STING

STING製品

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  • STING阻害剤 (7)
  • STING活性剤(2)
  • STING拮抗剤(2)
  • STING作動薬(8)
  • 新製品
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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
J Adv Res, 2024, S2090-1232(24)00499-5
Cancer Lett, 2024, 586:216695
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.
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.
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
J Adv Res, 2024, S2090-1232(24)00499-5
Cancer Lett, 2024, 586:216695
E1066 SN-011 SN-011 is a STING-specific antagonist with IC50 of 76 nM.
Mol Cancer, 2024, 23(1):186
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).
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.
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.
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.

STING阻害剤の選択性比較

Tags: STING antagonist | STING inhibitor | STING agonist