A cGAS inhibitor
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G150

Item No. 28318

Technical Information
Formal Name
1-[9-(6-amino-3-pyridinyl)-6,7-dichloro-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indol-2-yl]-2-hydroxy-ethanone
CAS Number
2369751-30-2
Molecular Formula
C18H16Cl2N4O2
Formula Weight
Purity
≥95%
Formulation
A crystalline solid
λmax
234, 301 nm
SMILES
ClC1=CC(C2=CC=C(N)N=C2)=C3C(NC4=C3CN(C(CO)=O)CC4)=C1Cl
InChi Code
InChI=1S/C18H16Cl2N4O2/c19-12-5-10(9-1-2-14(21)22-6-9)16-11-7-24(15(26)8-25)4-3-13(11)23-18(16)17(12)20/h1-2,5-6,23,25H,3-4,7-8H2,(H2,21,22)
InChi Key
VVUOUIPXYFIWLE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    G150 is an inhibitor of cyclic GMP-AMP synthase (cGAS; IC50 = 10.2 nM for the human enzyme).1 It is selective for human cGAS over mouse cGAS (IC50 = 25,000 nM). G150 inhibits dsDNA-induced expression of IFNB1 in THP-1 cells and isolated human monocyte-derived macrophages (IC50s = 1.96 and 0.62 µM, respectively) but not LPS-induced expresssion of TNF or poly(I:C)-induced rRNA degradation in the same cells when used at a concentration of 10 µM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lama, L., Adura, C., Xie, W., et alDevelopment of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression. Nat. Commun. 10(1), 2261 (2019).