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Immunology/Inflammation

Aryl Hydrocarbon Receptor

Immunology/Inflammation related

NOD-like Receptor (NLR)

Prostaglandin Receptor

Reactive Oxygen Species

Thrombopoietin Receptor

cGAS

Cyclic GMP-AMP synthase (cGAS, cGAMP synthase), belonging to the nucleotidyltransferase family, is a cytosolic DNA sensor that activates a type-I interferon response. It is part of the cGAS-STING DNA sensing pathway. It 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. Mice lacking cGAS are more vulnerable to lethal infection by DNA viruses and RNA viruses. In addition, cGAS has been shown to be an innate immune sensor of retroviruses including HIV. The human gene encoding cGAS is MB21D1 on chromosome 6.

Filter HomeSignaling PathwaysImmunology/InflammationcGAS

2',3'-cGAMP sodium

2'-3'-cyclic GMP-AMP sodium

T10065L2734858-36-5In house

2',3'-cGAMP sodium (2'-3'-cyclic GMP-AMP sodium) is a second messenger in cellular innate immunity, catalyzed by cGAMP synthase (cGAS) under DNA binding conditions. It binds to STING to form a dimer, inducing the production and expression of interferon-β and other cytokines.

cGAS Endogenous Metabolite IFNAR STING

$247

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RU.521

RU320521

T54862262452-06-0

RU.521 (RU3205217) is a selective cyclic GMP-AMP synthetase (cGAS) inhibitor (mouse: IC50=0.11 μM), (human: IC50=2.94 μM). RU.521 is an inhibitor of the receptor activated by dsDNA (IC50=700 nM). RU.521 inhibits cGAS-mediated interferon upregulation. RU.521 reduces constitutive interferon expression in macrophages derived from a mouse model of Aicardi-Goutieres syndrome.

cGAS DNA

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Cited

G108

G-108, G 108

T696632369750-66-1In house

G108 is an inhibitor of human cGAS and is used in the study of autoimmune diseases associated with human cGAS.

cGAS

$490

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G150

T113442369751-30-2

G150 inhibited interferon expression triggered by DSDNA with IC50 of 10.2 nM.G150 is an effective and highly selective inhibitor of human cyclic GMP-AMP synthase (H-CGAS).

cGAS DNA

$128

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G140

T92132369751-07-3

G140 is a potent and selective inhibitor of cyclic GMP-AMP synthase (cGAS).

cGAS

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Decoyinine

Decynylene, Angustmycin A

T150912004-04-8

Decoyinine (Decynylene), a selective inhibitor of GMP synthase, is a novel potential microbial insecticide, a secondary metabolite produced by Streptomyces hygroscopicus.Decoyinine induces resistance in rice to the small brown ladybug Laodelphax striatellus.

cGAS Others

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HA-1004

T2752591742-10-8In house

HA-1004 is a inhibitor of PKG, PKA, PKC and MLC.

cGAS ERK PKA PKC Serine/threonin kinase

$195

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PF-06928215

T124322378173-15-8

PF-06928215 is an inhibitor of cGAS (cyclic GMP-AMP Synthase) (IC50 of 4.9 μΜ).

cGAS

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3'-Adenylic acid

T2005584-21-9

3'-Adenylic acid is an agent of bioactive chemical.

cGAS Nucleoside Antimetabolite/Analog Others

$133

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IRAK4-IN-4

T116731850276-58-2

IRAK4-IN-4 (compound 15) inhibits cyclic GMP-AMP synthase (cGAS) with an IC50 of 2.1 nM.IRAK4-IN-4 is an interleukin-1 receptor–associated kinase 4 (IRAK4) inhibitor, has an IC50 of 2.8 nM.

cGAS IRAK

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HA-1004 dihydrochloride

T868192564-34-6

HA-1004 dihydrochloride is an inhibitor of PKA, PKC, cGKI, MYLK, and calcium channel protein

Calcium Channel cGAS ERK PKA PKC

$370

6-8 weeks

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CU-32

T383282400954-16-5

CU-32 is an inhibitor of cyclic GMP-AMP (cGAMP) synthase (cGAS; IC50= 0.45 μM).1It reduces DNA-, but not Sendai virus-, induced dimerization of IFN regulatory factor 3 in THP-1 cells, indicating selectivity for the cGAS DNA sensing pathway over the RIG-I-MAVS RNA sensing pathway. It is also selective for cGAS over toll-like receptors (TLRs) at 50 μM. CU-32 decreases IFN-stimulatory DNA-induced production of IFN-β in THP-1 cells when used at concentrations of 10, 30, and 100 μM. 1.Padilla-Salinas, R., Sun, L., Anderson, R., et al.Discovery of small-molecule cyclic GMP-AMP synthase inhibitorsJ. Org. Chem.85(3)1579-1600(2020)

cGAS Others

$287

35 days

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Cladophorol A

T203535146776-30-9

Cladophorol A is a cGAS inhibitor that obstructs its activity by binding to the conserved adenosine nucleotide binding site of cGAS. It effectively suppresses the overactivation of the cGAS-STING pathway at non-cytotoxic concentrations, with an IC50 of 370 nM. Cladophorol A holds potential for research into inflammatory diseases linked to the overactivation of the cGAS-STING pathway.

