| 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. It is also a STING agonist with potential antineoplastic activity, potently inducing IFN-β but relatively low TNF-α expression in vitro. This compound has antiviral activity. Phase 3.
|
-
Cell Chem Biol, 2025, 32(2):280-290.e14
-
Commun Biol, 2025, 8(1):1470
-
Front Pharmacol, 2025, 16:1528459
|
|
| 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. This compound, the protonophore, can inhibits STING-mediated IFN-β production via disrupting mitochondrial membrane potential (MMP).
|
-
Mol Cell, 2025, 85(7):1467-1476.e6
-
Life Sci, 2025, 380:123965
-
iScience, 2025, 28(8):112972
|
|
| S8133 |
Resiquimod (R-848)
|
Resiquimod (R-848, S28463) is an immune response modifier that acts as a potent TLR 7/TLR 8 agonist, inducing the upregulation of cytokines such as TNF-α, IL-6 and IFN-α. This compound reduces hepatitis C virus (HCV) infection. Phase 2.
|
-
Nature, 2025, 644(8078):1058-1068
-
J Virol, 2025, e0128025.
-
Int J Nanomedicine, 2024, 19:3589-3605
|
|
| S7259 |
FLLL32
|
FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM. This compound inhibits the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells.
|
-
Stem Cell Reports, 2025, 20(10):102673
-
Cancer Commun -Lond), 2023, 43(10):1117-1142
-
Microbiol Res, 2023, 276:127480
|
|
| S3544 |
VBIT-4
|
VBIT-4 is a voltage-dependent anion channel (VDAC) oligomerization inhibitor that decreases mitochondrial DNA (mtDNA) release, type I interferon (IFN) signaling, neutrophil extracellular traps, and disease severity in a mouse model of systemic lupus erythematosus.
|
-
Cell Rep, 2025, 44(5):115605
-
Cell Rep, 2025, 44(6):115834
-
Aging Cell, 2025, e70135
|
|
| S3023 |
Bufexamac
|
Bufexamac (Bufexamic acid) is a COX inhibitor for IFN-α release with EC50 of 8.9 μM.
|
-
Biomedicines, 2024, 12(6)1203
-
Int J Mol Sci, 2021, 22(9)4559
-
Reprod Sci, 2021, 10.1007/s43032-021-00533-2
|
|
| S5588 |
Creatine
|
Creatine (Methylguanidoacetic acid) is a nitrogenous organic acid that occurs naturally in vertebrates. It facilitates the recycling of adenosine triphosphate (ATP) primarily in muscle and brain tissue. This compound can inhibit the JAK-STAT1 signal transmission by inhibiting the interaction of IFN-γ receptors with JAK2 in an ATP-independent manner, thereby inhibiting downstream pro-inflammatory gene expression.
|
-
Aging (Albany NY), 2022, 14(16):6796-6808
-
Cancer Cell, 2021, S1535-6108(21)00445-1
-
Histochem Cell Biol, 2021, 156(3):227-237
|
|
| S3924 |
Ginsenoside Rb1
|
Ginsenoside Rb1 (Gypenoside Ⅲ) is a protopanaxadiol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-obesity actions. This compound, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with IC50 of 6.3±1.0 μM. It also inhibits IRAK-1 activation and phosphorylation of NF-κB p65. This chemical reduces the expressions of TLR3, TLR4 and TRAF-6, and down-regulates the levels of TNF-α, IFN-β and iNOS.
|
-
J Biol Chem, 2024, 300(8):107542
-
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
-
J Biol Chem, 2021, S0021-9258(21)00790-0
|
|
| S2259 |
Aloe-emodin
|
Aloe-emodin (NSC 38628, Rhabarberone) is an interferon-inducing agent with IC50 of about 1 μg/mL for JEV and of about 0.33 μg/mL for EV71.
|
-
PLoS One, 2019, 14(4):e0215664
-
J Tradit Complement Med, 2015, 5(2):96-9
|
|
| S8879 |
Deucravacitinib (BMS-986165)
|
Deucravacitinib (BMS-986165) is a highly potent and selective allosteric inhibitor of Tyk2 with a Ki value of 0.02 nM for binding to the Tyk2 pseudokinase domain. It is highly selective against a panel of 265 kinases and pseudokinases.
|
-
Res Sq, 2025, rs.3.rs-6079043
-
Nat Commun, 2024, 15(1):1718
-
Nat Commun, 2024, 15(1):1337
|
|
| S0289 |
KIN1148
|
KIN1148 is an agonist of interferon regulatory factor 3 (IRF3) that induces dose-dependent IRF3 nuclear translocation and specific activation of IRF3-responsive promoters. This compound is an influenza vaccine adjuvant that enhances flu vaccine efficacy.
|
-
J Allergy Clin Immunol, 2022, S0091-6749(22)01423-3
|
|
| 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. This compound 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
|
|
| S0437 |
SAR-20347
|
SAR-20347 is a potent inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50 of 0.6 nM, 23 nM, 26 nM and 41 nM, respectively. This compound inhibits TYK2- and JAK1-mediated IL-12 and IFN-α signaling.
