跳至主要内容

A major introduction to VER-155008!

VER-155008 is an adenosine-derived inhibitor of heat shock protein 70 (Hsp70; IC50 = 0.5 μM) tIt targets the nucleotide-binding domain (NBD) of Hsp70 and similarly binds the NBDs of Hsp70 cognates Hsc70 (Ki = 10 μM) and glucose-regulated protein 78 (Grp78; KD = 80 nM).hat is selective over Hsp90. VER-155008 inhibits the proliferation of human breast and colon cancer cell lines, inducing apoptosis or caspase-independent cell death. It induces the proteasome-dependent degradation of Hsp
90 client proteins and potentiates the apoptotic activity of Hsp90 inhibitors.

评论

发表评论

此博客中的热门博文

Custom Synthesis

MuseChem engages in total-support business for research and development of organic compounds for the chemical, pharmaceutical and agrochemical industries. We provide custom manufacturing and process research services on scales ranging from milligrams to kilograms. MuseChem’s scientists in the chemistry team are well trained, can handle even the most complex chemical synthesis and characterization projects, completing the project on your required timeframe. Your inquiry will b e evaluated within a few days to provide you with a quote complemented by a synthetic scheme. The quote is calculated on the basis of the current FTE rate. We deliver detailed biweekly reports with expected delivery dates. Each project is treated under the confidentiality agreement. We won't charge our clients for failed syntheses. We offer high-quality and cost-effective custom synthesis service under strict confidentiality including the following: ● Small-Scale and large scale manufacturing ● Process dev...
发表评论
阅读全文

AP-III-a4 hydrochloride((ENOblock HCl) )|Musechem

AP-III-a4 hydrochloride((ENOblock HCl) )| Musechem ENOblock Hcl(AP-III-a4 Hcl) is a novel small molecule which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity (IC50=0.576 uM); inhibit cancer cell metastasis in vivo.  Enolase is a component of the glycolysis pathway and a “moonlighting” protein, with important roles in diverse cellular processes that are not related to its function in glycolysis. However, small molecule tools to probe enolase function have been restricted to crystallography or enzymology. In this study, we report the discovery of the small molecule “ENOblock”, which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity. ENOblock was isolated by small molecule screening in a cancer cell assay to detect cytotoxic agents that function in hypoxic conditions, which has previously been shown to induce drug resistance. Further analysis revealed that ENOblock can inhibit cancer cell met...
发表评论
阅读全文

GW590735 CAS No. : 622402-22-6 is in stock now!

GW590735 is a potent and selective agonist of PPARα with an EC50 value of 4 nM for the expression a GAL4-responsive reporter gene and at least 500-fold selectivity versus PPARγ and PPARδ. GW590735 significantly increased HDL cholesterol, decreased LDL and VLDL cholesterol, and significantly reduced triglycerides. Maximal increases in HDL cholesterol were 37%, 53%, and 84% with fenofibrate, torcetrapib, and GW590735, respectively.
发表评论
阅读全文