1. Immunology/Inflammation
  2. 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 (10):

Cat. No. Product Name Effect Purity
  • HY-114181
    IRAK4-IN-4 Inhibitor 99.85%
    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[1].
  • HY-114180
    RU.521 Inhibitor 99.89%
    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 0.7 μM. RU.521 reduces constitutive expression of interferon in macrophages from a mouse model of Aicardi-Goutières syndrome (AGS)[1].
  • HY-128583
    G150 Inhibitor 98.61%
    G150 is a highly selective human cyclic GMP-AMP synthase (h-cGAS) inhibitor with an IC50 of 10.2 nM. G150 represses dsDNA-triggered interferon expression, and G150 can be used for the research of inflammatory[1].
  • HY-114182
    PF-06928215 Inhibitor
    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)[1].
  • HY-133916
    G140 Inhibitor 98.11%
    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[1].
  • HY-112348
    HA-1004 hydrochloride Inhibitor
    HA-1004 hydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 hydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein (Cyclic GMP-AMP Synthase), and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 hydrochloride an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models[1][2][3][4].
  • HY-162459
    cGAS-IN-3 Inhibitor
    cGAS-IN-3 (compound 30d-S) is an orally active cyclic GMP-AMP synthase (Cyclic GMP-AMP Synthase/cGAS) inhibitor with good plasma exposure and low clearance. cGAS-IN-3 has anti-inflammatory activity and can significantly reduce lung inflammation in rats[1].
  • HY-160546
    cGAS-IN-2 Inhibitor
    cGAS-IN-2 (compound 109) is a potent inhibitor of Cyclic GMP-AMP Synthase (cGAS), with IC50 of 0.01512 μM for h-cGAS[1].
  • HY-149526
    cGAS-IN-1 Inhibitor 98.29%
    cGAS-IN-1 (compound C20) is a flavonoid and Cyclic GMP-AMP Synthase (cGAS) inhibitor with IC50s of 2.28 μM (human cGAS) and 1.44 μM (mouse cGAS). Abnormal activation of cGAS is associated with a variety of immune-mediated inflammatory diseases, and cGAS-IN-1 has potential anti-inflammatory activity[1].
  • HY-123468
    HA-1004 Inhibitor 99.03%
    HA-1004 is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models[1][2][3].