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首页-小分子抑制剂&激动剂-Epigenetics-HDAC-GV-001
GV-001

Chemical Structure : GV-001

CAS No.: 3082707-76-1

GV-001 (GV001)

货号: PC-26486Not For Human Use, Lab Use Only.

GV-001 is a potent, selective and orally bioavailable HDAC6 inhibitor with IC50 of 1.18 nM, shows >200- and 1900-fold selectivity over HDAC1 and HDAC8.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

GV-001 is a potent, selective and orally bioavailable HDAC6 inhibitor with IC50 of 1.18 nM, shows >200- and 1900-fold selectivity over HDAC1 and HDAC8.
GV-001 inhibits tubulin deacetylation in a dose-dependent manner with IC50 of 0.19 uM for Ac-α-tubulin, exhibits selective upregulation of acetylated α-tubulin expression.
GV-001 significantly decreased inflammation-related markers (I-TAC, sIL-6, MCP-1), modulation of fibrosis-related matrix proteins (decreased Collagen I and III; increased Collagen IV; modulated MMP-1), and reduces tissue remodeling/wound healing markers (tPA, uPA, sVEGF).
GV-001 attenuates the expression of inflammatory and immunoregulatory chemokines, EMT markers, and ECM components in human primary cell-based models of renal fibrotic diseases.
GV-001 inhibits the growth of human ADPKD cysts in vitro.
GV-001 (0, 60, or 120 mg/kg) attenuates the progression of cyst growth in the ADPKD mouse model.

物理化学性质&存储条件

分子量 309.33
分子式 C17H15N3O3
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-hydroxy-4-((3-methyl-4-oxo-3,4-dihydroquinazolin-2-yl)methyl)benzamide

参考文献

1. Wu SS, et al. J Med Chem. 2026 Apr 6. doi: 10.1021/acs.jmedchem.5c03139.

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