[CAS NO. 6505-99-3] JA2131
PRODUCTS SPECIFICATIONS [6505-99-3]
DESCRIPTION [6505-99-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 341.45 |
| Molecular Formula | C13H19N5O2S2 |
| SMILES | O=C(N1C)N(C)C2=C(N=C(SCCN3CCOCC3)N2)C1=S |
Summary
JA2131 is a small molecular inhibitor of Poly(ADP-ribose) Glycohydrolase (PARG) ( IC 50 =0.4 μM). JA2131 regulate DNA damage responses, causes replication fork stalling and cancer cell death [1] [2] .
In Vitro
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 IC
50
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. |
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
References
- [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.