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cGAS inhibitor

" in MedChemExpress (MCE) Product Catalog:

42

Inhibitors & Agonists

3

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3

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3

Isotope-Labeled Compounds

2

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P5997

    Autophagy Cyclic GMP-AMP Synthase Inflammation/Immunology
    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-170362A

    Cyclic GMP-AMP Synthase Inflammation/Immunology
    (R)-cGAS-IN-4 (Compound 77A*) is the R-enantiomer of cGAS-IN-4 (HY-170362). cGAS-IN-4 is an orally active inhibitor for cyclic GMP-AMP synthase (cGAS) .
    (R)-cGAS-IN-4
  • HY-160546

    Cyclic GMP-AMP Synthase Inflammation/Immunology
    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

    Cyclic GMP-AMP Synthase Inflammation/Immunology
    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-172208

    PROTACs Cyclic GMP-AMP Synthase Inflammation/Immunology
    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-133916
    G140
    4 Publications Verification

    Cyclic GMP-AMP Synthase Inflammation/Immunology
    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-162966

    Cyclic GMP-AMP Synthase Cancer
    MS7829 is a cGAS inhibitor-based deubiquitinase-targeted chimera (DUBTAC), a targeted protein stabilization (TPS) technology. cGAS is a key component in the cGAS-STING pathway. .
    MS7829
  • HY-12464

    WC-9717; CGA-276854

    Herbicide Others
    Butafenacil (WC-9717; CGA-276854) is an herbicide that inhibits protoporphyrinogen oxidase .
    Butafenacil
  • HY-N15159

    Cyclic GMP-AMP Synthase STING
    Cladophorol A is a cGAS inhibitor that binds to the conserved adenosine nucleobase binding site of cGAS, thereby blocking its activity. At non-cytotoxic concentrations, Cladophorol A effectively inhibits the overactivation of the cGAS-STING pathway with an IC50 of 370 nM. Cladophorol A holds potential for research on inflammatory diseases related to the overactivation of the cGAS-STING pathway .
    Cladophorol A
  • HY-170362

    Cyclic GMP-AMP Synthase Inflammation/Immunology
    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-174802

    Cyclic GMP-AMP Synthase IKK IFNAR Inflammation/Immunology
    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 has no obvious cytotoxicity within the effective concentration range and is suitable for subsequent cell function experiments. XL-3158 overcomes species selectivity barriers and serves as a drug candidate for cGAS-dependent inflammatory diseases.
    XL-3158
  • HY-114730

    IKK Inflammation/Immunology
    CGA-JK3 is CGA-JK3 is an ATP-competitive inhibitor of IKKβ-catalyzed kinase activity. CGA-JK3 inhibits IκBα phosphorylation in LPS (HY-D1056) - induced RAW 264.7 cells .
    CGA-JK3
  • HY-12464R

    WC-9717 (Standard); CGA-276854 (Standard)

    Herbicide Reference Standards Others
    Butafenacil (Standard) is the analytical standard of Butafenacil. This product is intended for research and analytical applications. Butafenacil (WC-9717; CGA-276854) is an herbicide that inhibits protoporphyrinogen oxidase .
    Butafenacil (Standard)
  • HY-116214R

    CGA-219417 (Standard)

    Reference Standards Fungal Androgen Receptor Aryl Hydrocarbon Receptor PERK Cytochrome P450 Infection Endocrinology
    Cyprodinil (Standard) (CGA-219417 (Standard)) is the analytical standard of Cyprodinil (HY-116214). This product is intended for research and analytical applications. Cyprodinil (CGA-219417) is a broad-spectrum anilinopyrimidine fungicide and an activator of the aryl hydrocarbon receptor. Cyprodinil also has anti-androgenic and androgenic activities. Cyprodinil can inhibit the biosynthesis of methionine in plant-pathogenic fungi and protect fruits and vegetables from a variety of pathogens.
    Cyprodinil (Standard)
  • HY-W021040S

