Hsp90 inhibitor 5b

Chemical Structure : Hsp90 inhibitor 5b

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货号: PC-72333Not For Human Use, Lab Use Only.

Hsp90 inhibitor 5b is a first-in-class, small molecule inhibitor of the C-terminal (CTD) Hsp90 dimerization with KD of 3.42 uM, IC50 of 1.3 uM against leukemia cell line K562.

规格	价格	库存	数量
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

Hsp90 inhibitor 5b is a first-in-class, small molecule inhibitor of the C-terminal (CTD) Hsp90 dimerization with KD of 3.42 uM, IC50 of 1.3 uM against leukemia cell line K562.
Hsp90 inhibitor 5b inhibits Hsp90 chaperone function, does not show any interaction with the NTD of Hsp90.
Hsp90 inhibitor 5b down-regulated the phospho-BCR-ABL1 and total-BCR-ABL1 levels, as well as the related downstream signaling pathways, additionally reduced the expression of client proteins associated with Hsp90 chaperone activity, involving Akt, Stat5, and c-Myc.
Hsp90 inhibitor 5b inhibited leukemic cell lines (K562, KCL22 and HL60) proliferation and induced apoptosis in a caspase 3/7 enzyme-dependent assay.
Hsp90 inhibitor 5b is effective against resistant leukemia cells and in the zebrafish xenotransplantation model.

物理化学性质&存储条件

分子量	778.827
分子式	C39H42N10O8
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-benzamido-N-(1-(sec-butyl)-2-((1-isobutyl-2-(methylcarbamoyl)-6-oxo-1,6-dihydropyrimidin-5-yl)carbamoyl)-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(4-methoxybenzyl)-6-oxo-1,6-dihydropyrimidine-2-carboxamide

参考文献

1. Sanil Bhatia, et al. ACS Cent Sci. 2022 May 25;8(5):636-655.