Modulateurs d'enzymes

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