| Bioactivity | cGAS-IN-4 (Compound 36) is an orally active inhibitor for cyclic GMP-AMP synthase (cGAS) with IC50 of 32 nM and 5.8 nM for h-cGAS and m-cGAS. cGAS-IN-4 inhibits the cGAMP in THP-1 cell with an IC50 of 60 nM, which improves the cellular potency. cGAS-IN-4 exhibits anti-inflammatory efficacy in Concanavalin A (HY-P2149)-induced acute liver injury in mouse models[1].orally active, THP-1, C57Bl/6 mouse, orally active |
| CAS | 2987886-49-5 |
| Formula | C19H18Cl2N4O3 |
| Molar Mass | 421.28 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Cyr P, et al., Discovery of Potent and Orally Bioavailable Pyrimidine Amide cGAS Inhibitors via Structure-Guided Hybridization. ACS Med Chem Lett. 2024 Nov 25;15(12):2201-2209. |
cGAS-IN-4
CAS: 2987886-49-5 F: C19H18Cl2N4O3 W: 421.28
cGAS-IN-4 (Compound 36) is an orally active inhibitor for cyclic GMP-AMP synthase (cGAS) with IC50 of 32 nM and 5.8 nM f
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