| S8879 |
BMS-986165 (Deucravacitinib)
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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.
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Res Sq, 2025, rs.3.rs-6079043
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Nat Commun, 2024, 15(1):1718
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Nat Commun, 2024, 15(1):1337
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| S8133 |
Resiquimod (R-848)
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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.
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Nature, 2025, 644(8078):1058-1068
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J Virol, 2025, e0128025.
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Int J Nanomedicine, 2024, 19:3589-3605
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| S1189 |
Aprepitant
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Aprepitant is a potent and selective neurokinin-1 receptor antagonist with IC50 of 0.1 nM. This compound reduces levels of pro-inflammatory cytokines including G-CSF, IL-6, IL-8 and TNFα. It inhibits HIV infection of human macrophages.
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Br J Cancer, 2024, 10.1038/s41416-024-02608-8
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Inflammation, 2023, 46(1):256-269
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Nat Commun, 2022, 13(1):4995
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| S1709 |
17β-Estradiol
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Estradiol (17β-estradiol, β-Estradiol, E2, 17β-Oestradiol) is a human sex hormone and steroid, and the primary female sex hormone. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.
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Cancer Cell, 2025, 43(5):891-904.e10
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Nat Commun, 2025, 16(1):758
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Cell Rep Med, 2025, 6(7):102192
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| S7124 |
SC144
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SC144 is the first-in-class orally active small-molecule gp130 inhibitor that induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes.
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Cell Rep Med, 2025, S2666-3791(25)00102-8
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Respir Res, 2025, 26(1):285
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bioRxiv, 2025, 2025.01.20.633954
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| S8301 |
Ossirene (AS101)
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A potent in vitro and in vivo immunomodulator, Ossirene (AS101) is a novel inhibitor of IL-1beta converting enzyme.
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Mol Neurodegener, 2025, 20(1):5
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Cell Biosci, 2025, 15(1):18
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Stem Cell Rev Rep, 2025, none
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| S4267 |
Diacerein
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Diacerein is an inhibitor of pro-inflammatory cytokine Interleukin-1B (IL-1B) production, prescribed for osteoarthritis and chronic inflammatory arthritis.
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MedComm (2020), 2024, 5(8):e668
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Oral Dis, 2022, 10.1111/odi.14294
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Free Radic Biol Med, 2021, 165:171-183
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| S9727 |
Ac-YVAD-cmk
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Ac-YVAD-cmk (Caspase-1 Inhibitor II) is a selective IL-1β converting enzyme (ICE) inhibitor with neuroprotective and anti-inflammatory effects, effectively suppresses the expression of IL-1β and IL-18.
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Cell Commun Signal, 2024, 22(1):368
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J Transl Med, 2024, 22(1):1139
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Int J Mol Sci, 2024, 25(4)2185
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| S0785 |
Apilimod mesylate
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Apilimod mesylate is a potent and orally-available inhibitor of the cytokines interleukin-12 (IL-12) and interleukin-23 (IL-23) with the potential to treat certain autoimmune and inflammatory diseases. This compound inhibits IL-12 with IC50 of 1 nM, 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs, human monocytes and mouse PBMCs, respectively. It is also a cell permeable small molecule that specifically inhibits PIKfyve with IC50 of 14 nM.
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bioRxiv, 2024, 2024.02.28.582543
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Stem Cell Reports, 2022, 17(2):397-412
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Hum Mol Genet, 2021, 29(22):3589-3605
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| S0472 |
EC330
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EC330 is a steroidal inhibitor of leukemia inhibitory factor (LIF, an interleukin 6 class cytokine). This compound inhibits the LIF/LIF-R signaling and blocks the promoting effects of LIF on growth and migration of cancer cells.
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NPJ Precis Oncol, 2024, 8(1):246
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Br J Cancer, 2021, 10.1038/s41416-021-01631-3
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