SML3698

G150

≥98% (HPLC)

• Synonym(s): 1-(9-(6-Aminopyridin-3-yl)-6,7-dichloro-3,4-dihydro-1H-pyrido[4,3-b]indol-2(5H)-yl)-2-hydroxyethanone, 1-[9-(6-Amino-3-pyridinyl)-6,7-dichloro-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indol-2-yl]-2-hydroxyethanone
• Empirical Formula (Hill Notation): C₁₈H₁₆Cl₂N₄O₂
• CAS Number: 2369751-30-2
• Molecular Weight: 391.25
• MDL number: MFCD32067964
• UNSPSC Code: 12352200
• NACRES: NA.21

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear (warmed)
• storage temp.: 2-8°C

Description

Biochem/physiol Actions

G150 is a substrate site-targeting, potent and selective human cyclic GMP-AMP synthase (cGAS) inhibitor (IC50 = 10.2 nM; 100 nM h-cGAS, 0.1 mM ATP & GTP, 25 nM 100-bp dsDNA) with no murine cGAS potency (IC50 >25 μM) and low cytotoxicity (THP1 LD50 = 53 μM). G150 selectively inhibits dsDNA-induced IFNB1/CXCL10 transcription in THP1 (IC50 = 1.96/7.57 μM) & primary human macrophages (IC50 = 0.62/0.87 μM) without affecting adenylyl cyclase activity, direct STING activation by cGAMP, or immune responses induced by hpRNA (RIG-I pathway), poly(I:C) (OAS/RNase L pathway), LPS (TLR4 pathway).

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable