E0127New |
C-170
|
C-170 is a covalent small-molecule inhibitor of STING. C-170 efficiently inhibits both hsSTING and mmSTING through the same covalent modification with C-171.
|
|
|
E0128New |
C-171
|
C-171 is a covalent small-molecule inhibitor of STING. C-171 efficiently inhibits both hsSTING and mmSTING through covalently target the predicted transmembrane cysteine residue 91 and thereby block the activation-induced palmitoylation of STING.
|
|
|
S1113 |
GSK690693
|
GSK690693 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. |
-
Am J Cancer Res, 2022, 12(4):1535-1555
-
Cell Death Discov, 2022, 8(1):197
-
Mech Ageing Dev, 2022, 202:111633
|
|
S6494 |
CCCP
|
CCCP (Carbonyl cyanide m-chlorophenyl hydrazone, Carbonyl cyanide 3-chlorophenylhydrazone), 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). |
-
Cell Res, 2022, 32(2):119-138
-
Cell Death Dis, 2022, 13(5):436
-
Biochem Pharmacol, 2022, S0006-2952(22)00226-X
|
|
S6575 |
C-176
|
STING inhibitor C-176 is a potent, small-molecule inhibitor of STING, a central signaling component of the intracellular DNA sensing pathway. |
-
Cell Rep, 2022, 39(7):110814
-
FASEB J, 2022, 36(5):e22266
-
Cell Biol Toxicol, 2022, 10.1007/s10565-021-09692-z
|
|
S6667 |
STING inhibitor C-178
|
C-178 is a covalent inhibitor of STING,covalently bind to Cys91. |
|
|
S7904 |
2',3'-cGAMP Sodium Salt
|
2',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. |
|
|
S7905 |
3',3'-cGAMP
|
3',3'-cGAMP (3',3'-cyclic GMP-AMP, Cyclic GMP-AMP, cGAMP) activates the endoplasmic reticulum (ER)-resident receptor stimulator of interferon genes (STING), thereby inducing an antiviral state and the secretion of type I IFNs. |
|
|
E1066New |
SN-011 (GUN35901)
|
SN-011 (GUN35901) is a STING-specific antagonist with IC50 of 76 nM.
|
|
|
S6652 |
H-151
|
H-151 is a highly potent and covalent antagonist of STING that has noteworthy inhibitory activity both in human cells and in vivo. |
-
Cell Rep, 2022, 39(7):110814
-
Sci Immunol, 2021, 6(59)eabi9007
-
Cell Mol Life Sci, 2021, 10.1007/s00018-021-03902-x
|
|
E2664New |
Cridanimod
|
Cridanimod, a low-Mw interferon-inducer (IFN-inducer), recognizes the intracellular signaling protein stimulator of interferon genes (STING), resulting in the STING-TBK1-IRF3 pathway activation and synthesis of type I IFNs (subtypes IFN-α and IFN-β). |
|
|
S0853 |
SR-717 lithium
|
SR-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. |
-
Signal Transduct Target Ther, 2021, 6(1):382
|
|
S1537 |
Vadimezan (ASA404)
|
Vadimezan (ASA404, NSC 640488, DMXAA) 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. |
-
Cell, 2022, 185(1):169-183.e19
-
Nat Immunol, 2022, 23(2):287-302
-
Nat Cell Biol, 2022, 24(5):766-782
|
|
S3804 |
Alpha-Mangostin
|
Alpha-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. |
-
Front Pharmacol, 2021, 12:692806
|
|
S8796 |
diABZI STING agonist (Compound 3)
|
diABZI STING agonist (diABZI STING agonist-1, Compound 3, Tautomerism) is a potent non-nucleotide STING agonist and has tremendous potential to improve treatment of cancer in humans. |
-
Nat Cell Biol, 2022, 24(5):766-782
-
J Exp Med, 2022, 219(1)e20211818
-
Cell Rep, 2022, 38(2):110236
|
|
S8954 |
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. |
|
|
S9618New |
E7766 diammonium salt
|
E7766 diammonium salt, a macrocycle-bridged STING agonist with a Kd of 40 nM, shows potent pan-genotypic and antitumor activities. |
|
|
S9681 |
MSA-2
|
MSA-2 is an orally available non-nucleotide human STING agonist with antitumor activity. |
|
|
E0127New |
C-170
|
C-170 is a covalent small-molecule inhibitor of STING. C-170 efficiently inhibits both hsSTING and mmSTING through the same covalent modification with C-171.
|
|
|
E0128New |
C-171
|
C-171 is a covalent small-molecule inhibitor of STING. C-171 efficiently inhibits both hsSTING and mmSTING through covalently target the predicted transmembrane cysteine residue 91 and thereby block the activation-induced palmitoylation of STING.
|
|
|
S1113 |
GSK690693
|
GSK690693 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. |
- Am J Cancer Res, 2022, 12(4):1535-1555
- Cell Death Discov, 2022, 8(1):197
- Mech Ageing Dev, 2022, 202:111633
|
|
S6494 |
CCCP
|
CCCP (Carbonyl cyanide m-chlorophenyl hydrazone, Carbonyl cyanide 3-chlorophenylhydrazone), 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). |
- Cell Res, 2022, 32(2):119-138
- Cell Death Dis, 2022, 13(5):436
- Biochem Pharmacol, 2022, S0006-2952(22)00226-X
|
|
S6575 |
C-176
|
STING inhibitor C-176 is a potent, small-molecule inhibitor of STING, a central signaling component of the intracellular DNA sensing pathway. |
- Cell Rep, 2022, 39(7):110814
- FASEB J, 2022, 36(5):e22266
- Cell Biol Toxicol, 2022, 10.1007/s10565-021-09692-z
|
|
S6667 |
STING inhibitor C-178
|
C-178 is a covalent inhibitor of STING,covalently bind to Cys91. |
|
|
E2664New |
Cridanimod
|
Cridanimod, a low-Mw interferon-inducer (IFN-inducer), recognizes the intracellular signaling protein stimulator of interferon genes (STING), resulting in the STING-TBK1-IRF3 pathway activation and synthesis of type I IFNs (subtypes IFN-α and IFN-β). |
|
|
S0853 |
SR-717 lithium
|
SR-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. |
- Signal Transduct Target Ther, 2021, 6(1):382
|
|
S1537 |
Vadimezan (ASA404)
|
Vadimezan (ASA404, NSC 640488, DMXAA) 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. |
- Cell, 2022, 185(1):169-183.e19
- Nat Immunol, 2022, 23(2):287-302
- Nat Cell Biol, 2022, 24(5):766-782
|
|
S3804 |
Alpha-Mangostin
|
Alpha-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. |
- Front Pharmacol, 2021, 12:692806
|
|
S8796 |
diABZI STING agonist (Compound 3)
|
diABZI STING agonist (diABZI STING agonist-1, Compound 3, Tautomerism) is a potent non-nucleotide STING agonist and has tremendous potential to improve treatment of cancer in humans. |
- Nat Cell Biol, 2022, 24(5):766-782
- J Exp Med, 2022, 219(1)e20211818
- Cell Rep, 2022, 38(2):110236
|
|
S8954 |
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. |
|
|
S9618New |
E7766 diammonium salt
|
E7766 diammonium salt, a macrocycle-bridged STING agonist with a Kd of 40 nM, shows potent pan-genotypic and antitumor activities. |
|
|
S9681 |
MSA-2
|
MSA-2 is an orally available non-nucleotide human STING agonist with antitumor activity. |
|
|