For research use only. Not for therapeutic Use.
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 (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].
| Catalog Number | I042324 |
| CAS Number | 6505-99-3 |
| Synonyms | 1,3-dimethyl-8-(2-morpholin-4-ylethylsulfanyl)-6-sulfanylidene-7H-purin-2-one |
| Molecular Formula | C13H19N5O2S2 |
| Purity | ≥95% |
| InChI | InChI=1S/C13H19N5O2S2/c1-16-10-9(11(21)17(2)13(16)19)14-12(15-10)22-8-5-18-3-6-20-7-4-18/h3-8H2,1-2H3,(H,14,15) |
| InChIKey | XHNSOGDMSSHQFY-UHFFFAOYSA-N |
| SMILES | CN1C2=C(C(=S)N(C1=O)C)NC(=N2)SCCN3CCOCC3 |
| 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. |
