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首页-小分子抑制剂&激动剂-Epigenetics-Bromodomain-DUAL946
DUAL946

Chemical Structure : DUAL946

CAS No.: 1868180-45-3

DUAL946 (DUAL 946)

货号: PC-21726Not For Human Use, Lab Use Only.

DUAL946 is a sub-micromolar inhibitor of both BET and class I & IIb HDAC proteins with IC50 of 0.05/0.25/0.42/14.13/34.89 uM for BRD4/HDAC1/HDAC2/HDAC5/HDAC7/HDAC9, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

DUAL946 is a sub-micromolar inhibitor of both BET and class I & IIb HDAC proteins with IC50 of 0.05/0.25/0.42/14.13/34.89 uM for BRD4/HDAC1/HDAC2/HDAC5/HDAC7/HDAC9, respectively.
DUAL946 shows an equilibrium binding constant of 57 nM against the BRD4 WT tandem bromodomains and 53 nM versus BRD4-BD2.
DUAL946 engaged BET and HDAC dependent mechanisms in an NMC cell line, as demonstrated by down regulation of c-myc expression levels and an increase on acetylation of histone H4, respectively.
DUAL946 also inhibited growth in NMC and AML cells.

物理化学性质&存储条件

分子量 552.67
分子式 C30H40N4O6
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

isopropyl ((2S,4R)-1-acetyl-6-(4-(8-(hydroxyamino)-8-oxooctanamido)phenyl)-2-methyl-1,2,3,4-tetrahydroquinolin-4-yl)carbamate

参考文献

1. Stephen J. Atkinson, et al. MedChemComm (2014), 5 (3), 342-351.

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