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Immunology/Inflammation

Aryl Hydrocarbon Receptor

Immunology/Inflammation related

NOD-like Receptor (NLR)

Prostaglandin Receptor

Reactive Oxygen Species

Thrombopoietin Receptor

STING

Stimulator of interferon genes (STING), also known as transmembrane protein 173 (TMEM173) and MPYS/MITA/ERIS is a protein that in humans is encoded by the STING1 gene. STING plays an important role in innate immunity. STING induces type I interferon production when cells are infected with intracellular pathogens, such as viruses, mycobacteria and intracellular parasites. Type I interferon, mediated by STING, protects infected cells and nearby cells from local infection by binding to the same cell that secretes it (autocrine signaling) and nearby cells (paracrine signaling.) It thus plays an important role, for instance, in controlling norovirus infection. STING works as both a direct cytosolic DNA sensor (CDS) and an adaptor protein in Type I interferon signaling through different molecular mechanisms. It has been shown to activate downstream transcription factors STAT6 and IRF3 through TBK1, which are responsible for antiviral response and innate immune response against intracellular pathogen.

Filter HomeSignaling PathwaysImmunology/InflammationSTING

Dazostinag disodium

T724822553413-93-5In house

Dazostinag disodium (TAK-676) is a synthetic novel interferon gene (STING) agonist that triggers STING signaling pathway activation and type I interferon activation. Dazostinag disodium (TAK-676) is also a highly effective immune system modulator with complete resolution and lasting memory of T cell immunity and the ability to promote lasting interferon-dependent anti-tumor immune responses.

$498

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2',3'-cGAMP 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.

$247

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diABZI STING agonist-1 trihydrochloride

T55162138299-34-8In house

diABZI STING agonist-1 (trihydrochloride) is a stimulator of interferon genes (STING) receptor agonist.

$175

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Cited

H-151

T5674941987-60-6

H-151 is a highly potent and selective STING antagonist. H-151 covalently binds to Cys91 of STING and inhibits palmitoylation of Cys91, thereby inhibiting STING activity. H-151 can be used in the study of autoinflammatory diseases in vivo and ex vivo.

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Vadimezan

T6273117570-53-3

Vadimezan (DMXAA) is a vascular disrupting agent, a murine STING agonist, and an inducer of cytokines such as type I IFN. Vadimezan has antitumor activity and induces a rapid cessation of blood flow in tumors without affecting blood flow in normal tissues.

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diABZI STING agonist-1 (Tautomerism)

T110352138498-18-5

diABZI STING agonist-1 (Tautomerism) (diABZI STING agonist (Compound 3)) is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively.

$168

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Omaveloxolone

T69191474034-05-3

Omaveloxolone (RTA-408) (RTA-408) is a synthetic triterpenoid that activates the cytoprotective transcription factor Nrf2 and inhibits NF-κB signaling. Phase 2.

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SR-717

T86552375421-09-1

SR-717 is a cGAMP analog, a non-nucleoside STING agonist that induces a closed activation conformation of STING. SR-717 has antitumor activity and promotes activation of immune cells and cross-presentation of antigens.

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Cyclic-di-GMP disodium

T369832222132-40-1

Cyclic-di-GMP disodium (5GP-5GP disodium) is a STING agonist and a second messenger in bacteria. It is involved in a variety of processes in prokaryotes, including biofilm formation, motility, and cell cycle progression. Cyclic-di-GMP disodium (5GP-5GP disodium) exhibits antiproliferative activity against cancer cells, inducing increased CD4 receptor expression and cell cycle arrest, and is a novel therapeutic agent that can be developed to prevent or treat cancer.

$139

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MSA-2

T8798129425-81-6

MSA-2 is an orally available non-nucleotide STING agonist. The non-covalent dimer of MSA-2 binds to STING with nanomolar affinity. It shows anti-tumor activity in syngeneic mouse tumor models, synergizes with anti-PD-1, stimulates tumor secretion of interferon-β, induces tumor regression, and has long-lasting anti-tumor immunity. [3]

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C-176

T5154314054-00-7

C-176 (STING inhibitor 1) is a STING inhibitor with selectivity and blood-brain barrier permeability. C-176 inhibits STING-mediated IFNβ production and possesses anti-inflammatory activity.

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diABZI STING agonist-1

T737462138299-33-7In house

diABZI STING agonist-1 is a selective and potent interferon gene-stimulating receptor (STING) agonist with potential antitumor and anti-inflammatory activity for the study of cancer.

$148

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CCCP

T7081555-60-2

CCCP (Carbonyl Cyanide m-Chlorophenylhydrazone) is an oxidative phosphorylation (OXPHOS) inhibitor and mitochondrial proton carrier uncoupler. CCCP inhibits the activation of STING and its downstream signaling molecules TBK1 and IRF3.

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STING activator Compound 53

T98532259624-71-8

STING activator Compound 53 based on an oxindole core structure demonstrated robust on-target functional activation of STING (human EC50 185 nM) in immortalised and primary cells and a cytokine induction fingerprint consistent with STING activation.

