Modulateurs d'enzymes

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