| Bioactivity | JA2131 is a small molecular inhibitor of Poly(ADP-ribose) Glycohydrolase (PARG) (IC50=0.4 μM). JA2131 regulate DNA damage responses, causes replication fork stalling and cancer cell death[1][2]. | ||||||||||||
| Invitro | JA2131 (10 mM; 1-2 h) induces hyperPARylation of PARP1 in PC3 cells[1].JA2131 (10 μM; 2 wk) inhibits colony formation of MCF-7, PC3, and MDA-MB-231 cells, and (0.1 μM-1 mM; 72 h) shows cytotoxicity to inhibit MRC-50 cells with an IC50 value of 132 μM[1].JA2131 (5 μM; 72 h) inhibits PC3, and A172 glioblastoma cells viability[1].JA2131 (10 μM; 2 h) could be acting at the replication fork in HeLa cells[1]. Cell Viability Assay[1] Cell Line: | ||||||||||||
| Name | JA2131 | ||||||||||||
| CAS | 6505-99-3 | ||||||||||||
| Formula | C13H19N5O2S2 | ||||||||||||
| Molar Mass | 341.45 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Houl JH, et al. Selective small molecule PARG inhibitor causes replication fork stalling and cancer cell death. Nat Commun. 2019 Dec 11;10(1):5654. [2]. Brosey CA, et al. Targeting SARS-CoV-2 Nsp3 macrodomain structure with insights from human poly(ADP-ribose) glycohydrolase (PARG) structures with inhibitors. Prog Biophys Mol Biol. 2021 Aug;163:171-186. |