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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Heat Shock Protein (HSP)-VWK147
VWK147

Chemical Structure : VWK147

CAS No.:

VWK147 (VWK-147)

货号: PC-25911Not For Human Use, Lab Use Only.

VWK147 is a specific second-generation small-molecule inhibitor targeting HSP90 CTD dimerization, induces cell death in cisplatin-sensitive and resistant UC cells (UCCs), and re-sensitizes resistant cells to cisplatin treatment.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

VWK147 is a specific second-generation small-molecule inhibitor targeting HSP90 CTD dimerization, induces cell death in cisplatin-sensitive and resistant UC cells (UCCs), and re-sensitizes resistant cells to cisplatin treatment.
VWK147, but not the N-terminal domain-targeting HSP90 inhibitor 17-AAG, in combination with mTOR inhibitors synergistically kills cisplatin-sensitive and -resistant UCCs.
VWK147 interacts with helices H4 and H5 of the CTD in a manner that would prevent CTD dimerization.
VWK147 destabilizes HSP90 client proteins in urothelial carcinoma cells but does not induce a heat shock response.
VWK147 induces LC3-II accumulation and inhibits autophagosome-lysosome fusion.
VWK147 induces conjugation of ATG8 proteins to single membranes (CASM).

物理化学性质&存储条件

分子量 674.72
分子式 C32H38N10O7
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-amino-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. David C, et al. Cell Death Dis. 2025 Dec 23. doi: 10.1038/s41419-025-08330-4.

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