A2041New |
Emapalumab (anti-IFNγ)
|
Emapalumab (anti-IFNγ), a monoclonal antibody directed against IFNγ, is the first global approval for the treatment of pediatric and adult patients with primary hemophagocytic lymphohistiocytosis (HLH) with refractory. |
|
|
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. SAR-20347 inhibits TYK2- and JAK1-mediated IL-12 and IFN-α signaling. |
|
|
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). |
|
|
S3023 |
Bufexamac
|
Bufexamac is a COX inhibitor for IFN-α release with EC50 of 8.9 μM. |
-
Int J Mol Sci, 2021, 22(9)4559
-
Reprod Sci, 2021, 10.1007/s43032-021-00533-2
-
Autophagy, 2016, 12(10):1738-1758
|
|
S3544New |
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. |
-
Curr Protoc, 2022, 2(2):e372
|
|
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. |
|
|
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. Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65. Ginsenoside Rb1 reduces the expressions of TLR3, TLR4 and TRAF-6, and down-regulates the levels of TNF-α, IFN-β and iNOS. |
-
J Biol Chem, 2021, S0021-9258(21)00790-0
-
Mol Immunol, 2021, 139:140-152
-
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
|
|
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.Creatine can inhibits 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. |
-
Cancer Cell, 2021, S1535-6108(21)00445-1
-
Histochem Cell Biol, 2021, 156(3):227-237
|
|
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
|
|
S6727 |
AX-024 HCl
|
AX-024 HCl blocks the interaction of the CD3ε PRS with SH3.1(Nck). AX-024 HCl also inhibits IL-6, TNF-α, IFN-γ, IL-10 and IL-17A. |
|
|
S7259 |
FLLL32
|
FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM. FLLL32 inhibits the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells.
|
-
Syst Biol Reprod Med, 2022, 1-15
-
Int Immunopharmacol, 2021, 92:107304
-
Onco Targets Ther, 2021, 14:379-392
|
|
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. |
|
|
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
|
|
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
|
|
S2952 |
SM-276001
|
SM-276001 is a potent and selective agonist of TLR7 that induces antitumor immune responses. SM-276001 is an orally active interferon (IFN) inducer. |
|
|
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. |
|
|
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. |
|
|
S8133 |
Resiquimod (R-848)
|
Resiquimod (R-848, S28463) is an immune response modifier that acts as a potent TLR 7/TLR 8 agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α. Resiquimod reduces hepatitis C virus (HCV) infection. Phase 2. |
-
Small, 2022, 18(4):e2103552
-
Adv Mater, 2021, 33(51):e2104362
-
Pharmaceutics, 2021, 13(3)365
|
|
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. |
|
|
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. KIN1148 is an influenza vaccine adjuvant that enhances flu vaccine efficacy. |
|
|
A2041New |
Emapalumab (anti-IFNγ)
|
Emapalumab (anti-IFNγ), a monoclonal antibody directed against IFNγ, is the first global approval for the treatment of pediatric and adult patients with primary hemophagocytic lymphohistiocytosis (HLH) with refractory. |
|
|
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. SAR-20347 inhibits TYK2- and JAK1-mediated IL-12 and IFN-α signaling. |
|
|
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). |
|
|
S3023 |
Bufexamac
|
Bufexamac is a COX inhibitor for IFN-α release with EC50 of 8.9 μM. |
- Int J Mol Sci, 2021, 22(9)4559
- Reprod Sci, 2021, 10.1007/s43032-021-00533-2
- Autophagy, 2016, 12(10):1738-1758
|
|
S3544New |
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. |
- Curr Protoc, 2022, 2(2):e372
|
|
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. |
|
|
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. Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65. Ginsenoside Rb1 reduces the expressions of TLR3, TLR4 and TRAF-6, and down-regulates the levels of TNF-α, IFN-β and iNOS. |
- J Biol Chem, 2021, S0021-9258(21)00790-0
- Mol Immunol, 2021, 139:140-152
- J Ethnopharmacol, 2021, S0378-8741(21)00169-0
|
|
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.Creatine can inhibits 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. |
- Cancer Cell, 2021, S1535-6108(21)00445-1
- Histochem Cell Biol, 2021, 156(3):227-237
|
|
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
|
|
S6727 |
AX-024 HCl
|
AX-024 HCl blocks the interaction of the CD3ε PRS with SH3.1(Nck). AX-024 HCl also inhibits IL-6, TNF-α, IFN-γ, IL-10 and IL-17A. |
|
|
S7259 |
FLLL32
|
FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM. FLLL32 inhibits the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells.
|
- Syst Biol Reprod Med, 2022, 1-15
- Int Immunopharmacol, 2021, 92:107304
- Onco Targets Ther, 2021, 14:379-392
|
|
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. |
|
|
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
|
|
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
|
|
S2952 |
SM-276001
|
SM-276001 is a potent and selective agonist of TLR7 that induces antitumor immune responses. SM-276001 is an orally active interferon (IFN) inducer. |
|
|
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. |
|
|
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. |
|
|
S8133 |
Resiquimod (R-848)
|
Resiquimod (R-848, S28463) is an immune response modifier that acts as a potent TLR 7/TLR 8 agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α. Resiquimod reduces hepatitis C virus (HCV) infection. Phase 2. |
- Small, 2022, 18(4):e2103552
- Adv Mater, 2021, 33(51):e2104362
- Pharmaceutics, 2021, 13(3)365
|
|
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. |
|
|