SML3698

G150

≥98% (HPLC)

• 別名: 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
• 実験式（ヒル表記法）: C₁₈H₁₆Cl₂N₄O₂
• CAS番号: 2369751-30-2
• 分子量: 391.25
• MDL番号: MFCD32067964
• UNSPSCコード: 12352200
• NACRES: NA.21

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• フォーム: powder
• 色: white to beige
• 溶解性: DMSO: 2 mg/mL, clear (warmed)
• 保管温度: 2-8°C

詳細

生物化学的／生理学的作用

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).

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable