Cyclic GMP-AMP Synthase

cGAS

Cyclic GMP-AMP Synthase

Related Products

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 (27)
Antibodies (1)

By Effects:	Control (1) Inhibitors (21) Agonist (1) Degraders (2) Activators (2)

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).

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.

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.

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 (K_d).

HY-101835

Decoyinine	Inhibitor	99.96%
Decoyinine is a selective inhibitor of GMP synthetase (GMPS).

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))

HY-170362A

(R)-cGAS-IN-4	Control	99.94%
(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).

HY-174802

XL-3158	Inhibitor
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.

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.

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.

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.

HY-W587488

Adenosine 3′-monophosphate	Agonist	≥98.0%
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 A_2B receptors.

HY-164288

TDI-6570	Inhibitor	99.64%
TDI-6570 is a Cyclic GMP-AMP Synthase (cGAS) inhibitor with the IC₅₀ of 0.138 μM.

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.

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.

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

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.

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.

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.

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.

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Cyclic GMP-AMP Synthase

Cyclic GMP-AMP Synthase

Cyclic GMP-AMP Synthase Related Products (27)

Antibodies (1)

Cyclic GMP-AMP Synthase Related Products (27):