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SN-011

T91372249435-90-1

SN-011 (GUN35901) is a STING inhibitor, which inhibited the activation of the STING signal pathway and to prevent or treat a STING- mediated disease. It is a demethyl analogue of DUN99845.

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Gelsevirine

TN167838990-03-3

Gelsevirine, a novel STING-specific inhibitor, is an alkaloid from Gelsemium elegans with anxiolytic and antiproliferative activities that inhibits interferon and inflammatory cytokine induction in macrophages exposed to STING agonists, and attenuates STING-related inflammation in sepsis.

$243

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diABZI-C2-NH2

T395972137975-93-8

diABZI-C2-NH2 is an agonist of the interferon gene STING that modulates STING-dependent type I interferon production and can be used to study STING-mediated diseases.

$699

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Cridanimod

T531738609-97-1

Cridanimod (10-carboxymethyl-9-acridanone, CMA) is a potent STING agonist that directly binds to STING and triggers a strong antiviral response through the TBK1 IRF3 route.

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STING agonist-1

T8328702662-50-8

STING agonist-1 (G10) is a human-specific agent that elicits antiviral activity against emerging Alphaviruses.

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STING agonist-4

T130152138300-40-8

STING agonist-4 is an agonist of stimulator of Interferon Genes (STING) receptor(IC50 of 20 nM).

$163

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STING-IN-2

T9028346691-38-1

STING-IN-2 (C-170) is a potent, covalent inhibitor of STING, effectively targeting both mouse (mmSTING) and human STING (hsSTING), and is applicable for autoinflammatory disease research.

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STING-IN-3

T90292244881-69-2

STING-IN-3 (C-171) is an inhibitor of stimulator of interferon genes (STING). It binds to STING, inhibits its palmitoylation, and prevents the recruitment and phosphorylation of TBK1.

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SN-001

T9204727699-84-5

SN-001 was reported as a STING inhbiitor, which inhibited the activation of the STING signal pathway and to prevent or treat a STING- mediated disease.

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SN-008

T95542249106-01-0In house

SN-008 is a less active analog SN-011 which is a STING antagonist. SN-008 can be used as a negative control.

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ChX710

T136132438721-44-7

ChX710 activates the type I interferon response to cytosolic DNA by priming specific Interferon-Stimulated Genes (ISGs), inducing the ISRE promoter sequence, and facilitating the phosphorylation of Interferon Regulatory Factor (IRF) 3.

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C-178

T7329329198-87-0

C-178 is a covalent inhibitor of STING, binds to Cys91 on STING to block its palmitoylation and prevents recruitment and phosphorylation of TBK1 in HEK293T cells.

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STING agonist-30

T748092951078-67-2In house

STING agonist-30 is a potent activator of STING-dependent immune responses, demonstrating broad-spectrum antiviral effects against viruses such as HSV (Herpes Simplex Virus), rotavirus, and SARS-CoV-2 (Severe Acute Respiratory Syndrome Coronavirus 2).

$293

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STING (WT/R232) activity regulator 126

T60000702662-64-4

STING (WT R232) activity regulator 126 is a STING modulator with antibacterial and antiviral effects.

$117

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ADU-S100 ammonium salt

T10252L21638750-96-5

ADU-S100 ammonium salt is an activator of stimulator of interferon genes (STING). ADU-S100 ammonium salt leads to potent and systemic tumor regression and immunity.

$433

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Astin C

TN3464148057-23-2

Astin C (Asterin), a naturally occurring cyclic peptide that can be extracted from Aster tataricus, specifically blocks IRF3 recruitment at the STING signalosome inhibiting cGAS-STING signaling and innate inflammatory responses triggered by cytoplasmic dna, resulting in mice that are more susceptible to HSV-1 infection and significantly attenuating autoinflammatory responses.

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2',3'-cGAMP

T100651441190-66-4

2',3'-cGAMP (2'-3'-cyclic GMP-AMP) 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.

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Cited

C-di-IMP disodium

T82760

C-di-IMP disodium, a STING agonist, is utilized in tumor research [1].

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Enpp-1-IN-25

T2051383067908-20-4

Enpp-1-IN-25 (Compound 30) is an ENPP1 inhibitor with an IC50 of 8.05 nM and exhibits low oral bioavailability. By inhibiting cGAMP degradation, it effectively activates the intracellular STING pathway. Enpp-1-IN-25 can enhance immune cell infiltration and type I interferon response in the tumor microenvironment, thereby increasing the antitumor efficacy of anti-PD-L1 antibodies. It is applicable for research in cancer immunotherapy.

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10-14 weeks

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Anti-inflammatory agent 65

T830473035442-58-8

Anti-inflammatory agent 65 (compound 29), a Hederagonic acid derivative, exhibits potent activity by inhibiting nitric oxide (NO) release, nuclear translocation of IRF3 and p65, and disrupting the STING IRF3 NF-κB signaling pathway, thus attenuating the inflammatory response [1].

