Modulateurs d'enzymes

Antirheumatic; immunosuppressant; neuroprotective; neuroregenerative

Inhibitor of AKR1C3 (type 5 17β-hydroxysteroid dehydrogenase)

Inhibitor of VEGFR; antineoplastic

Moclobemide is a monoamine oxidase inhibitor that is used to treat major depressive disorder and dipolar disorder. This drug’s mechanism of action involves the reversible inhibition of the enzyme MAO-A. The inhibition of this enzyme results in a decreased metabolism and destruction of neurotransmitters thus relieving the symptoms of depression and bipolar disorder. Moclobemide 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 novel survivin suppressant with an IC50 of 0.54 nM for the negative regulation of the survivin promoter.

Multi-kinase inhibitor; inhibits epoxide hydrolase; antineoplastic

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.

JAK3 enzyme inhibitor

Ibandronate is a bisphosphate used in the treatment of osteoporosis in postmenopausal women. This drug slows down the activity of osteoclasts resulting in a slower process of bone breakdown. This drug also inhibits farnesyl diphosphate and induces apoptosis of hematopoietic tumor cells. Ibandronate sodium salt 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.

Inhibits c-MET tyrosine kinases

Amino acids 359-409 of human glycogen synthase kinase 3 β (GSKβ), a multifunctional serine/threonine kinase widely expressed in most mammalian cells. GSKβ is highly active under basal conditions and acts downstream of phosphoinositide 3-kinase (PI3K) signalling. PI3K activation results in Akt phosphorylation and the subsequent phosphorylation of GSKβ at serine-9 and its inactivation. GSKβ in turn activates the production of pro-inflammatory cytokines including IL-1β, IL-6, IL-12, IL-17, TNFalpha and IFNγ, and supresses the production of IL-10, IL-1Ra, and IFNβ by immune cells. Under resting conditions, GSKβ is constitutively active due to tyrosine-216 phosphorylation, and it phosphorylates and inhibits a diverse group of pro-oncogenic substrates, such as: β-catenin- cyclin D1- c-Jun- c-Myc and CREB. GSKβ is also involved in Wnt signalling pathways.Aberrant expression of GSKβ has been shown to promote cell growth in some cancers and to suppress it in others. GSKβ inhibition leads to the accumulation of β-catenin in the nucleus, enhancing the progression of many cancers. However the inhibition of GSKβ also induces apoptosis in various types of cancers, such as pancreatic, colorectal and bladder cancer. Inhibition of GSKβ can also have neuroprotective effects on dopaminergic neurons such as in Parkinson's disease.

Inhibits non-receptor tyrosine kinase BTK; antineoplastic

Inhibits multiple receptor tyrosine kinases (RTKs), including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl. Sitravatinib inhibits proliferation of sarcoma cells and reduced tumor growth in vivo. Promotes immune response in tumor microenvironment and enhances sensitivity to immune checkpoint inhibitors. This compound is undergoing several clinical trials as a potential anti-cancer therapeutic agent.

A selective inhibitor of PI3Kα. Inhibits cancer cell proliferation by blocking the G0/G1 phase of the cell cycle. Anti-tumor effect of BYL 719 has been demonstrated in models of tumors with PI3KCA mutation and amplification in vivo. BYL 719 also suppresses tumor growth in pre-clinical models of osteosarcoma.

Inhibits isocitrate dehydrogenase 1 (IDH-1) harbouring a gain of function mutation at R132, which causes impaired cellular differentiation via epigenetic modulation. By inhibiting mutant IDH1, synthesis of oncometabolite 2-hydroxyglutarate is reduced. This compound therefore has therapeutic potential in solid and haematological malignancies, such as acute myeloid leukemia (AML).

Inhibitor of acetylcholinesterase

Inhibitor of cytochrome P450; inhibitor of prostaglandin synthesis

Epalrestat is a carboxylic acid derivative that is used for the treatment of diabetic neuropathy. This drug is an aldose reductase inhibitor and aims to reduce the accumulation of intracellular sorbitol. Studies in rats have shown this drug to improve morphological abnormalities of nerves. Epalrestat 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 inhibitor of EGFR with sensitizing and T790M resistance mutations, selective over the wild-type form of the receptor. Causes tumour regression in EGFR mutant T790M transgenic and xenograft models in vivo.

Inhibitor of metalloendopeptidase neprilysin