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首页-小分子抑制剂&激动剂-Others-Other Targets-UNC10142
UNC10142

Chemical Structure : UNC10142

CAS No.:

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UNC10142 (UNC-10142)

货号: PC-23450Not For Human Use, Lab Use Only.

UNC10142 is a first-in-class, specific, cell-active small molecule antagonist of the tandem chromodomains of CHD1 (Chromodomain-Helicase DNA-Binding Protein 1) with binding IC50 of 1.7 uM in TR-FRET assays.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

UNC10142 is a first-in-class, specific, cell-active small molecule antagonist of the tandem chromodomains of CHD1 (Chromodomain-Helicase DNA-Binding Protein 1) with binding IC50 of 1.7 uM in TR-FRET assays.
UNC10142 dispalys >30-fold selective for CHD1 against other Kme readers MPP8, PHF19, and SETDB1.
UNC10142 binds to the tandem chromodomains of CHD1 with ITC Kd of 4.3 uM.
UNC10142 engages endogenous CHD1 and leads to loss of viability in PTEN-deficient cells.
UNC10142 phenocopies genetic loss of CHD1 in PTEN-deficient prostate cancer cells.
UNC10142 treatment results in synthetic lethality in PTEN-deficient prostate cancer cells while sparing PTEN-intact prostate cancer cells.

物理化学性质&存储条件

分子量 580.82
分子式 C33H52N6O3
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

1-(4-((2-(Azonan-1-yl)-6-methoxy-7-(3-(piperidin-1-yl)propoxy)quinazolin-4-yl)(methyl)amino)piperidin-1-yl)ethan-1-one

参考文献

1. Johnson RL, et al. J Med Chem. 2024 Nov 7. doi: 10.1021/acs.jmedchem.4c01172.

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