STING
Inhibitory Selectivity
STING Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1113 |
GSK690693GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1. |
UPN cells were treated with GSK690693 or MK2206 (1 uM) for 1h followed by LPA (10 uM), EGF or IGF-1 (10 ng/ml) for another 1h and Western blot was performed. Band intensities of phospho-AKT (p-AKTS473), phospho-S6 (p-S6S240/S244), phospho-YB-1 (p-YB-1S102) and YB-1 were quantified and normalized to the intensity of ERK2. It directly determined the role of AKT using two potent, AKT inhibitors with distinct actions—a catalytic domain inhibitor, GSK690693, and an allosteric inhibitor, MK2206 -in UPN and SKOV3 cells, which showed appreciable AKT and YB-1 phosphorylation upon growth factor stimulation. GSK690693 increased basal and growth factor-induced AKT phosphorylation due to blocking a negative feedback loop downstream of AKT, whereas MK2206 abolished both basal and growth-factor-induced AKT phosphorylation.
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| S6494 |
CCCPCCCP (Carbonyl cyanide m-chlorophenyl hydrazone), an oxidative phosphorylation inhibitor, is a protonophore mitochondrial uncoupler that increases membrane permeability to protons, leading to a disruption in the mitochondrial membrane potential. Carbonyl cyanide 3-chlorophenylhydrazone (CCCP), the protonophore, can inhibits STING-mediated IFN-β production via disrupting mitochondrial membrane potential (MMP). |
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| S6667 |
STING inhibitor C-178C-178 is a covalent inhibitor of STING,covalently bind to Cys91. |
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| S6575 |
C-176 (STING inhibitor)STING inhibitor C-176 is a potent, small-molecule inhibitor of STING, a central signaling component of the intracellular DNA sensing pathway. |
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| S7904New |
2',3'-cGAMP Sodium Salt2',3'-cGAMP Sodium Salt (2'-3'-cyclic GMP-AMP Sodium) is produced in response to DNA in the cytoplasm in mammalian cells and binds STING with high affinity and is an effective inducer of interferon-β (IFNβ). 2',3'-cGAMP binds to STING with Kd of 3.79 nM. |
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| S7905New |
3',3'-cGAMP3',3'-cGAMP (3',3'-cyclic GMP-AMP) activates the endoplasmic reticulum (ER)-resident receptor stimulator of interferon genes (STING), thereby inducing an antiviral state and the secretion of type I IFNs. |
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| S6652 |
H-151H-151 is a highly potent and covalent antagonist of STING that has noteworthy inhibitory activity both in human cells and in vivo. |
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| S1537 |
DMXAA (Vadimezan)DMXAA (Vadimezan) is a vascular disrupting agents (VDA) and competitive inhibitor of DT-diaphorase with Ki of 20 μM and IC50 of 62.5 μM in cell-free assays, respectively. DMXAA (Vadimezan) is also a STING agonist with potential antineoplastic activity. DMXAA (Vadimezan) potently induces IFN-β but relatively low TNF-α expression in vitro. DMXAA (Vadimezan) has antiviral activity. Phase 3. |
(B and C) sh-scrambled or sh-ck2a–transducted L929 cells (B) and Raw cells (C) were stimulated by DMXAA (100 μg/ml) for various times. Cytosolic and nuclear extracts were prepared as described in Materials and Methods. Five percent of the cytosolic proteins and 20% of the nuclear proteins were resolved by 10% SDS-PAGE. Subsequently, immunoblotting was conducted by indicated Abs. The amounts of Tubulin and Lamin B1 in cytosol versus nuclei detected by respective Abs were used as internal control for fractionation.
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| S8954New |
STING agonist-1 (G10)STING agonist-1 (G10) is a novel human-specific STING agonist that triggers IFN regulatory factor 3 (IRF3)/ type I interferon (IFN)-associated transcription in human fibroblasts. STING agonist-1 (G10) potently reduces growth of Chikungunya virus (CHIKV) with IC90 of 8.01 μM and blocks replication of Alphavirus species Venezuelan Equine Encephalitis Virus (VEEV) with IC90 of 24.57 μM. |
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| S9681New |
MSA-2MSA-2 is an orally available non-nucleotide human STING agonist with antitumor activity. |
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| S0853New |
SR-717 lithiumSR-717 lithium is a non-nucleotide STING agonist that demonstrates broad interspecies and interallelic specificity with EC50 of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 (cGAS KO) cell lines, respectively. SR-717 lithium also induces the expression of clinically relevant targets, including programmed cell death 1 ligand 1 (PD-L1), in a STING-dependent manner. SR-717 lithium exhibits antitumor activity. |
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| S9616New |
diABZI STING agonist-1diABZI STING agonist-1 is a selective agonist of the stimulator of interferon genes (STING) with EC50 of 130 nM and 186 nM for human STING and mouse STING activation, respectively. |
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| S3804 |
Alpha-MangostinAlpha-mangostin is the main xanthone purified from mangosteen and has health promoting benefits including anti-bacterial, anti-inflammatory, anti-oxidant, anti-cancer and cardioprotective activities. alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a Ki of 2.85 μM. Alpha-mangostin is also an agonist of human STING. |
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| S8796 |
diABZI STING agonist (Compound 3)diABZI STING agonist (Compound 3) is a potent non-nucleotide STING agonist and has tremendous potential to improve treatment of cancer in humans. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1113 |
GSK690693GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1. |
UPN cells were treated with GSK690693 or MK2206 (1 uM) for 1h followed by LPA (10 uM), EGF or IGF-1 (10 ng/ml) for another 1h and Western blot was performed. Band intensities of phospho-AKT (p-AKTS473), phospho-S6 (p-S6S240/S244), phospho-YB-1 (p-YB-1S102) and YB-1 were quantified and normalized to the intensity of ERK2. It directly determined the role of AKT using two potent, AKT inhibitors with distinct actions—a catalytic domain inhibitor, GSK690693, and an allosteric inhibitor, MK2206 -in UPN and SKOV3 cells, which showed appreciable AKT and YB-1 phosphorylation upon growth factor stimulation. GSK690693 increased basal and growth factor-induced AKT phosphorylation due to blocking a negative feedback loop downstream of AKT, whereas MK2206 abolished both basal and growth-factor-induced AKT phosphorylation.
