| Identification | Back Directory | [Name]
INDEX NAME NOT YET ASSIGNED | [CAS]
2369751-30-2 | [Synonyms]
Ethanone, 1-[9-(6-amino-3-pyridinyl)-6,7-dichloro-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indol-2-yl]-2-hydroxy- | [Molecular Formula]
C18H16Cl2N4O2 | [MDL Number]
MFCD32067964 | [MOL File]
2369751-30-2.mol | [Molecular Weight]
391.25 |
| Chemical Properties | Back Directory | [Boiling point ]
694.0±55.0 °C(Predicted) | [density ]
1.545±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: soluble | [form ]
A crystalline solid | [pka]
13.47±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
G150 is a highly selective human cyclic GMP-AMP synthase (h-cGAS) inhibitor with an IC50 of 10.2 nM. G150 represses dsDNA-triggered interferon expression, and G150 can be used for the research of inflammatory[1]. | [Biological Activity]
G150 is a substrate site-targetingpotent and selective human cyclic GMP-AMP synthase (cGAS) inhibitor (IC50 = 10.2 nM; 100 nM h-cGAS0.1 mM ATP & GTP25 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 activitydirect STING activation by cGAMPor immune responses induced by hpRNA (RIG-I pathway)poly(I:C) (OAS/RNase L pathway)LPS (TLR4 pathway). | [References]
[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. DOI:10.1038/s41467-019-08620-4 |
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