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首页-小分子抑制剂&激动剂-Epigenetics-HDAC-class I HDACs inhibitor JT86
class I HDACs inhibitor JT86

Chemical Structure : class I HDACs inhibitor JT86

CAS No.: 2708136-83-6

class I HDACs inhibitor JT86

货号: PC-25167Not For Human Use, Lab Use Only.

class I HDACs inhibitor JT86 is a potent class I HDACs inhibitor with IC50 of 0.72/8.0/2.0 nM for HDAC1/2/3 respectively, 61-fold selectivity over HDAC8 (IC50 44 nM) and 11-fold over HDAC2.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

class I HDACs inhibitor JT86 is a potent class I HDACs inhibitor with IC50 of 0.72/8.0/2.0 nM for HDAC1/2/3 respectively, 61-fold selectivity over HDAC8 (IC50 44 nM) and 11-fold over HDAC2.
JT86 is much less active against the class IIa enzyme HDAC7.
JT86 shows potent cytotoxic effect (IC50= 0.02-0.1 μM) across the five cancer cell lines with 15- to 23-fold increased potency over AR-42.
JT86 induces concentration-dependent accumulation of acetylated histone H4 in MM96L melanoma cells, indicating inhibition of endogenous HDAC1.

物理化学性质&存储条件

分子量 390.44
分子式 C23H22N2O4
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-(4-(Hydroxycarbamoyl)phenyl)-4-(naphthalen-2-yl)tetrahydro-2H-pyran-4-carboxamide

参考文献

1. Jiahui Tng, et al. J Med Chem. 2020 Jun 11;63(11):5956-5971.

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