|
|
| S6494 |
CCCPCCCP (Carbonyl cyanide m-chlorophenyl hydrazone), an oxidative phosphorylation inhibitor, is a protonophore mitochondrial uncoupler that increases membrane permeability to protons, leading to a disruption in the mitochondrial membrane potential. Carbonyl cyanide 3-chlorophenylhydrazone (CCCP), the protonophore, can inhibits STING-mediated IFN-β production via disrupting mitochondrial membrane potential (MMP). |
||
| S6667 |
STING inhibitor C-178C-178 is a covalent inhibitor of STING,covalently bind to Cys91. |
||
| S6575 |
C-176 (STING inhibitor)STING inhibitor C-176 is a potent, small-molecule inhibitor of STING, a central signaling component of the intracellular DNA sensing pathway. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7904New |
2',3'-cGAMP Sodium Salt2',3'-cGAMP Sodium Salt (2'-3'-cyclic GMP-AMP Sodium) is produced in response to DNA in the cytoplasm in mammalian cells and binds STING with high affinity and is an effective inducer of interferon-β (IFNβ). 2',3'-cGAMP binds to STING with Kd of 3.79 nM. |
||
| S7905New |
3',3'-cGAMP3',3'-cGAMP (3',3'-cyclic GMP-AMP) activates the endoplasmic reticulum (ER)-resident receptor stimulator of interferon genes (STING), thereby inducing an antiviral state and the secretion of type I IFNs. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S6652 |
H-151H-151 is a highly potent and covalent antagonist of STING that has noteworthy inhibitory activity both in human cells and in vivo. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1537 |
DMXAA (Vadimezan)DMXAA (Vadimezan) is a vascular disrupting agents (VDA) and competitive inhibitor of DT-diaphorase with Ki of 20 μM and IC50 of 62.5 μM in cell-free assays, respectively. DMXAA (Vadimezan) is also a STING agonist with potential antineoplastic activity. DMXAA (Vadimezan) potently induces IFN-β but relatively low TNF-α expression in vitro. DMXAA (Vadimezan) has antiviral activity. Phase 3. |
(B and C) sh-scrambled or sh-ck2a–transducted L929 cells (B) and Raw cells (C) were stimulated by DMXAA (100 μg/ml) for various times. Cytosolic and nuclear extracts were prepared as described in Materials and Methods. Five percent of the cytosolic proteins and 20% of the nuclear proteins were resolved by 10% SDS-PAGE. Subsequently, immunoblotting was conducted by indicated Abs. The amounts of Tubulin and Lamin B1 in cytosol versus nuclei detected by respective Abs were used as internal control for fractionation.
|
|
| S8954New |
STING agonist-1 (G10)STING agonist-1 (G10) is a novel human-specific STING agonist that triggers IFN regulatory factor 3 (IRF3)/ type I interferon (IFN)-associated transcription in human fibroblasts. STING agonist-1 (G10) potently reduces growth of Chikungunya virus (CHIKV) with IC90 of 8.01 μM and blocks replication of Alphavirus species Venezuelan Equine Encephalitis Virus (VEEV) with IC90 of 24.57 μM. |
||
| S9681New |
MSA-2MSA-2 is an orally available non-nucleotide human STING agonist with antitumor activity. |
||
| S0853New |
SR-717 lithiumSR-717 lithium is a non-nucleotide STING agonist that demonstrates broad interspecies and interallelic specificity with EC50 of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 (cGAS KO) cell lines, respectively. SR-717 lithium also induces the expression of clinically relevant targets, including programmed cell death 1 ligand 1 (PD-L1), in a STING-dependent manner. SR-717 lithium exhibits antitumor activity. |
||
| S9616New |
diABZI STING agonist-1diABZI STING agonist-1 is a selective agonist of the stimulator of interferon genes (STING) with EC50 of 130 nM and 186 nM for human STING and mouse STING activation, respectively. |
||
| S3804 |
Alpha-MangostinAlpha-mangostin is the main xanthone purified from mangosteen and has health promoting benefits including anti-bacterial, anti-inflammatory, anti-oxidant, anti-cancer and cardioprotective activities. alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a Ki of 2.85 μM. Alpha-mangostin is also an agonist of human STING. |
||
| S8796 |
diABZI STING agonist (Compound 3)diABZI STING agonist (Compound 3) is a potent non-nucleotide STING agonist and has tremendous potential to improve treatment of cancer in humans. |
