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

Cyclic GMP-AMP Synthase

cGAS

Cyclic GMP-AMP Synthase

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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 99.20%
    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-180211
    cGAS-IN-8
    		Inhibitor
    cGAS-IN-8 is an indazole cyclic GMP-AMP synthase (cGAS) inhibitor with an IC50 of 6 nM for human cGAS. cGAS-IN-8 inhibits cGAMP production in THP-1 cells with an IC50 of 0.12 µM. cGAS-IN-8 does not inhibits hERG activity. cGAS-IN-8 can be used for the research of autoimmune diseases.
    cGAS-IN-8
  • HY-179624
    cGAS-IN-7
    		Inhibitor
    cGAS-IN-7 is a cyclic GMP-AMP synthase (cGAS) inhibitor with an IC50 of 0.66 μM for human cGAS. cGAS-IN-7 modestly decreases cGAMP levels in THP1 cells. cGAS-IN-7 can be used for the research of Alzheimer's disease.
    cGAS-IN-7
  • HY-181850
    Telomeric G4s ligand 2
    		Activator
    Telomeric G4s ligand 2 is an orally active, selective ligand of telomeric G-quadruplex (G4), with an IC50 of 0.4 μM. Telomeric G4s ligand 2 binds to dimeric telomeric G4, inhibits the activities of DHX36 and BLM helicases. Telomeric G4s ligand 2 activates cGAS-STING and TERRA-ZBP1 pathways, inducing autophagy and G2/M cell cycle arrest, and exhibits antiproliferative effects across cancer cell lines. Telomeric G4s ligand 2 can be used for the study of colorectal cancer.
    Telomeric G4s ligand 2
  • HY-172208
    PROTAC cGAS degrader-1
    		Degrader 99.07%
    PROTAC cGAS degrader-1 is a potent 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 induces proteasome-mediated degradation of cGAS, inhibits the cGAS signaling pathway, and attenuates double-stranded DNA-induced activation of cGAS in human and mouse cells. PROTAC cGAS degrader-1 is applicable to research related to ulcerative colitis.
    PROTAC cGAS degrader-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-149526
    cGAS-IN-1
    		Inhibitor 98.21%
    cGAS-IN-1 (Compound C20) is a cyclic GMP-AMP synthase (cGAS) inhibitor with IC50s of 2.28 μM (human cGAS, h-cGASFL) and 1.44 μM (mouse cGAS, m-cGASCD). cGAS-IN-1 can be used for the studies of autoimmune diseases and chronic inflammation.
    cGAS-IN-1
  • HY-P5997
    XQ2B
    		Inhibitor 99.45%
    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-114181
    IRAK4-IN-4
    		Inhibitor 99.55%
    IRAK4-IN-4 (Compound 15) is an interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor, with 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 can be used for research of autoimmune diseases.
    IRAK4-IN-4
  • HY-164288
    TDI-6570
    		Inhibitor 99.64%
    TDI-6570 (TDI-006570) is a blood-brain barrier-permeable, orally active cGAS inhibitor with an IC50 of 1.64 μM. TDI-6570 exhibits high gastrointestinal absorption and a long brain half-life in mice, and shows no toxicity to primary neurons. By inhibiting the cGAS-STING-IFN signaling pathway, TDI-6570 reduces STING levels and the activation of TBK1, blocks double-stranded DNA-induced cGAS activation and downstream interferon-stimulated gene expression, thereby reducing tau protein spread and improving synaptic loss. TDI-6570 reverses memory deficits, increases the amplitude of long-term potentiation, enhances the MEF2C transcriptional network, restores PSD-95 and vGAT punctate structures, and significantly improves cognitive resilience. TDI-6570 can be applied to the research of Alzheimer's disease, Parkinson's disease, systemic lupus erythematosus, as well as various central nervous system and autoimmune diseases.
    TDI-6570
  • HY-170362
    cGAS-IN-4
    		Inhibitor 99.28%
    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
  • HY-174801
    XL-3156
    		Inhibitor 99.91%
    XL-3156 is a cGAS inhibitor. XL-3156 occupies both allosteric and orthosteric sites simultaneously, and inhibits the interaction and phase separation between cGAS and DNA by stabilizing the closed conformation of the activation loop. XL-3156 can be used in the research of diseases such as autoimmune diseases and inflammation.
    XL-3156
  • HY-W587488
    Adenosine 3′-monophosphate
    		Agonist 99%
    Adenosine 3’-monophosphate (3’-AMP) is a nucleotide. Adenosine 3’-monophosphate is a cyclic AMP production agonist. Adenosine 3’-monophosphate increases cyclic AMP levels concentration-dependently in NG108-15 cells. Adenosine 3’-monophosphate can be used in the determination of acid phosphatase activity of human serum, which is estabilished as a laboratory procedure in the diagnosis of prostate cancer, metastatic mammary cancer and Gaucher’s disease. Adenosine 3’-monophosphate inhibits human aortic and coronary vascular smooth muscle cell proliferation via A2B receptors.
    Adenosine 3′-monophosphate
  • HY-124700
    LYPLAL1-IN-1
    		Inhibitor 99.9%
    LYPLAL1-IN-1 (compound 11) is a selective, covalent, and irreversible inhibitor of the lysophospholipase-like enzyme LYPLAL1 (IC50 = 6 nM). LYPLAL1-IN-1 shows selectivity against other serine hydrolases such as carboxylesterase CES1 (IC50 > 50 μM for CES1). LYPLAL1-IN-1 inhibits the depalmitoylation function of LYPLAL1, blocking its depalmitoylation modification of cyclic GMP-AMP synthase (cGAS), thereby promoting cGAS dimerization and activation, and initiating the cGAS-STING pathway-mediated innate immune response. LYPLAL1-IN-1 can enhance DNA-induced type I interferon production, upregulate PD-L1 expression in tumor cells, and promote the accumulation of tumor-infiltrating CD8+ T cells, with the core function of strengthening the anti-tumor immune response. LYPLAL1-IN-1 is primarily used in tumor immunology research, especially in combination with PD-1/PD-L1 inhibitors.
    LYPLAL1-IN-1
  • HY-174802
    XL-3158
    		Inhibitor 99.55%
    XL-3158 is a selective and cross-species Cyclic GMP-AMP synthase (cGAS) inhibitor (IC50: 11.1 μM for human cGAS, 2.19 μM for mouse cGAS). XL-3158 simultaneously occupy allosteric and orthosteric sites, stabilizing the activation loop in a closed, inactive conformation and thereby attenuating the cGAS-DNA interactions. XL-3158 inhibits cGAS by targeting phase separation. XL-3158 efficiently penetrates cells by inhibiting aggregate formation, effectively reducing the local concentration of cGAS within cells. XL-3158 can be used for the study of cGAS-dependent inflammatory diseases.
    XL-3158
  • HY-B1730
    Phensuximide
    		99.41%
    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
Cat. No. Product Name / Synonyms Application Reactivity