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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Heat Shock Protein (HSP)-VER-49009
VER-49009

Chemical Structure : VER-49009

CAS No.: 558640-51-0

VER-49009 (CCT0129397)

货号: PC-49669Not For Human Use, Lab Use Only.

VER-49009 (CCT0129397, VER49009) is a potent, selective small-molecule inhibitor of Hsp90 with IC50 of 25 nM and Kd value of 78 nM, inhibits ATPase activity of full length yeast Hsp90 protein with IC50 of 0.14 uM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

VER-49009 (CCT0129397, VER49009) is a potent, selective small-molecule inhibitor of Hsp90 with IC50 of 25 nM and Kd value of 78 nM, inhibits ATPase activity of full length yeast Hsp90 protein with IC50 of 0.14 uM.
VER-49009 caused significant reduction in cellular levels of Raf-1, and the client protein CDK4.
VER-49009 potently inhibits HCT116 cell proliferation with GI50 of 0.26 uM.
VER-49009 caused induction of HSP72 and HSP27 alongside depletion of client proteins, including C-RAF, B-RAF, and survivin, and the protein arginine methyltransferase PRMT5.
VER-49009 exhibited mean cellular antiproliferative GI(50) values of685 nM against a human cancer cell line panel, induced cell cycle arrest and apoptosis.

物理化学性质&存储条件

分子量 387.82
分子式 C19H18ClN3O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-(5-Chloro-2,4-dihydroxyphenyl)-N-ethyl-4-(4-methoxyphenyl)-1H-pyrazole-3-carboxamide

参考文献

1. Dymock BW, et al. J Med Chem. 2005 Jun 30;48(13):4212-5.

2. Sharp SY, et al. Mol Cancer Ther. 2007 Apr;6(4):1198-211.

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