|
-
Cancer Discov, 2023, 13(2):410-431
-
Cancer Discov, 2023, 13(2):410-431
|
|
| S1833 |
Butoconazole nitrate
|
Butoconazole nitrate (RS-35887) is an anti-fungal agent that inhibits PHA-stimulated release of cytokines-- IL-2, TNFα, IFN and GM-CSF from human peripheral blood lymphocytes (IC50 of 7.2 μg/mL, 14.4 μg/mL, 7.36 μg/mL and 7.6 μg/mL, respectively).
|
|
|
| E2982 |
IFN alpha-IFNAR-IN-1 hydrochloride
|
IFN alpha-IFNAR-IN-1 hydrochloride is a nonpeptidic, low-molecular-weight inhibitor that inhibits the interaction between IFN-α and IFNAR. This compound inhibits modified Vaccinia virus ankara (MVA)-induced IFN-α responses in murine bone-marrow-derived, Flt3- L-differentiated pDC cultures (BM-pDCs) with IC50 value of 2-8 μM.
|
|
|
| S3827 |
Royal jelly acid
|
Royal jelly acid (10-Hydroxy-trans-2-decenoic acid, 10H2DA) is the principal lipid component in royal jelly which is the food for queen and larvae honeybees. It is involved in several treatment processes of autoimmune and inflammatory diseases, including inhibition of lipopolysaccharide (LPS)- and interferon (IFN)-γ-stimulated macrophage responses, inhibition of T-cell proliferation and anti-rheumatoid activity.
|
|
|
| S5020 |
Tilorone dihydrochloride
|
Tilorone dihydrochloride is a broad-spectrum, orally active antiviral agent that activates interferon production. It has antitumor, anti-inflammatory properties.
|
|
|
| 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.
|
-
Cancer Sci, 2025, 10.1111/cas.70162
-
J Biol Chem, 2025, 301(10):110653
-
Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0
|
|
| 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.
|
|
|
| E5781 |
2',3'-cGAMP
|
2',3'-cGAMP (2'-3'-cyclic GMP-AMP) is an endogenous cyclic GMP-AMP produced in mammalian cells in response to cytoplasmic DNA. It binds STING with high affinity Kd of 3.79 nM and is a potent inducer of interferon-β (IFNβ).
|
-
Commun Biol, 2025, 8(1):1470
|
|
| E0448 |
RO8191
|
RO8191 (CDM-3008, RO4948191), an imidazonaphthyridine compound, is an orally active and potent agonist of interferon (IFN) receptor. This compound binds directly to the IFNα/β receptor 2 (IFNAR2), activating IFN-stimulated genes (ISGs) expression and the phosphorylation of JAK/STAT signaling.
|
|
|
| S6727 |
AX-024 HCl
|
AX-024 HCl blocks the interaction of the CD3ε PRS with SH3.1(Nck). This compound also inhibits IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
|
-
Cell Rep Med, 2025, S2666-3791(25)00231-9
|
|
| 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. This compound, the protonophore, can inhibits STING-mediated IFN-β production via disrupting mitochondrial membrane potential (MMP). |
- Mol Cell, 2025, 85(7):1467-1476.e6
- Life Sci, 2025, 380:123965
- iScience, 2025, 28(8):112972
|
|
| S7259 |
FLLL32
|
FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM. This compound inhibits the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells. |
- Stem Cell Reports, 2025, 20(10):102673
- Cancer Commun -Lond), 2023, 43(10):1117-1142
- Microbiol Res, 2023, 276:127480
|
|
| S3544 |
VBIT-4
|
VBIT-4 is a voltage-dependent anion channel (VDAC) oligomerization inhibitor that decreases mitochondrial DNA (mtDNA) release, type I interferon (IFN) signaling, neutrophil extracellular traps, and disease severity in a mouse model of systemic lupus erythematosus. |
- Cell Rep, 2025, 44(5):115605
- Cell Rep, 2025, 44(6):115834
- Aging Cell, 2025, e70135
|
|
| S3023 |
Bufexamac
|
Bufexamac (Bufexamic acid) is a COX inhibitor for IFN-α release with EC50 of 8.9 μM. |
- Biomedicines, 2024, 12(6)1203
- Int J Mol Sci, 2021, 22(9)4559
- Reprod Sci, 2021, 10.1007/s43032-021-00533-2
|
|
| S5588 |
Creatine
|
Creatine (Methylguanidoacetic acid) is a nitrogenous organic acid that occurs naturally in vertebrates. It facilitates the recycling of adenosine triphosphate (ATP) primarily in muscle and brain tissue. This compound can inhibit the JAK-STAT1 signal transmission by inhibiting the interaction of IFN-γ receptors with JAK2 in an ATP-independent manner, thereby inhibiting downstream pro-inflammatory gene expression. |
