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

Cyclic GMP-AMP Synthase

cGAS

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-114180
    RU.521
    Inhibitor 99.95%
    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).
    RU.521
  • HY-133916
    G140
    Inhibitor 99.17%
    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.
    G140
  • HY-128583
    G150
    Inhibitor 99.12%
    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.
    G150
  • HY-114182
    PF-06928215
    Inhibitor 99.68%
    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).
    PF-06928215
  • HY-101835
    Decoyinine
    Inhibitor 99.96%
    Decoyinine is a selective inhibitor of GMP synthetase (GMPS).
    Decoyinine
  • HY-B1730R
    Phensuximide (Standard)
    Inhibitor
    Phensuximide (Standard) is the analytical standard of Phensuximide. This product is intended for research and analytical applications. Phensuximide is an orally active succinimide antiepileptic and anticonvulsant agent. Phensuximide inhibits cyclic AMP and cyclic GMP accumulation in depolarized brain tissue. Phensuximide can be used for the study of seizure and petit mal.
    Phensuximide (Standard)
  • HY-159925
    QKY-613
    Activator
    QKY-613 is a prodrug that enhances immune surveillance by targeting nucleic acid modification pathways. QKY-613 promotes the selective incorporation of 6mdA (N6-methyldeoxyadenosine) into viral DNA, enhancing the phase separation potential of DNA, thereby increasing the activation of cGAS and strengthening host immune surveillance. In virus-infected mouse models, QKY-613 significantly reduced mortality in aged mice. QKY-613 holds promise for research on nucleic acid modification-based immune surveillance mechanisms.
    QKY-613
  • HY-172208
    PROTAC cGAS degrader-1
    Degrader
    PROTAC cGAS degrader-1 (Compound TH35) is an effective and selective cGAS PROTAC degrader, with DC50 values of 0.9 μM and 4.6 μM in THP-1 and RAW 264.7 cells, respectively. PROTAC cGAS degrader-1 can inhibit the activation of cGAS signaling induced by dsDNA. PROTAC cGAS degrader-1 has anti-inflammatory activity and can be used in the research of cGAS-related inflammatory diseases. (Pink: cGAS inhibitor (HY-133916); Black: Linker (HY-W411604); Blue: E3 ligase ligand (HY-43722))
    PROTAC cGAS degrader-1
  • 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.
    IRAK4-IN-4
  • 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.
    cGAS-IN-1
  • HY-160546
    cGAS-IN-2
    Inhibitor 99.67%
    cGAS-IN-2 (compound 109) is a potent inhibitor of Cyclic GMP-AMP Synthase (cGAS), with IC50 of 0.01512 μM for h-cGAS.
    cGAS-IN-2
  • HY-P5997
    XQ2B
    Inhibitor 99.19%
    XQ2B is a specific cGAS inhibitor targeting protein-DNA interaction and phase separation. XQ2B markedly reduces ISD-induced Autophagy. XQ2B inhibits herpes simplex virus 1 (HSV-1)-induced antiviral immune responses and enhances HSV-1 infection.
    XQ2B
  • 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.
    HA-1004
  • HY-138646
    Poly(deoxyadenylic-thymidylic) acid sodium
    Activator
    Polydeoxyadenylic-thymidylic acid (Poly(dA:dT)) sodium is a synthetic DNA polymer. Poly(dA:dT) sodium can be used to determine the activity of bound and free ribonucleic acid polymerase. Poly(dA:dT) sodium is recognized by multiple PRRs (cytosolic DNA sensors (CDS), including cGAS, AIM2, DAI, DDX41, IFI16, and LRRFIP1), and triggers the production of type I interferons. Poly(dA:dT) sodium can be used for the research of cancer and virus infection.
    Poly(deoxyadenylic-thymidylic) acid sodium
  • HY-164288
    TDI-6570
    Inhibitor 99.64%
    TDI-6570 is a Cyclic GMP-AMP Synthase (cGAS) inhibitor with the IC50 of 0.138 μM.
    TDI-6570
  • HY-132221
    CU-32
    Inhibitor 98.8%
    CU-32 is a potent cGAS inhibitor with an IC50 of 0.45 µM. CU-32 decreases IFN-stimulatory DNA-induced production of IFN-β in THP-1 cells.
    CU-32
  • 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.
    HA-1004 hydrochloride
  • HY-134919
    CU-76
    Inhibitor
    CU-76 is an inhibitor for human cyclic GMP-AMP synthase (hcGAS) with an IC50 of 0.24 μM. CU-76 selectively inhibits the DNA pathway in human cells, and can be used in autoimmune research.
    CU-76
  • 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.
    cGAS-IN-3
  • HY-170362
    cGAS-IN-4
    Inhibitor
    cGAS-IN-4 (Compound 36) is an orally active inhibitor for cyclic GMP-AMP synthase (cGAS) with IC50 of 32 nM and 5.8 nM for h-cGAS and m-cGAS. cGAS-IN-4 inhibits the cGAMP in THP-1 cell with an IC50 of 60 nM, which improves the cellular potency. cGAS-IN-4 exhibits anti-inflammatory efficacy in Concanavalin A (HY-P2149)-induced acute liver injury in mouse models. orally active, THP-1, C57Bl/6 mouse, orally active
    cGAS-IN-4
Cat. No. Product Name / Synonyms Application Reactivity