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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Heat Shock Protein (HSP)-DDO-5936
DDO-5936

Chemical Structure : DDO-5936

CAS No.: 2355377-13-6

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DDO-5936 (DDO5936)

货号: PC-73076Not For Human Use, Lab Use Only.

DDO-5936 (DDO5936) is a cell-active, specidic small-molecule inhibitor of Hsp90-Cdc37 protein-protein interaction (PPI) without ATPase inhibition, binds to Hsp 90 with Kd of 3.86 uM.

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5 mg ￥1280 In stock
10 mg ￥1980 In stock
25 mg ￥3580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

DDO-5936 (DDO5936) is a cell-active, specidic small-molecule inhibitor of Hsp90-Cdc37 protein-protein interaction (PPI) without ATPase inhibition, binds to Hsp90 with Kd of 3.86 uM.
DDO-5936 exhibits little effect on Hsp90 ATPase activity, DDO-5936 targets a surface binding site on Hsp90 to inhibit the Hsp90-Cdc37 PPI.
DDO-5936 binding affinity was remarkably decreased for the E47A mutant (KD> 100 μM) and moderately lower for the R46A mutant (KD =6.53 μM) and Q133A mutant (KD=5.18 μM).
DDO-5936 represses cell proliferation through a strong correlation with the Hsp90-Cdc37 expression level, and selectively down-regulates kinase clients of Hsp90, arrests the cell cycle in HCT116 cells in a Cdc37-dependent manner.
DDO-5936 (50-100 mg/kg, ip) dose-dependently impairs the growth of xenografted HCT116 cells in nude mice.

物理化学性质&存储条件

分子量 495.598
分子式 C25H29N5O4S
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

N-(mesitylsulfonyl)-N-(4-((2-(pyrrolidin-1-yl)pyrimidin-4-yl)amino)phenyl)glycine

参考文献

1. Lei Wang, et al. Sci Adv. 2019 Sep 18;5(9):eaax2277.

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