6505-99-3

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].

JA2131 is a cell penetrantpotent and selective poly(ADP-ribose) glycohydrolase (PARG) inhibitor th at selectively kills cancer cells. JA2131 induces PARP1 hyper-PARylation and sensitizes cancer cells to radiation-induced DNA damage. JA2131 induces replication fork defects.

[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. DOI:10.1038/s41467-019-13508-4
[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. DOI:10.1016/j.pbiomolbio.2021.02.002