    CGA-173506-13C3

    Isotope-Labeled Compounds Fungal Apoptosis Infection Cancer
    Fludioxonil- 13C3 (CGA-173506- 13C3) is 13C labeled Fludioxonil. Fludioxonil (CGA-173506) is a phenylpyrrole-type fungicide with oral activity that can inhibit the growth of S. sclerotiorum. Fludioxonil promotes tumor growth and metastasis, and induces cardiac toxicity. Fludioxonil causes cytoskeletal disruption, DNA damage, and apoptosis in mouse glioma cells .
    Fludioxonil-13C3
  • HY-116214S

    CGA-219417-d5

    Isotope-Labeled Compounds Fungal Androgen Receptor Aryl Hydrocarbon Receptor PERK Cytochrome P450 Infection Endocrinology
    Cyprodinil-d5(CGA-219417-d5) is the deuterium labeled Cyprodinil (HY-116214). Cyprodinil (CGA-219417) is a broad-spectrum anilinopyrimidine fungicide and an activator of the aryl hydrocarbon receptor. Cyprodinil also has anti-androgenic and androgenic activities. Cyprodinil can inhibit the biosynthesis of methionine in plant-pathogenic fungi and protect fruits and vegetables from a variety of pathogens .
    Cyprodinil-d5
  • HY-162459

    Cyclic GMP-AMP Synthase Inflammation/Immunology
    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-116214S1

    CGA-219417-13C6

    Isotope-Labeled Compounds Fungal Androgen Receptor Aryl Hydrocarbon Receptor PERK Cytochrome P450 Infection Endocrinology
    Cyprodinil- 13C6 (CGA-219417- 13C6) is the 13C6 labeled Cyprodinil (HY-116214). Cyprodinil (CGA-219417) is a broad-spectrum anilinopyrimidine fungicide and an activator of the aryl hydrocarbon receptor. Cyprodinil also has anti-androgenic and androgenic activities. Cyprodinil can inhibit the biosynthesis of methionine in plant-pathogenic fungi and protect fruits and vegetables from a variety of pathogens .
    Cyprodinil-13C6
  • HY-116214

    CGA-219417

    Fungal Androgen Receptor Aryl Hydrocarbon Receptor PERK Cytochrome P450 Infection Endocrinology
    Cyprodinil (CGA-219417) is a broad-spectrum anilinopyrimidine fungicide and an activator of the aryl hydrocarbon receptor. Cyprodinil also has anti-androgenic and androgenic activities. Cyprodinil can inhibit the biosynthesis of methionine in plant-pathogenic fungi and protect fruits and vegetables from a variety of pathogens .
    Cyprodinil
  • HY-W021040

    CGA-173506

    Fungal Apoptosis Infection Cancer
    Fludioxonil (CGA-173506) is a phenylpyrrole-type fungicide with oral activity that can inhibit the growth of S. sclerotiorum. Fludioxonil promotes tumor growth and metastasis, and induces cardiac toxicity. Fludioxonil causes cytoskeletal disruption, DNA damage, and apoptosis in mouse glioma cells .
    Fludioxonil
  • HY-164288

    TDI-006570

    Cyclic GMP-AMP Synthase Inflammation/Immunology Cancer
    TDI-6570 is a Cyclic GMP-AMP Synthase (cGAS) inhibitor with the IC50 of 0.138 μM .
    TDI-6570
  • HY-174801

    Cyclic GMP-AMP Synthase Inflammation/Immunology
    XL-3156 is a potent, selective, and cross-species cGAS inhibitor. XL-3156 can simultaneously occupy both allosteric and orthosteric sites, and inhibit 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 autoimmune diseases, inflammatory conditions and other diseases .
    XL-3156
  • HY-114180
    RU.521
    Maximum Cited Publications
    55 Publications Verification

    RU320521

    Cyclic GMP-AMP Synthase Metabolic Disease
    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-114182
    PF-06928215
    3 Publications Verification

    Cyclic GMP-AMP Synthase Inflammation/Immunology
    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-132221

    Cyclic GMP-AMP Synthase Inflammation/Immunology
    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-128583
    G150
    4 Publications Verification

