For research use only. Not for therapeutic Use.
G140 is a potent and selective inhibitor of cyclic GMP-AMP synthase (cGAS), with IC50s of 14.0 nM and 442 nM for h-cGAS and m-cGAS, respectively. G140 has anti-inflammatory activity[1].
G140 (0.1-100 μM; 4 h) inhibits h-cGAS in a dose-dependent manner with IC50s of 1.70 and 0.86?μM in human THP1 and primary macrophages, respectively[1].?
G140 (0.1-100 μM; 24 h) inhibits cells viability with a LD50 of >100 μM in THP1 cells[1].
| Catalog Number | I045352 |
| CAS Number | 2369751-07-3 |
| Synonyms | 1-[6,7-dichloro-9-(1-methylpyrazol-3-yl)-1,3,4,5-tetrahydropyrido[4,3-b]indol-2-yl]-2-hydroxyethanone |
| Molecular Formula | C17H16Cl2N4O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C17H16Cl2N4O2/c1-22-4-2-13(21-22)9-6-11(18)16(19)17-15(9)10-7-23(14(25)8-24)5-3-12(10)20-17/h2,4,6,20,24H,3,5,7-8H2,1H3 |
| InChIKey | NVPFAXHXXODQRO-UHFFFAOYSA-N |
| SMILES | CN1C=CC(=N1)C2=CC(=C(C3=C2C4=C(N3)CCN(C4)C(=O)CO)Cl)Cl |
| Reference | [1]. Lama L, et, al. Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression. Nat Commun. 2019 May 21; 10(1): 2261. |
