Interleukins

Interleukins製品

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S7455 Resatorvid (TAK-242) Resatorvid (TAK-242, CLI-095) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α and IL-6 in macrophages with IC50 of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy.
EMBO J, 2025, 10.1038/s44318-025-00515-z
Carbohydr Polym, 2025, 350:122980
J Neuroinflammation, 2025, 22(1):38
S1189 Aprepitant Aprepitant is a potent and selective neurokinin-1 receptor antagonist with IC50 of 0.1 nM. Aprepitant reduces levels of pro-inflammatory cytokines including G-CSF, IL-6, IL-8 and TNFα. Aprepitant inhibits HIV infection of human macrophages.
Br J Cancer, 2024, 10.1038/s41416-024-02608-8
Inflammation, 2023, 46(1):256-269
Nat Commun, 2022, 13(1):4995
Aprepitant-S118901W0220161031.gif
S1709 17β-Estradiol 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.
Cancer Cell, 2025, 43(5):891-904.e10
Nat Commun, 2025, 16(1):758
Cell Rep Med, 2025, 6(7):102192
S8966 T-5224 T-5224 is a selective inhibitor of transcription factor c-Fos/activator protein (AP)-1 with anti-inflammatory effects. T-5224 specifically inhibits the DNA binding activity of c-Fos/c-Jun and the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription.
MedComm (2020), 2025, 6(4):e70154
MedComm (2020), 2025, 6(4):e70154
Cells, 2025, 14(7)474
S7124 SC144 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.
Cell Rep Med, 2025, S2666-3791(25)00102-8
Respir Res, 2025, 26(1):285
bioRxiv, 2025, 2025.01.20.633954
SC144-S712401Y0220161118.gif
S6414 Apilimod (STA-5326) Apilimod 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. Apilimod (STA-5326) 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. Apilimod (STA-5326) is also a cell permeable small molecule that specifically inhibits PIKfyve with IC50 of 14 nM.
Nat Commun, 2025, 16(1):8123
Nat Commun, 2025, 16(1):6397
J Cell Biol, 2025, 224(6)e202408158
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.
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. FLLL32 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
FLLL32-S725901Z0520161121.gif
S8301 Ossirene (AS101) Ossirene (AS101), a potent in vitro and in vivo immunomodulator, is a novel inhibitor of IL-1beta converting enzyme.
Mol Neurodegener, 2025, 20(1):5
Cell Biosci, 2025, 15(1):18
Stem Cell Rev Rep, 2025, none
S9668 PKR-IN-C16 PKR-IN-C16 (C16, Imidazolo-oxindole PKR inhibitor C16) is a specific inhibitor of RNA-dependent protein kinase (PKR, Protein Kinase R, EIF2AK2). PKR-IN-C16 prevents apoptosis and IL-1β production in an acute excitotoxic rat model with a neuroinflammatory component.
Immunity, 2025, 58(10):2489-2504.e8
Exp Mol Med, 2024, 56(2):408-421.
EMBO J, 2024, 43(5):780-805.
S8879 BMS-986165 (Deucravacitinib) 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
S4267 Diacerein Diacerein is an inhibitor of pro-inflammatory cytokine Interleukin-1B (IL-1B) production, prescribed for osteoarthritis and chronic inflammatory arthritis.
MedComm (2020), 2024, 5(8):e668
Oral Dis, 2022, 10.1111/odi.14294
Free Radic Biol Med, 2021, 165:171-183
Diacerein-S426701Z0720161110.gif
S6898 RCM-1 RCM-1 is a nontoxic inhibitor of Forkhead box M1 (FOXM1) that suppresses goblet cell metaplasia and prevents IL-13 and STAT6 signaling in allergen-exposed mice. RCM-1 decreases carcinogenesis and nuclear β-catenin.
Gut, 2025, gutjnl-2025-335163
Parasit Vectors, 2025, 18(1):100
bioRxiv, 2025, 2025.05.25.655133
S9727 Ac-YVAD-cmk 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.
