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About This Item
Empirical Formula (Hill Notation):
C18H16Cl2N4O2
CAS Number:
Molecular Weight:
391.25
UNSPSC Code:
12352200
NACRES:
NA.21
MDL number:
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear (warmed)
storage temp.
2-8°C
Quality Level
Related Categories
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).
Substrate site-targeting, non-cytotoxic, potent and selective human cyclic GMP-AMP synthase (cGAS) inhibitor against cellular STING signaling.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression
Nature Communications, 10(1), 2261-2261 (2019)
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