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. |
-
EMBO J, 2024, 10.1038/s44318-024-00244-9
-
EMBO Mol Med, 2024, 10.1038/s44321-024-00136-9
-
CNS Neurosci Ther, 2024, 30(8):e14913
|
|
S1537 |
Vadimezan (DMXAA)
|
Vadimezan (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. |
-
Mol Cancer, 2024, 23(1):186
-
Nat Commun, 2024, 15(1):1750
-
Cell Rep Med, 2024, 5(7):101648
|
|
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. |
-
Nature, 2024, 625(7995):585-592
-
Cell, 2024, 187(15):4043-4060.e30
-
Cell Rep Med, 2024, 5(7):101648
|
|
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. |
-
Nat Commun, 2024, 15(1):1785
-
Nat Commun, 2024, 15(1):1669
-
Redox Biol, 2024, 69:103002
|
|
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, 2024, 187(15):4043-4060.e30
-
Cancer Lett, 2024, 586:216695
-
J Transl Med, 2024, 22(1):796
|
|
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.Solutions are unstable and should be fresh-prepared. |
-
Mol Cell, 2024, 84(20):3979-3996.e9
-
Acta Pharm Sin B, 2024, 14(5):2194-2209
-
EMBO J, 2024, 10.1038/s44318-024-00244-9
|
|
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. |
-
Mol Neurobiol, 2022, 59(11):7006-7024
-
J Inflamm Res, 2022, 15:5103-5119
-
Signal Transduct Target Ther, 2021, 6(1):382
|
|
S6667 |
STING inhibitor C-178
|
C-178 is a covalent inhibitor of STING,covalently bind to Cys91. |
-
Research Square, 2023, Version 2
-
Cell Chem Biol, 2022, 29(10):1517-1531.e7
-
Cancer Cell, 2021, 39-9:1214-1226.e10
|
|
E0128 |
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. |
-
Cell Reports, 2023, 112328
-
Cell Rep, 2023, 42(4):112328
|
|
S8954 |
G10 (STING agonist-1)
|
G10 (STING agonist-1) 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. |
-
Int J Biol Sci, 2023, 19(11):3428-3440
|
|
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
|
|
E1787New |
SN-001
|
SN-001 is a potent inhibitor of STING that specifically inhibits STING activation and STING-dependent signaling. SN-011 significantly decreases inflammatory cytokine production and osteoclast formation in vivo. |
|
|
S9618 |
E7766 diammonium salt
|
E7766 diammonium salt, a macrocycle-bridged STING agonist with a Kd of 40 nM, shows potent pan-genotypic and antitumor activities. |
|
|
E1881New |
NVS-STG2
|
NVS-STG2(HY-157214) is a potent, allosteric small molecule agonist of STING. It binds at the transmembrane domain (TMD) interface of STING, thereby acting as a molecular glue to promote STING oligomerization and contribute to its activation. It may be used in research of STING-related autoimmune diseases. |
|
|
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. |
-
Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0
-
Life Sci Alliance, 2024, 7(6)e202402644
|
|
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. |
|
|
E1066 |
SN-011
|
SN-011 is a STING-specific antagonist with IC50 of 76 nM.
|
-
Mol Cancer, 2024, 23(1):186
|
|
E2664 |
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). |
|
|
E0127 |
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. |
|
|
S1537 |
Vadimezan (DMXAA)
|
Vadimezan (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. |
-
Mol Cancer, 2024, 23(1):186
-
Nat Commun, 2024, 15(1):1750
-
Cell Rep Med, 2024, 5(7):101648
|
|
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.Solutions are unstable and should be fresh-prepared. |
-
Mol Cell, 2024, 84(20):3979-3996.e9
-
Acta Pharm Sin B, 2024, 14(5):2194-2209
-
EMBO J, 2024, 10.1038/s44318-024-00244-9
|
|
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. |
-
Mol Neurobiol, 2022, 59(11):7006-7024
-
J Inflamm Res, 2022, 15:5103-5119
-
Signal Transduct Target Ther, 2021, 6(1):382
|
|
S8954 |
G10 (STING agonist-1)
|
G10 (STING agonist-1) 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. |
-
Int J Biol Sci, 2023, 19(11):3428-3440
|
|
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
|
|
S9618 |
E7766 diammonium salt
|
E7766 diammonium salt, a macrocycle-bridged STING agonist with a Kd of 40 nM, shows potent pan-genotypic and antitumor activities. |
|
|
E1881New |
NVS-STG2
|
NVS-STG2(HY-157214) is a potent, allosteric small molecule agonist of STING. It binds at the transmembrane domain (TMD) interface of STING, thereby acting as a molecular glue to promote STING oligomerization and contribute to its activation. It may be used in research of STING-related autoimmune diseases. |
|
|
E2664 |
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). |
|
|
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. |
- EMBO J, 2024, 10.1038/s44318-024-00244-9
- EMBO Mol Med, 2024, 10.1038/s44321-024-00136-9
- CNS Neurosci Ther, 2024, 30(8):e14913
|
|
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. |
- Nature, 2024, 625(7995):585-592
- Cell, 2024, 187(15):4043-4060.e30
- Cell Rep Med, 2024, 5(7):101648
|
|
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. |
- Nat Commun, 2024, 15(1):1785
- Nat Commun, 2024, 15(1):1669
- Redox Biol, 2024, 69:103002
|
|
S6667 |
STING inhibitor C-178
|
C-178 is a covalent inhibitor of STING,covalently bind to Cys91. |
- Research Square, 2023, Version 2
- Cell Chem Biol, 2022, 29(10):1517-1531.e7
- Cancer Cell, 2021, 39-9:1214-1226.e10
|
|
E0128 |
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. |
- Cell Reports, 2023, 112328
- Cell Rep, 2023, 42(4):112328
|
|
E1787New |
SN-001
|
SN-001 is a potent inhibitor of STING that specifically inhibits STING activation and STING-dependent signaling. SN-011 significantly decreases inflammatory cytokine production and osteoclast formation in vivo. |
|
|
E0127 |
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. |
|
|
S1537 |
Vadimezan (DMXAA)
|
Vadimezan (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. |
- Mol Cancer, 2024, 23(1):186
- Nat Commun, 2024, 15(1):1750
- Cell Rep Med, 2024, 5(7):101648
|
|
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.Solutions are unstable and should be fresh-prepared. |
- Mol Cell, 2024, 84(20):3979-3996.e9
- Acta Pharm Sin B, 2024, 14(5):2194-2209
- EMBO J, 2024, 10.1038/s44318-024-00244-9
|
|
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. |
- Mol Neurobiol, 2022, 59(11):7006-7024
- J Inflamm Res, 2022, 15:5103-5119
- Signal Transduct Target Ther, 2021, 6(1):382
|
|
S8954 |
G10 (STING agonist-1)
|
G10 (STING agonist-1) 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. |
- Int J Biol Sci, 2023, 19(11):3428-3440
|
|
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
|
|
S9618 |
E7766 diammonium salt
|
E7766 diammonium salt, a macrocycle-bridged STING agonist with a Kd of 40 nM, shows potent pan-genotypic and antitumor activities. |
|
|
E1881New |
NVS-STG2
|
NVS-STG2(HY-157214) is a potent, allosteric small molecule agonist of STING. It binds at the transmembrane domain (TMD) interface of STING, thereby acting as a molecular glue to promote STING oligomerization and contribute to its activation. It may be used in research of STING-related autoimmune diseases. |
|
|
E2664 |
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). |
|
|