| S1623 |
N-Acetylcysteine (NAC chemical, N-Acetyl-L-Cysteine)
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Acetylcysteine (N-acetyl-l-cysteine, NAC,N-acetylcysteine) is a ROS(reactive oxygen species) inhibitor that antagonizes the activity of proteasome inhibitors. It is also a tumor necrosis factor production inhibitor. Acetylcysteine(N-acetyl-l-cysteine) suppresses TNF-induced NF-κB activation through inhibition of IκB kinases. Acetylcysteine(N-acetyl-l-cysteine) induces apoptosis via the mitochondria-dependent pathway. Acetylcysteine(N-acetyl-l-cysteine) inhibits ferroptosis and virus replication.Solutions are unstable and should be fresh-prepared.
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Signal Transduct Target Ther, 2025, 10(1):341
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J Exp Med, 2025, 222(3)e20241248
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Adv Sci (Weinh), 2025, 12(36):e06150
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| S1029 |
CC-5013 (Lenalidomide)
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Lenalidomide is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis.
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Signal Transduct Target Ther, 2025, 10(1):29
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Nat Commun, 2025, 16(1):3800
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Cell Rep Med, 2025, S2666-3791(25)00102-8
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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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| S1537 |
Vadimezan (DMXAA)
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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.
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Cell Chem Biol, 2025, 32(2):280-290.e14
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Commun Biol, 2025, 8(1):1470
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Front Pharmacol, 2025, 16:1528459
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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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| S1567 |
Pomalidomide (CC-4047)
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Pomalidomide inhibits LPS-induced TNF-α release with IC50 of 13 nM in PBMCs. Pomalidomide can be utilized in PROTAC as a ligand for targeting E3 ligase and inhibiting the E3 ligase protein cereblon (CRBN). Pomalidomide promotes apoptosis and cell cycle arrest.
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Nat Commun, 2025, 16(1):6631
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Cell Rep Med, 2025, S2666-3791(25)00102-8
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J Med Virol, 2025, 97(8):e70537
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| S8037 |
Necrostatin-1 (Nec-1)
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Necrostatin-1 (Nec-1) is a specific RIP1 (RIPK1) inhibitor and inhibits TNF-α-induced necroptosis with EC50 of 490 nM in 293T cells. Necrostatin-1 also blocks IDO and suppresses autophagy and apoptosis.
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Cell Res, 2025, 10.1038/s41422-025-01167-8
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Signal Transduct Target Ther, 2025, 10(1):341
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Cancer Discov, 2025, 10.1158/2159-8290.CD-24-1317
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| S4238 |
Cepharanthine
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Cepharanthine (NSC-623442) is a biscoclaurine alkaloid inhibiting tumor necrosis factor (TNF)-α-mediated NFκB stimulation, plasma membrane lipid peroxidation and platelet aggregation and suppressing cytokine production.
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Emerg Microbes Infect, 2024, 13(1):2429624
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SLAS Discov, 2024, S2472-5552(24)00007-8
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Cell Death Dis, 2022, 13(11):1000
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| S6643 |
R-7050
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R-7050 is a cell permeable TNF-α receptor antagonist and is 2.3-fold more selective for TNF-α-mediated signaling than for that driven by IL-1β.
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Int Immunopharmacol, 2024, 143(Pt 2):113521
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Ren Fail, 2023, 45(1):2220418
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Elife, 2022, 11e73792
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| S0787 |
3-Deazaadenosine hydrochloride
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3-Deazaadenosine HCl (3-DZA, c3Ado) is a potent inhibitor of S-adenosylhomocysteine hydrolase with Ki of 3.9 µM. 3-Deazaadenosine HCl inhibits bacterial lipopolysaccharide-induced transcription of TNF-α and IL-1β. 3-Deazaadenosine HCl inhibits the transcriptional activity of NF-κB, prevents FCS-induced Ras carboxyl methylation and reduces FCS-induced ERK1/2 and Akt phosphorylation. 3-Deazaadenosine HCl has anti-inflammatory, anti-proliferative and anti-HIV activities.
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Virus Res, 2025, 358:199590
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J Exp Clin Cancer Res, 2022, 41(1):36
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Free Radic Biol Med, 2021, 168:25-43
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