    Cyclic GMP-AMP Synthase Inflammation/Immunology
    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-150751
    ODN TTAGGG
    1 Publications Verification

    ODN A151

    Toll-like Receptor (TLR) AIM2 Inflammation/Immunology
    ODN TTAGGG (A151), inhibitory oligonucleotide (ODN), is a TLR9, AIM2 and cGAS antagonist. ODN TTAGGG is immunosuppressive and inhibits AIM2 inflammasome activation, as well as cGAS activation, by competing with DNA. ODN TTAGGG can be used in the study of lupus erythematosus and other related autoimmune diseases. ODN TTAGGG sequence: 5'-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-3' .
    ODN TTAGGG
  • HY-150751C
    ODN TTAGGG sodium
    1 Publications Verification

    ODN A151 sodium

    AIM2 Toll-like Receptor (TLR) Inflammation/Immunology
    ODN TTAGGG sodium, inhibitory oligonucleotide (ODN), is a TLR9, AIM2 and cGAS antagonist. ODN TTAGGG sodium is immunosuppressive and inhibits AIM2 inflammasome activation, as well as cGAS activation, by competing with DNA. ODN TTAGGG sodium can be used in the study of lupus erythematosus and other related autoimmune diseases. ODN TTAGGG sequence: 5'-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-3' .
    ODN TTAGGG sodium
  • HY-163461

    PARP Cancer
    4F-DDC is a novel PARP1 inhibitor with an IC50 value of 82 nM. 4F-DDC induces DNA damage and activates the cGAS–STING pathway. 4F-DDC inhibits the growth of HCC-1937-derived tumor xenografts .
    4F-DDC
  • HY-N12507

    STING NF-κB Others
    Eupenicisirenin C (compound 1) is a sirenin derivative. Eupenicisirenin C has strong NF-κB inhibitory activities. Eupenicisirenin C suppresses effects on cGAS-STING pathway. Eupenicisirenin C inhibits RANKL-induced osteoclast differentiation in bone marrow macrophage cells .
    Eupenicisirenin C
  • HY-P3041

    Calcium Channel Endocrinology
    Chromostatin bovine is a chromogranin A (CGA) derivative peptide, which inhibits postassium or carbamoylcholine induced catecholamine release with an ID50 of 5 nM. Chromostatin bovine reduces calcium flux, enhances the desensitization process of the cholinergic-evoked secretory response and modulates the endocrine response associated with catecholamine .
    Chromostatin (bovine)
  • HY-176541

    STING Inflammation/Immunology Cancer
    diABZI-Mal is a STING agonist. diABZI-Mal activates cGAS-STING pathway to induce cytokine production such as interferon-type I. diABZI-Mal promotes maturation of DC cells and efficiently induces CD8 + T immune reaction. diABZI-Mal inhibits tumor growth .
    diABZI-Mal
  • HY-158126

    DNA/RNA Synthesis Cancer
    G-quadruplex ligand 2 (compound A3) is a triphenylamine-based ligand that targets mitochondrial DNA G4s. G-quadruplex ligand 2 activates the cGAS-STING pathway. G-quadruplex ligand 2 inhibits tumor growth and metastasis via regulation of TME .
    G-quadruplex ligand 2
  • HY-141831

    Phosphodiesterase (PDE) Cancer
    STF-1084 is a specific, cell-impermeable, competitive inhibitor of ENPP1 (Ki = 33 nM). STF-1084 increases extracellular cGAMP concentrations by preventing its degradation by ENPP1, thereby enhancing immune infiltration. STF-1084 acts synergistically with ionizing radiation (IR) and cGAMP to delay tumor progression. STF-1084 can be used to study cancers with low immunogenicity .
    STF-1084
  • HY-114181
    IRAK4-IN-4
    1 Publications Verification

    IRAK Cyclic GMP-AMP Synthase Inflammation/Immunology
    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-P1680

