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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Heat Shock Protein (HSP)-HVH-2930
HVH-2930

Chemical Structure : HVH-2930

CAS No.:

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HVH-2930 (HVH2930)

货号: PC-22212Not For Human Use, Lab Use Only.

HVH-2930 is a specfiic small molecule C-terminal HSP90 inhibitor with SPR KD of 97.2 uM (HSP90α), reduces cell viability and induces apoptosis in HER2-positive breast cancer cells, targets the C-terminal HSP90 without inducing heat shock response (HSR).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

HVH-2930 is a specfiic small molecule C-terminal HSP90 inhibitor with SPR KD of 97.2 uM (HSP90α), reduces cell viability and induces apoptosis in HER2-positive breast cancer cells, targets the C-terminal HSP90 without inducing heat shock response (HSR).
HVH-2930 effectively inhibited the activity of C-terminal HSP90 by competitively interfering with the binding capability of the co-chaperone PPID, similar to the well-characterized C-terminal HSP90 inhibitor novobiocin.
HVH-2930 dose-dependently reduces cell viability in both trastuzumab-sensitive [BT474 and SKBR3] and -resistant cells [JIMT-1 and MDA-MB453] with IC50 of 6.86 μM, 5.13 μM, 3.94 and 3.93 μM, respectively.
HVH-2930 shows much more higher affinity than novobiocin.
HVH-2930 is a potent C-terminal hHSP90 inhibitor because it not only inhibits the binding of ATP but also stabilizes its open conformation.
HVH-2930-induced apoptosis is accompanied by activation of effector caspases and mitochondrial dysfunction.
HVH-2930 suppresses the HER2 signaling pathway by degrading HSP90 clients.
HVH-2930 inhibits tumor growth of trastuzumab-resistant JIMT-1 xenografts, attenuates CSC-like properties in HER2-positive breast cancer cells.

物理化学性质&存储条件

分子量 488.63
分子式 C29H36N4O3
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-methoxy-2,2-dimethyl-N-(3-methyl-1-(2-(1-methylpiperidin-4-yl)ethyl)-1H-indazol-6-yl)-2H-chromene-6-carboxamide

参考文献

1. Minsu Park, et al. Theranostics. 2024 Mar 31;14(6):2442-2463

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