Bioactivity | 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]. | ||||||||||||
Target | IC50: 14.0 nM (h-cGAS), 442 nM (m-cGAS) | ||||||||||||
Invitro | 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]. | ||||||||||||
Name | G140 | ||||||||||||
CAS | 2369751-07-3 | ||||||||||||
Formula | C17H16Cl2N4O2 | ||||||||||||
Molar Mass | 379.24 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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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. |