WS6 is a novel small molecule that promotes β cell proliferation in rodent and human primary islets with EC50 of 0.28 uM(R7T1 cell viability).EC50 value: 0.28 uM Target: β cell proliferation agonistin vitro: WS6 induced up to 4% of rat β cells to proliferate, with an EC50 of 0.4 μM. In the same format, WS6 also induced 3% of human β cells to proliferate, with a similar potency to the rat β cells. WS6 induced R7T1 proliferation in dose response, with EC50 value of 0.28 μM, Proliferatio
p21-activated kinase 1 (PAK1) is a member of a family non-receptor serine/threonine kinases that are vital to normal cell function. Binding of various upstream partners to PAK1 results in release of an autoinhibitory domain that blocks activity of the kinase domain. PAK1 expression and activity is upregulated in several human cancers and is a potential therapeutic target for cancer intervention. IPA-3 is a cell-permeable allosteric inhibitor of PAK1 that is non-competitive with respect to ATP binding (IC50 = 2.5 μM). It does not, however, inhibit the activity of PAK1 that has been pre-activated with Cdc42. IPA-3 binds covalently to the PAK1 regulatory domain (apparent Kd = 1.9 uM) and prevents binding to the upstream activator Cdc42.[Cayman Chemical]
Tie2 kinase inhibitor
Tunica interna endothelial cell kinase 2 (Tie2, also known as angiopoietin-1 receptor or tek) is an endothelium-specific receptor tyrosine kinase important for the development of embryonic vasculature and for angiogenesis and vascular maintenance in adult tissues. Tie2 kinase inhibitor reversibly and selectively blocks Tie2 kinase activity with an IC50 value of 250 nM. It is 200-fold more potent for inhibition of Tie2 compared to p38. Tie2 kinase inhibitor has been shown to reduce angiogenesis in a Matrigel neovascularization assay and to delay tumor growth in MOPC-315 plasmacytoma and SVR angiosarcoma xenograft models.[Cayman Chemical]
CYP3cide is a potent and selective time dependent inactivator of Cytochrome P450 3A4 (CYP3A4). CYP3A4 is an important enzymes involved in the metabolism of xenobiotics in the human body and constitutes to about a quarter of all CYPs in the human body. CYP3cide provides a useful in vitro tool in defining the individual roles of CYP3A4 versus CYP3A5 in the metabolism of drugs.
It is a cytotoxic nitrogen mustard derivative widely used in cancer chemotherapy. It cross-links DNA, causes strand breakage, and induces mutations. Its clinical activity is associated with a decrease in aldehyde dehydrogenase 1 (ALDH1) activity. This substance is listed as a known human carcinogen.
Noditinib-1 is a potent and selective inhibitor of NOD1-induced NF-κB activation. Mutations in NOD proteins have been associated with various inflammatory diseases and Noditinib-1 shows promise as a potential therapeutic agent.
[4-[(4-Benzo[b]thien-2-yl-2-pyrimidinyl)amino]phenyl][4-(1-pyrrolidinyl)-1-piperidinyl]-methanone is a potential novel IκB kinase 2 (IKK2) inhibitor used in the treatment of various immune/inflammatory disorders.
N-(3-Chlorophenyl)-2-pyridinecarboxamide shows positive allosteric modulation at the mGlu4 receptors in combination with other antagonists resulting in treatment for the neurodegenerative Parkinson’s disease.
Small molecule inhibitors are a type of molecules that can interact with proteins and reduce the biological activity of target proteins, including enzyme inhibitors, transcription factor inhibitors, and ion channel blockers. It acts on popular signaling pathways, popular targets and popular research fields: MAPK, PI3K, JAK / STAT and other signaling pathways, HDAC, Aurora kinase, CDK and cell cycle regulators, integrase / protease, etc. Research fields such as epigenetics, CNS, GPCR, anti-virus, antibacterial / anti-inflammatory. It is an effective tool for cell biology research.