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8-10 weeks

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STING ligand-2

T2016811307526-16-4

STING ligand-2 serves as a ligand for STING and can be utilized as the target protein ligand in the synthesis of the PROTAC degrader STING-IN-10.

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Antitumor agent-114

T793202757762-91-5

Antitumor Agent-114, a potent STING (stimulator of interferon genes) agonist, activates immune responses and diminishes tumor size in mouse breast cancer models, demonstrating potential applications in immunity and cancer research [1].

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8-10 weeks

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F-CRI1

T79199

F-CRI1, a potent STING agonist with a dissociation constant (K d) of 40.62 nM, is an 18F-labeled radioactive probe employed for visualizing STING in the tumor microenvironment [1].

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ZSA-51

T204978

ZSA-51 is an effective, orally active STING agonist with anticancer properties. It has the capability to remodel the immune microenvironment within tumors and lymph nodes.

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Cyclic GMP

TN90567665-99-8

Cyclic GMP is an endogenous second messenger that initiates interferon production in response to cytoplasmic DNA. It activates the stimulator of interferon genes (STING), triggering a signaling cascade that results in the production of type I interferons and other immune mediators. The conjugate of cyclic GMP and AMP, known as Cyclic-GMP-AMP, can induce the phosphorylation and nuclear translocation of IRF3, thereby enhancing antiviral immune responses. Additionally, Cyclic GMP may activate PDE to degrade cAMP, inhibit the myocardial calcium current ICa, and regulate cardiac contractility. The derivative 8-Br-cGMP exhibits antiplatelet activity, and Cyclic GMP is used in research related to antiviral immunity and cardiovascular diseases.

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diABZI-V/C-DBCO

T200187

Compound 3 (diABZI-V C-DBCO) functions as an efficient STING agonist. This compound acts by releasing diABZI-amine under the action of cathepsin B to activate STING, thereby inducing the production of interferon and other immune-activating molecules, which enhances the immune system's response to tumors. In THP1-Dual cells, the EC50 values for STING activation by diABZI-V C-DBCO and diABZI-amine are 1.47 nM and 0.144 nM, respectively, and in primary mouse splenic cells, the EC50 values are 7.7 µM and 0.17 µM, respectively. diABZI-V C-DBCO is useful for research in the field of cancer immunotherapy.

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STING-IN-10

T200847

STING-IN-10 (P8) serves as both a dual degrader and inhibitor of STING, exhibiting an impressive DC50 value of 2.58 μM in THP-1 cells. This compound also demonstrates anti-inflammatory activity.

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LB244

T79730

LB244, a homologue of BB-Cl-amidine, functions as an orally effective STING inhibitor with an EC50 value of 0.8 μM, applicable in the treatment of STING-dependent inflammatory diseases. However, pharmacokinetic studies have shown that LB244 exhibits limited oral activity in mice [1].

35 days

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SAP-04

T79779

SAP-04 is a potent, orally active STING agonist exhibiting significant immunomodulatory effects appropriate for cancer therapy [1].

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hSTING agonist-1

T204491

hSTING agonist-1 (compound 17) is a potent activator of hSTING. It has poor oral bioavailability but plays a significant role in inflammation research.

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GHN105

T205672

GHN105 is an orally active STING inhibitor that suppresses STING-dependent IFN-β secretion in THP-1 human monocytes with an IC50 of 4.4 μM. In mice, GHN105 reduces serum levels of IFN-β, IL-6, and CXCL10, and alleviates colitis in a DSS-induced acute colitis mouse model. Additionally, GHN105 demonstrates favorable pharmacokinetic properties in mice, with an oral bioavailability of 43% and a half-life of 1.1 hours.

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STING-IN-7

T81082899947-07-0

STING-IN-7 (compound 21) is a potent inhibitor of the stimulator of interferon genes (STING) pathway, with an inhibitory concentration (IC50) of 11.5 nM, effectively hampering the phosphorylation of both STING and interferon regulatory factor 3 (IRF3) [1].

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8-10 weeks

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STING-IN-5

T750112920064-17-9

STING-IN-5, a potent inhibitor of the Stimulator of Interferon Genes (STING) pathway, significantly suppresses lipopolysaccharide (LPS)-induced nitric oxide (NO) synthesis in macrophages, exhibiting an IC50 of 1.15 μM. This compound dampens the inflammatory response and offers potential for research into anti-inflammatory diseases and sepsis [1].

$1,370

8-10 weeks

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diABZI-4

T2005312138299-65-5

DiABZI-4 is an orally active STING agonist that exhibits broad-spectrum antiviral activity. It functions by activating STING to induce the production of pro-inflammatory cytokines and activation of lymphocytes. This action inhibits the replication of Influenza A virus (IAV), SARS-CoV-2, and Human Rhinovirus (HRV), with an EC50 range of 11.8-199 nM.

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