML). This drug is also used for the treatment of CML that is resistant to imatinib. Nilotinib inhibits the tyrosine kinase activity of the BCR-ABL protein. It also inhibits PDGFR and c-kit. Nilotinib 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.