Modulateurs d'enzymes

Camostat is a serine protease inhibitor that is used for the treatment of chronic pancreatitis. This drug has shown to reduce inflammation and pain. Studies have shown that Camostat has also inhibited the entry of SARS-CoV-2 in lung cells by inhibiting the priming process of S-protein, necessary for the viral entry into host cells. Camostat mesylate 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.

Used for treatment of idiopathic pulmonary fibrosis

Inhibitor of glutathione peroxidase GPX4

A novel non-covalent inhibitor of the PLpro protease from SARS-CoV-2 and SARS-CoV viruses. GRL 0617 inhibits the proteolytic processing of the viral polypeptide. As PLpro also acts as a protease in pathways involved in innate immunity, there are indications that it can promote immunity against the virus.

Potent and selective GSK3-β inhibitor, with IC50 value of 48 nM. Increases Nanog expression and regulates self-renewal in murine embryonic stem cells (ESCs). Induces reprograming of induced pluripotent stem cells (iPSCs) to derive cells from specific lineages.

HMG-CoA reductase inhibitor; anti-hypercholesterolemia agent

Rapamycin is a macrolide antibiotic that has been studied as a potential anticancer agent. It binds to FK506 binding proteins (FKBPs) to form a complex that inhibits mammalian targets of rapamycin (mTOR). Rapamycin also blocks p70 S6 kinase activation by interleukin-2 and thereby inhibits proliferation of T cells. It induces differentiation of human pluripotent stem cells (hPSCs) to mesendoderm and blood progenitor cells.

AZD 1152 is an Aurora kinase inhibitor, which is a type of small-molecule therapeutic agent. It is derived from the pharmaceutical research conducted by AstraZeneca. Its primary mode of action involves the selective inhibition of Aurora B kinase, an enzyme crucial for the regulation of mitosis. By interfering with this enzyme, AZD 1152 disrupts the normal progression of cell division, leading to the inhibition of proliferation and induction of apoptosis in rapidly dividing cells. The compound has been primarily investigated for its applications in oncology, where abnormal Aurora kinase activity is commonly associated with tumorigenesis and cancer progression. AZD 1152 has shown promise in preclinical and clinical studies for the treatment of various malignancies, including acute myeloid leukemia and solid tumors. Its ability to selectively target cancer cells while sparing normal cells makes it a valuable candidate for combination therapies aimed at enhancing anti-cancer efficacy while minimizing toxicity.

Sumoylation inhibitor; reported to inhibit histone acetylation transferase

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.

Selective inhibitor of the Src kinase family with subnanomolar IC50 values and good selectivity over c-Abl, PDGFRα and c-Kit kinases. The compound is effective in inhibiting growth in drug resistant cancer cell lines. In a recent study, it inhibited the growth of HER2-positive breast cancer cell lines which were resistant to pan-HER family kinase inhibitors such as lapatinib.

Tegafur is an antineoplastic agent that is used for the treatment of gastric and colorectal cancers in combination with other medications. This drug is a prodrug of 5-fluorouracil and has anticancer properties by inhibiting thymidylate synthase during DNA synthesis. Additionally, Tegafur causes disruptions of RNA functions. Tegafur 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 factor Xa

Cyclin-dependent kinases (CDKs) are a family of kinases that regulate the cell cycle and gene transcription. Cyclin-dependent kinase 7 (CDK7) forms a trimeric complex with cyclin H and MAT1, which functions as a Cdk-activating kinase (CAK) and promotes cell cycle progression. CDK7 is an essential component of the transcription factor TFIIH, involved in DNA repair. CDK7 is also implicated in mRNA processing, transcription activation, pause induction, and pause release.CDK8 associates with the mediator complex and regulates transcription via several mechanisms, including influencing binding of RNA polymerase II to the mediator complex. CDK8 phosphorylates the Notch intracellular domain, SREBP, and STAT1. Its regulatory subunit is cyclin C. CDK9 is a component of the TAK/P-TEFb complex, which phosphorylates the part of RNA polymerase II. Its regulatory subunit is cyclin T or cyclin K. CDK9 interacts with HIV-1 Tat protein and TRAF2, and is involved in the differentiation of skeletal muscle.CDKs are often over expressed in cancers and may correlate with poor prognosis. This peptide is based on the C-terminal of RNA polymerase II and is used in kinase assays.

Selective inhibitor of the platelet derived growth factor receptor PDGFRβ with IC50 value of 4.2 nM. JNJ 10198409 inhibits the PDGFRβ kinase activity and its downstream signalling leading to anti-proliferative and anti-angiogenic effects, which were confirmed in various tumoral cell lines.

Dexrazoxane is a cytoprotective drug that is used in chemotherapy to provide cardio-protection against anthracycline toxicity. It is an antimitotic agent with immunosuppressive properties. Dexrazoxane works by binding to iron in the cell, preventing it from being released. Dexrazoxane is also a catalytic inhibitor of topoisomerase II. Dexrazoxane 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 FLT3 and AXL tyrosine kinases

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 tosylate also has the potential for drug interactions with other drugs that are metabolized by cytochrome P450 enzymes. Sorafenib tosylate 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 peptide is phosphorylated by Janus kinase 2 (JAK2) 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.

Anastrozole is a non-steroidal drug that belongs to the class of aromatase inhibitors. It inhibits the production of estrogen by blocking the conversion of androgens to estrogens in peripheral tissues. The drug has been shown to be effective in treating breast cancer in postmenopausal women. In vitro assays have shown that Anastrozole can inhibit tumor growth as well as induce apoptosis in human serum cells, which suggests that it may be effective against a variety of cancers. Anastrozole 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.