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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-PARP-COH34
COH34

Chemical Structure : COH34

CAS No.: 906439-72-3

COH34 (PARG inhibitor COH34, NSC191252)

货号: PC-72966Not For Human Use, Lab Use Only.

COH34 (PARG inhibitor COH34, NSC191252) is a potent, selective and cell-active PARG inhibitor (IC50=0.37 nM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

COH34 (PARG inhibitor COH34, NSC191252) is a potent, selective and cell-active PARG inhibitor (IC50=0.37 nM).
COH34 specifically inhibits poly(ADP-ribose) glycohydrolase (PARG) and strongly binds to the catalytic domain of PARG with Asn869 as a key binding residue (Kd=0.547 uM), does not suppress the activity of PARP1 and had little impact on TARG1 at 1 uM.
COH34 suppresses the PARG-dependent dePARylation process, suppresses DNA repair in cells.
COH34 exhibits lethality in BRCA-mutant and PARP inhibitor–resistant cancer cells UWB1.289 and PEO-1 (EC50=2.1 and 0.8 uM, respectively), selectively kills BRCA-mutant and PARP inhibitor–resistant cancer cells.
COH34 exhibits antitumor activity (at 20 mg/kg) in PARP inhibitor-resistant and DNA damage repair–defective cell line xenografts.

物理化学性质&存储条件

分子量 293.384
分子式 C18H15NOS
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

(E)-1-(((p-tolylthio)imino)methyl)naphthalen-2-ol

参考文献

1. Shih-Hsun Chen, et al. Sci Adv. 2019 Apr 10;5(4):eaav4340.

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