1. Signaling Pathways
  2. Immunology/Inflammation
  3. Cyclic GMP-AMP Synthase

Cyclic GMP-AMP Synthase

Cyclic GMP-AMP synthase (cGAS) is a cytosolic DNA sensor that activates a type-I interferon response. cGAS binds to microbial DNA as well as self DNA that invades the cytoplasm, and catalyzes cGAMP synthesis. cGAMP then functions as a second messenger that binds to and activates the endoplasmic reticulum protein STING to trigger type-I IFNs production. STING recruits TBK1, which phosphorylates transcription factors, such as IRF3/7, and other substrates, such as IKKα, cRel, and p62.

cGAS is a critical regulator of inflammatory and autophagy responses in Huntington disease (HD). cGAS can induce signaling that is known to promote the up-regulation of inflammatory genes and play a critical role in age-related macular degeneration and cellular senescence. cGAS also plays a major role in the regulation of autophagy; this indicates that there is a close molecular and signaling link between inflammatory response and autophagy.

Cyclic GMP-AMP Synthase Related Products (5):

Cat. No. Product Name Effect Purity
  • HY-114180
    RU.521
    Inhibitor 98.67%
    RU.521 (RU320521) is a potent and selective cyclic GMP-AMP synthase (cGAS) inhibitor and inhibits cGAS-mediated interferon upregulation. RU.521 suppresses dsDNA-activated reporter activity with an IC50 of 700 nM. RU.521 reduces constitutive expression of interferon in macrophages from a mouse model of Aicardi-Goutières syndrome (AGS).
  • HY-128583
    G150
    Inhibitor 98.20%
    G150 is a potent and highly selective human cyclic GMP-AMP synthase (h-cGAS) inhibitor for repression of dsDNA-triggered interferon expression, with an IC50 of 10.2 nM.
  • HY-114182
    PF-06928215
    Inhibitor ≥99.0%
    PF-06928215 is a cGAS (cyclic GMP-AMP Synthase) inhibitor with an IC50 of 4.9 μΜ. PF-06928215 has a high binding affinity of 0.2 μM (Kd).
  • HY-114181
    IRAK4-IN-4
    Inhibitor 99.72%
    IRAK4-IN-4 is an interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor extracted from patent CN107163044A, Compound15, has an IC50 of 2.8 nM. IRAK4-IN-4 also inhibits cyclic GMP-AMP synthase (cGAS) with an IC50 of 2.1 nM.
  • HY-133916
    G140
    Inhibitor 98.38%
    G140 is a potent and selective inhibitor of cyclic GMP-AMP synthase (cGAS), with IC50s of 14.0 nM and 442 nM for h-cGAS and m-cGAS, respectively. G140 has anti-inflammatory activity.
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