    Asterin

    STING HSV Infection Inflammation/Immunology Cancer
    Astin C (Asterin) is a cyclopeptide that can be extracted from Aster tataricus. Astin C has anti-inflammatory and anti-cancer activities. Astin C can specifically inhibit the cGAS-STING signaling pathway, block the recruitment of IRF3 to the STING signalosome, and thus inhibit the innate inflammatory response. Astin C can be used in the research of autoimmune diseases and cancers .
    Astin C
  • HY-158045

    PROTACs PARP Inflammation/Immunology Cancer
    PROTAC PARP1 degrader-1 (Compound CN0) is a PROTAC degrader of PARP1. PROTAC PARP1 degrader-1 activates the cGAS/STING immunity pathway and eventually enhances T cell killing of tumor cells. PROTAC PARP1 degrader-1 inhibits DNA damage repair, resulting in highly efficient accumulation of cytosolic DNA fragments (Blue: CRBN ligand, Black: linker; Pink: PARP1 inhibitor) .
    PROTAC PARP1 degrader-1
  • HY-13735H

    Acriquine acetate

    Parasite Sodium Channel DNA Stain Apoptosis Cancer
    Quinacrine (Acriquine) acetate is a small molecule modulator of the cGAS-STING-TBK1 signaling pathway, possessing immune stimulatory activity. Quinacrine acetate has been explored for its potential therapeutic applications in enhancing anti-tumor immunity. Quinacrine acetate can improve the effectiveness of cancer immunotherapies by addressing the poor immunogenicity of various tumors. Quinacrine acetate also presents a promising strategy for overcoming the limitations associated with immune checkpoint inhibitors in cancer treatment.
    Quinacrine acetate
  • HY-169225

    PDIC-NS free base

    STING Apoptosis Reactive Oxygen Species (ROS) Inflammation/Immunology Cancer
    PDIC-NN (PDIC-NS free base) is a STING activator with anticancer activity. PDIC-NN promotes the content and biostability of endogenous cyclic dinucleotides (CDNs). PDIC-NN triggers ROS burst and causes serious damage to mitochondria. PDIC-NN induces cell apoptosis and inhibits DNA replication. PDIC-NN activates cGAS-STING signaling pathway, enhances the immunogenicity of tumor cells and activates a robust innate immune response .
    PDIC-NN
  • HY-169225A

    PDIC-NS

    STING Apoptosis Reactive Oxygen Species (ROS) Inflammation/Immunology Cancer
    PDIC-NN dimethanesulfonate (PDIC-NS) is a STING activator with anticancer activity. PDIC-NN dimethanesulfonate promotes the content and biostability of endogenous cyclic dinucleotides (CDNs). PDIC-NN dimethanesulfonate triggers ROS burst and causes serious damage to mitochondria. PDIC-NN dimethanesulfonate induces cell apoptosis and inhibits DNA replication. PDIC-NN dimethanesulfonate activates cGAS-STING signaling pathway, enhances the immunogenicity of tumor cells and activates a robust innate immune response .
    PDIC-NN dimethanesulfonate
  • HY-162944

    Ferroptosis Mitochondrial Metabolism STING Autophagy Cancer
    NA-Ir is a Ferroptosis inducer. NA-Ir targets mitochondrial DNA (mtDNA) and activates the cGAS-STING pathway to induce ferritinophagy (Autophagy), while also generating reactive oxygen species (ROS) through photodynamic therapy (PDT), depleting glutathione (GSH), and downregulating glutathione peroxidase 4 (GPX4), thereby triggering lipid peroxidation and Ferroptosis. NA-Ir exhibits higher anticancer activity under light exposure and selectively inhibits cancer cells with high H2S levels .
    NA-Ir
  • HY-160406

    STING IFNAR Cancer
    SNX281 is a systemically active non-CDN STING agonist that binds to the STING protein. SNX281 promotes signal transduction of the cGAS-STING pathway, and increases cellular responses to tumor cells. SNX281 activates STING and leads to the production of type I IFNs and proinflammarory cytokines, ultimately stimulating the infilatration of immune cells into the tumor microenvironment. SNX281 enhances anti-tumor immunity, potentially overcoming resistance to checkpoint inhibitors in some cancer. SNX281 can be used in the research for anti-tumor immunity .
    SNX281

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