Cell Commun Signal, 2024, 22(1):368
J Transl Med, 2024, 22(1):1139
Int J Mol Sci, 2024, 25(4)2185
S1733 Methylprednisolone Methylprednisolone (NSC-19987,U 7532) is a synthetic glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation. Methylprednisolone activates ACE2 and reduces IL-6 levels, thus improves severe or critical COVID-19. Methylprednisolone markedly reduces autophagy and apoptosis.
Food Chem Toxicol, 2024, 188:114665
Drug Test Anal, 2020, 10.1002/dta.2917
Nat Med, 2017, 23(4):424-428
Methylprednisolone-S173301X0220161108.gif
S3871 Muscone Muscone (3-Methylcyclopentadecanone, Methylexaltone), a flavouring ingredient, is an organic compound that is the primary contributor to the odor of musk and also a potent anti-inflammatory agent. Muscone significantly downregulats the levels of LPS-induced inflammatory cytokines and inhibits NF-κB and NLRP3 inflammasome activation in BMDMs. Muscone remarkably decreases the levels of inflammatory cytokines (IL-1β, TNF-α and IL-6).
Ecotoxicol Environ Saf, 2025, 292:117961
Invest Ophthalmol Vis Sci, 2025, 66(5):21
Toxicol Appl Pharmacol, 2025, 503:117494
S8261 GSK583 GSK583 is a highly potent and selective inhibitor of RIP2 kinase with IC50 of 5 nM. GSK583 also inhibits both TNF-α and IL-6 production with IC50 of ~200 nM in explant cultures.
J Invest Dermatol, 2025, S0022-202X(25)00494-4
Cancer Res, 2020, canres.530.2020
J Neuroinflammation, 2020, 17(1):364
S0785 Apilimod mesylate 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. Apilimod mesylate (STA-5326 mesylate) 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. Apilimod mesylate (STA-5326 mesylate) is also a cell permeable small molecule that specifically inhibits PIKfyve with IC50 of 14 nM.
bioRxiv, 2024, 2024.02.28.582543
Stem Cell Reports, 2022, 17(2):397-412
Hum Mol Genet, 2021, 29(22):3589-3605
S0787 3-Deazaadenosine hydrochloride 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.
Virus Res, 2025, 358:199590
J Exp Clin Cancer Res, 2022, 41(1):36
Free Radic Biol Med, 2021, 168:25-43
S3292 (3R,8S)-Falcarindiol Falcarindiol (FAD, (3R,8S)-Falcarindiol, FaDOH) is a natural polyacetylene compound found rich in many plants of the Umbelliferae family. Falcarindiol suppresses LPS-stimulated expression of inducible nitric oxide synthase (iNOS), tumor necrosis factor alpha (TNFα), interleukin-6 (IL-6), and interleukin-1 beta (IL-1β). Falcarindiol attenuates the LPS-induced activation of JNK, ERK, STAT1, and STAT3 signaling molecules.
Antioxidants (Basel), 2024, 13(12)1533
Front Cell Infect Microbiol, 2023, 13:1128000
Front Pharmacol, 2021, 12:656697
S2979 CU-T12-9 CU-T12-9 is a specific agonist of Toll-like receptor (TLR) 1/2 with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.
Nat Commun, 2025, 16(1):2743
Biomedicine & Pharmacotherapy, 2023, 114638
Biomed Pharmacother, 2023, 162:114638
S0826 A-740003 A-740003 is a potent, selective and competitive antagonist of P2X7 receptor with IC50 of 18 nM and 40 nM for rat and human P2X7 receptors, respectively. A-740003 potently blocks agonist-evoked IL-1β release and pore formation with IC50 of 156 nM and 92 nM in differentiated human THP-1 cells.
Am J Cancer Res, 2024, 14(2):585-600
Cell Rep, 2023, 42(7):112696
S9052 Auraptene Auraptene (7-geranyloxycoumarin) is a natural coumarin derived from citrus plants and possesses valuable pharmacological properties, including anticarcinogenic, anti-inflammatory, antihelicobacter, antigenotoxic, and neuroprotective effects. Auraptene inhibits matrix metalloproteinase 2 (MMP-2) as well as key inflammatory mediators, including IL-6, IL-8 and chemokine (C-C motif) ligand-5(CCL5).
