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Chemical Structure : COH34
CAS No.: 906439-72-3
Catalog No.: 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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|---|---|---|---|
| 5 mg | $228 | In stock | |
| 10 mg | $358 | In stock | |
| 25 mg | $558 | In stock | |
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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.
| M.Wt | 293.384 | |
| Formula | C18H15NOS | |
| Appearance | Solid | |
| Storage |
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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 |
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1. Shih-Hsun Chen, et al. Sci Adv. 2019 Apr 10;5(4):eaav4340.
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