JA2131

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].

Research Areas >> Cancer

JA2131 (10 mM; 1-2 h) 诱导 PC3 细胞 PARP1 过度磷酸化[1]。 Ja2131 (10 μM; 2 周) 抑制 MCF-7、PC3 和 MDA-MB-231 细胞集落形成，(0.1 μM-1 mM; 72 h) 对 MRC-50 细胞有抑制作用，IC50 为 132 μM[1]。 Ja2131 (5 μM; 72 h) 抑制 PC3 和 A172 胶质母细胞瘤细胞活力[1]。 Ja2131 (10 μM; 2 h) 可能作用于 HeLa 细胞的复制叉[1]。 Cell Viability Assay[1] Cell Line: PC3, and A172 glioblastoma cells Concentration: 0.1 μM-10 mM Incubation Time: 72 hours Result: Inhibited cell viability with IC50s of 33.05 μM (PC3 cells) and 55.34 μM (A172 cells), respectively.

[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.