- Aging (Albany NY), 2022, 14(16):6796-6808
- Cancer Cell, 2021, S1535-6108(21)00445-1
- Histochem Cell Biol, 2021, 156(3):227-237
|
|
| S3924 |
Ginsenoside Rb1
|
Ginsenoside Rb1 (Gypenoside Ⅲ) is a protopanaxadiol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-obesity actions. This compound, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with IC50 of 6.3±1.0 μM. It also inhibits IRAK-1 activation and phosphorylation of NF-κB p65. This chemical reduces the expressions of TLR3, TLR4 and TRAF-6, and down-regulates the levels of TNF-α, IFN-β and iNOS. |
- J Biol Chem, 2024, 300(8):107542
- J Ethnopharmacol, 2021, S0378-8741(21)00169-0
- J Biol Chem, 2021, S0021-9258(21)00790-0
|
|
| S8879 |
Deucravacitinib (BMS-986165)
|
Deucravacitinib (BMS-986165) is a highly potent and selective allosteric inhibitor of Tyk2 with a Ki value of 0.02 nM for binding to the Tyk2 pseudokinase domain. It is highly selective against a panel of 265 kinases and pseudokinases. |
- Res Sq, 2025, rs.3.rs-6079043
- Nat Commun, 2024, 15(1):1718
- Nat Commun, 2024, 15(1):1337
|
|
| S0437 |
SAR-20347
|
SAR-20347 is a potent inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50 of 0.6 nM, 23 nM, 26 nM and 41 nM, respectively. This compound inhibits TYK2- and JAK1-mediated IL-12 and IFN-α signaling. |
- Cancer Discov, 2023, 13(2):410-431
- Cancer Discov, 2023, 13(2):410-431
|
|
| S1833 |
Butoconazole nitrate
|
Butoconazole nitrate (RS-35887) is an anti-fungal agent that inhibits PHA-stimulated release of cytokines-- IL-2, TNFα, IFN and GM-CSF from human peripheral blood lymphocytes (IC50 of 7.2 μg/mL, 14.4 μg/mL, 7.36 μg/mL and 7.6 μg/mL, respectively). |
|
|
| E2982 |
IFN alpha-IFNAR-IN-1 hydrochloride
|
IFN alpha-IFNAR-IN-1 hydrochloride is a nonpeptidic, low-molecular-weight inhibitor that inhibits the interaction between IFN-α and IFNAR. This compound inhibits modified Vaccinia virus ankara (MVA)-induced IFN-α responses in murine bone-marrow-derived, Flt3- L-differentiated pDC cultures (BM-pDCs) with IC50 value of 2-8 μM. |
|
|
| S3827 |
Royal jelly acid
|
Royal jelly acid (10-Hydroxy-trans-2-decenoic acid, 10H2DA) is the principal lipid component in royal jelly which is the food for queen and larvae honeybees. It is involved in several treatment processes of autoimmune and inflammatory diseases, including inhibition of lipopolysaccharide (LPS)- and interferon (IFN)-γ-stimulated macrophage responses, inhibition of T-cell proliferation and anti-rheumatoid activity. |
|
|
| S6727 |
AX-024 HCl
|
AX-024 HCl blocks the interaction of the CD3ε PRS with SH3.1(Nck). This compound also inhibits IL-6, TNF-α, IFN-γ, IL-10 and IL-17A. |
- Cell Rep Med, 2025, S2666-3791(25)00231-9
|
|
| 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. It is also a STING agonist with potential antineoplastic activity, potently inducing IFN-β but relatively low TNF-α expression in vitro. This compound has antiviral activity. Phase 3. |
- Cell Chem Biol, 2025, 32(2):280-290.e14
- Commun Biol, 2025, 8(1):1470
- Front Pharmacol, 2025, 16:1528459
|
|
| S8133 |
Resiquimod (R-848)
|
Resiquimod (R-848, S28463) is an immune response modifier that acts as a potent TLR 7/TLR 8 agonist, inducing the upregulation of cytokines such as TNF-α, IL-6 and IFN-α. This compound reduces hepatitis C virus (HCV) infection. Phase 2. |
- Nature, 2025, 644(8078):1058-1068
- J Virol, 2025, e0128025.
- Int J Nanomedicine, 2024, 19:3589-3605
|
|
| S2259 |
Aloe-emodin
|
Aloe-emodin (NSC 38628, Rhabarberone) is an interferon-inducing agent with IC50 of about 1 μg/mL for JEV and of about 0.33 μg/mL for EV71. |
- PLoS One, 2019, 14(4):e0215664
- J Tradit Complement Med, 2015, 5(2):96-9
|
|
| 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. This compound 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
|
|
| S5020 |
Tilorone dihydrochloride
|
Tilorone dihydrochloride is a broad-spectrum, orally active antiviral agent that activates interferon production. It has antitumor, anti-inflammatory properties. |
|
|
| 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. |
|
|