Chemical Structure : COH34
CAS No.: 906439-72-3
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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1 mg | ¥1280 | In stock | |
5 mg | ¥2980 | In stock | |
10 mg | ¥4880 | In stock | |
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100 mg | Get quote |
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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.
分子量 | 293.384 | |
分子式 | C18H15NOS | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
(E)-1-(((p-tolylthio)imino)methyl)naphthalen-2-ol |
1. Shih-Hsun Chen, et al. Sci Adv. 2019 Apr 10;5(4):eaav4340.
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