Modulateurs d'enzymes

Inhibitor of glycogen synthase 3 (GSK-3) and cyclin-dependent kinases CDK1, CDK2 and CDK5. Kenpaullone can substitute transcription factor Klf4 in reprogramming of fibroblast to induced pluripotent stem cells when using the method of ectopic expression of transcriptional factors. In an in vitro model for Alzheimer’s disease, kenpaullone decreased production of amyloid beta peptides Aβ40 and Aβ42.

Rosuvastatin is a drug that belongs to the group of statins. It is used for the treatment of high cholesterol and as an adjunct therapy for patients with coronary heart disease. Rosuvastatin reduces serum cholesterol by inhibiting HMG-CoA reductase, which is the rate-limiting enzyme in the production of cholesterol. Furthermore, this drug has been shown to have anti-inflammatory properties, which may be due to its ability to inhibit prostaglandin synthesis. Rosuvastatin calcium 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.

Doxorubicin hydrochloride is an inhibitor of topoisomerase II with anti-neoplastic activity and belongs to the class of anthracyclines. It is cytotoxic, and interferes with the topoisomerase II-mediated repair of DNA causing accumulation of mutations. Doxorubicin also leads to the generation of reactive oxygen species (ROS), which further damages DNA as well as proteins and membranes. Doxorubicin is used as a chemotherapy treatment for various types of cancer, including breast cancer, lung cancer, ovarian cancer, and leukaemia. However, the compound presents with a risk of developing cardiomyopathy as well as drug resistance. Doxorubicin hydrochloride 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 PDE4 enzyme; anti-inflammatory

Thalidomide is a piperidinyl isoindole drug that is used to treat various cancers such as myeloma and erythema nodosum leprosum. This drug is immunosuppressive and has anti-angiogenic activity. Thalidomide’s mechanism of action is not fully understood however it is thought to block the activity of tumor necrosis factor-alpha (TNF-α). (+/-)-Thalidomide 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.

Ebselen is a non-toxic organoselenium compound with antioxidant, anti-inflammatory and cytoprotective properties. Ebselen is an inhibitor of lipoxygenases, nitric oxide (NO) synthases, protein kinase C, H+/K+-ATPase, thioredoxin reductase and NADPH oxidase. Recently, ebselen has been identified by several studies as a covalent inhibitor of the main protease Mpro from coronaviruses. For the SARS-CoV-2 main protease Mpro, the IC50 value is 0.67 μM and EC50 is 4.57 μM.

Lenvatinib is an anti-cancer drug that is a multi-kinase inhibitor for VEGFR1, VEGFR2 and VEGFR. It has been shown to be effective against several cancers such as thyroid cancer and is currently in clinical trials for the treatment of leukaemia and prostate cancer. Furthermore, Lenvatinib also inhibits the activity of other protein kinases, including those involved in inflammatory responses. Lenvatinib 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.

5-Fluorouracil is a cytotoxic drug that inhibits the synthesis of DNA. It is used in combination therapy to treat cancer and is a pyrimidine analog. This drug inhibits the formation of thymidylate synthase from uracil. As a result, this leads to DNA and RNA synthesis inhibition and cell death. 5-Fluorouracil 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.

Protein kinase B (also known as RAC-alpha serine/threonine-protein kinase: Atk) is a serum and glucocorticoid-regulated protein kinase with three highly homologous isoforms (Akt1, 2 and 3). Akt1 and Akt3 are the predominant isoforms expressed in the brain, whereas Akt2 is mainly expressed in skeletal muscle and embryonic brown fat. These proteins play major regulatory roles in a range of physiological processes including: growth, proliferation, cell survival, angiogenesis, metabolism and Akt is also considered a proto-oncogene.This peptide (AKTide) is a selective substrate for these kinases and enables quick, easy and sensitive assays of Akt activity.

Inhibitor of HMG-CoA reductase

A potent and selective inhibitor of cell death-inducing kinase RIP2 (IC50 = 5 nM). Reduces release of pro-inflammatory cytokines. Inhibits production of TNF-α and IL-6 in intestinal explants from patients with Crohn's disease and ulcerative colitis.

Multi-kinase inhibitor; inhibits epoxide hydrolase; antineoplastic

Fosinopril belongs to the angiotensin-converting enzyme (ACE) inhibitor class of drugs, which prevents the conversion of angiotensin I to angiotensin II. This leads to decreases in blood pressure and slows down the progression of kidney disease, hypertension and heart failure. Fosinopril 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.

Inhibitor of EGFR (ErbB1) and HER2 (ErbB2) receptor tyrosine kinases. Used for sensitization of HER2-overexpressing cancer cells to radiation as well as chemotherapy to tamoxifen- and trastuzumab-resistant cell lines. The compound blocks signalling via Akt and mitogen-activated protein kinase (MAPK) pathways leading to reduced cell survival. In trastuzumab resistant cancer cells, it inhibits HER2 phosphorylation, prevents receptor ubiquitination and causes accumulation of inactive HER2 dimers on the cell surface.

Inhibitor of tyrosinase in melanocytes: skin whitener

Potent inhibitor of histone deacetylase 6 (HDAC6), inducing elevated levels of acetylated α-tubulin. It inhibits pro-inflammatory cytokines TNF-α and IL-6 as well as nitric oxide secretion in human and murine macrophages. It is not neurotoxic and it rescues cognitive impairment in mice model for Alzheimer’s disease.

Cobicistat is an inhibitor of human cytochrome P450 3A enzymes (CYP) with no antiviral activity. Cobicistat is used in the treatment of HIV-1 infection, as an alternative to ritonavir, to increase the half-life of antiviral medications (von Hentig, 2016). Cobicistat acts as a booster by selectively inhibiting the hepatic degradation of the drugs, for example, in the pharmacological regime against HIV-1, which often includes protease inhibitors, such as, darunavir, atazanavir, and lopinavir, or the integrase inhibitor elvitegravir (Deeks, 2014).

Inhibitor of HIF-prolyl hydroxylase isozymes PHD1, PHD2 and PHD3 with Ki in nanomolar range. The compound mimics the binding of N-oxalylglycine, chelates catalytic iron and prevents substrate entry into catalytic site. Inhibition of PHD enzymes leads to stabilization of hypoxia-induced factors HIF1α and HIF2α, followed by the production of erythropoietin (EPO).

Gemcitabine is as a synthetic pyrimidine nucleoside prodrug. The hydrogen atoms on the 2' carbon of deoxycytidine are replaced by fluorine atoms. Gemcitabine works by being incorporated into the DNA of cancer cells during replication and inhibiting DNA synthesis. First gemcitabine is converted into its active form, gemcitabine triphosphate, by cellular enzymes including deoxycytidine kinase (DCK), after it is taken up by cancer cells. The gemcitabine triphosphate interferes with the normal functioning of the enzymes involved in replicating DNA, leading to the termination of DNA synthesis and ultimately, cell death. Gemcitabine is used as a chemotherapy drug used to treat various types of cancer, including pancreatic, lung, breast, and ovarian cancer. Gemcitabine 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 pan-Raf kinases