cGAS STING

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10-14 weeks

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cGAS-IN-4

T2046122987886-49-5

cGAS-IN-4 (Compound 36) is an orally active inhibitor of cyclic GMP-AMP synthase (cGAS) with IC50 values of 32 nM for human cGAS (h-cGAS) and 5.8 nM for mouse cGAS (m-cGAS). In THP-1 cells, cGAS-IN-4 inhibits cGAMP with an IC50 of 60 nM, enhancing cellular potency. Additionally, cGAS-IN-4 exhibits anti-inflammatory effects in a mouse model of Concanavalin A-induced acute liver injury.

cGAS

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10-14 weeks

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(R)-cGAS-IN-4

T2071612987886-48-4

(R)-cGAS-IN-4 (Compound 77A*) is the R-enantiomer of cGAS-IN-4, which acts as an orally active inhibitor of cyclic GMP-AMP synthase-adenosine synthase (cGAS).

cGAS

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10-14 weeks

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PROTAC cGAS degrader-1

T205651

PROTAC cGAS degrader-1 (Compound TH35) is a potent and selective cGAS PROTAC degrader, exhibiting DC50 values of 0.9 μM in THP-1 cells and 4.6 μM in RAW 264.7 cells. It effectively inhibits the activation of cGAS signaling induced by dsDNA. PROTAC cGAS degrader-1 also demonstrates anti-inflammatory properties, making it suitable for research into cGAS-related inflammatory diseases. (Pink: cGAS inhibitor; Black: Linker; Blue: E3 ligase ligand)

cGAS PROTACs

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CU-76

T383292400954-58-5

CU-76 is an inhibitor of cyclic GMP-AMP synthase (cGAS; IC50= 0.24 μM).1It reduces DNA-, but not Sendai virus-, induced dimerization of IFN regulatory factor 3 in THP-1 cells, indicating selectivity for the cGAS DNA sensing pathway over the RIG-I-MAVS RNA sensing pathway. CU-76 decreases IFN-stimulatory DNA-induced production of IFN-β in THP-1 cells when used at concentrations of 10, 30, and 100 μM. 1.Padilla-Salinas, R., Sun, L., Anderson, R., et al.Discovery of small-molecule cyclic GMP-AMP synthase inhibitorsJ. Org. Chem.85(3)1579-1600(2020)

cGAS Others

$987

35 days

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cGAS-IN-3

T209815

cGAS-IN-3 (compound 30d-S) is an orally active inhibitor of cyclic GMP-AMP synthase (cGAS) that exhibits excellent plasma exposure and low clearance rate. It demonstrates anti-inflammatory properties, significantly reducing pulmonary inflammation in rats.

cGAS

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MS7829

T200590

MS7829 is a first-class DUBTAC targeting cGAS, a critical component in the cGAS-STING pathway.

cGAS Others

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cGAS-IN-1

T78858858770-07-7

cGAS-IN-1 (compound C20), a flavonoid that acts as a Cyclic GMP-AMP Synthase (cGAS) inhibitor, demonstrates IC50 values of 2.28 μM for human cGAS and 1.44 μM for mouse cGAS. By inhibiting the abnormal activation of cGAS linked to numerous immune-mediated inflammatory diseases, cGAS-IN-1 possesses potential anti-inflammatory properties [1].

cGAS Others

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8-10 weeks

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cGAS-IN-2

T860422765273-11-6

cGAS-IN-2 (compound 109) serves as a potent inhibitor of Cyclic GMP-AMP Synthase (cGAS), exhibiting an IC50 of 0.01512 μM against h-cGAS [1].

cGAS

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10-14 weeks

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2',3'-cGAMP

Cyclic GMP-AMP, 2'-3'-Cyclic GMP-AMP

T100651441190-66-4

2',3'-cGAMP is an endogenous cyclic dinucleotide (CDN) produced by cGAS (cGAMP synthase) in response to double-stranded DNA in the cytoplasm. It acts as a STING activator and ligand, inducing interferons (IFNs) via the TBK1/IRF3 pathway and pro-inflammatory factors via the NF-κB pathway.

cGAS COX Endogenous Metabolite IFNAR Immunology/Inflammation related STING

$247

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Cited

QKY-613

T2031932484713-92-8

QKY-613 is a prodrug designed to enhance immune surveillance by targeting nucleic acid modification pathways. It selectively facilitates the incorporation of 6mdA (N6-methyl-deoxyadenosine) into viral DNA, boosting the DNA's phase separation potential and subsequently increasing cGAS activation levels to strengthen host immune surveillance. In mouse models of viral infection, QKY-613 significantly reduced mortality in aged mice. This compound holds promise for studying immune surveillance mechanisms based on nucleic acid modifications.

cGAS Others

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10-14 weeks

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