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G150

Chemical Structure : G150

CAS No.: 2369751-30-2

G150 (cGAS inhibitor G150)

Catalog No.: PC-73361Not For Human Use, Lab Use Only.

G150 is a potent, specific human cyclic GMP-AMP synthase (cGAS) small-molecule inhibitor with IC50 of 10.2 nM, shows no inhibition against m-cGAS.

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Biological Activity

G150 is a potent, specific human cyclic GMP-AMP synthase (cGAS) small-molecule inhibitor with IC50 of 10.2 nM, shows no inhibition against m-cGAS.
G150 binds to apo h-cGASCD, localized within the ATP and GTP binding pocket.
G150 showed dose-dependent inhibitory activity in THP1 cells with IC50 of 1.96 uM, as determined by qRT-PCR for IFNB1 mRNA.
G150 shows no off-target effect against other nucleotidyl transferase enzymes.
G150 inhibits the SEAP NF-κB pathway reporter with IC50 of 0.9 uM.

Physicochemical Properties

M.Wt 391.25
Formula C18H16Cl2N4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO (3.9 mg/mL)

Chemical Name/SMILES

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-

References

1. Lodoe Lama, et al. Nat Commun. 2019 May 21;10(1):2261.

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