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Merck
CN

SML3698

Sigma-Aldrich

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

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About This Item

Empirical Formula (Hill Notation):
C18H16Cl2N4O2
CAS Number:
2369751-30-2
Molecular Weight:
391.25
MDL number:
MFCD32067964
UNSPSC Code:
12352200
NACRES:
NA.21

Key Documents

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Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear (warmed)

storage temp.

2-8°C

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 Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000254970
0000254969
0000243140
0000243140
0000254970

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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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