Neuropharmacology, 2025, 269:110352
Plant Physiology, 2012, 81–94
S6620 Danirixin (GSK1325756) Danirixin (GSK1325756) is a small molecule, non-peptide, high affinity (IC50 for CXCL8 (IL-8) binding = 12.5 nM), selective, and reversible CXCR2 antagonist.
Redox Biol, 2024, 76:103323
Theranostics, 2019, 9(18):5332-5346
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.
Cancer Discov, 2023, 13(2):410-431
Cancer Discov, 2023, 13(2):410-431
S0472 EC330 EC330 is a steroidal inhibitor of leukemia inhibitory factor (LIF, an interleukin 6 class cytokine). EC330 inhibits the LIF/LIF-R signaling and blocks the promoting effects of LIF on growth and migration of cancer cells.
NPJ Precis Oncol, 2024, 8(1):246
Br J Cancer, 2021, 10.1038/s41416-021-01631-3
S2015 Suplatast Tosylate Suplatast Tosylate (IPD-1151T, Suplatast Tosilate) is a novel capsular anti-asthmatic agent that suppresses both IgE production, IL-4 and IL-5 synthesis with IC50 above 100 μM.
J Transl Med, 2022, 20(1):615
S6281 Sodium Thiocyanate Sodium Thiocyanate (NaSCN, Sodium rhodanide, Sodium sulfocyanate, Sodium rhodanate), one of the main sources of the thiocyanate anion, is used as a precursor for the synthesis of pharmaceuticals and other specialty chemicals. Sodium thiocyanate (NaSCN) reduces IL-6, whereas increases IL-10 levels. Sodium thiocyanate also reduces ROS.
Evid Based Complement Alternat Med, 2022, 2022:8315503
S0771 BRD6989 BRD6989 is a selective inhibitor of CDK8 and CDK19. BRD6989 upregulates IL-10. BRD6989 is an analog of the natural product cortistatin A (dCA).
Infect Drug Resist, 2021, 14:3135-3143
S0781 IQ 3 IQ 3 is a specific c-Jun N-terminal kinase (JNK) inhibitor with Kd of 66 nM, 240 nM and 290 nM for JNK3, JNK1 and JNK2, respectively. IQ 3 inhibits LPS-induced NF-κB/AP1 transcriptional activity in THP1-Blue cells with IC50 of 1.4 μM. IQ 3 also inhibits TNF-α and IL-6 production in vitro.
Int J Biol Sci, 2024, 20(6):2323-2338
S0094 SR 0987 SR 0987, a SR 1078 analog, is an agonist for T cell-specific RORγ (RORγt) with EC50 of 800 nM. SR 0987 represses PD-1, produces IL17 and is potential for the treatment of cancer.
Evid Based Complement Alternat Med, 2022, 2022:8315503.
P1235 Raleukin Anakinra (Raleukin, AMG-719) is an exogenous antagonist of recombinant human interleukin-1 receptor that also inhibits caspase-1 and caspase-9 activity with Ki of 0.201 μM and 0.31 μM respectively. It is used in research to study IL-1 blockade in inflammation, tumor growth, islet transplantation, and cardiac injury models.
Inflammation, 2025, 10.1007/s10753-025-02315-3
S5972 Hydrocortisone hemisuccinate Hydrocortisone hemisuccinate (A-hydrocort, Hydrocortisone 21-hemisuccinate), a physiological glucocorticoid with anti-inflammatory properties, is an inhibitor of proinflammatory cytokine with IC50 of 6.7 μM and 21.4 μM for Interleukin-6 (IL-6) and IL-3, respectively.
J Transl Med, 2023, 21(1):50
S9374 2',5'-Dihydroxyacetophenone 2',5'-Dihydroxyacetophenone (DHAP, 2-Acetylhydroquinone, Quinacetophenone) is a mixture of dihydroxyacetophenone isomers is used in food flavouring. 2',5'-Dihydroxyacetophenone significantly inhibits NO production via the suppression of iNOS expression. 2',5'-Dihydroxyacetophenone significantly decreases levels of the pro-inflammatory cytokines TNF-α and IL-6 by blocking the ERK1/2 and NF-κB signaling pathways.
Pathol Oncol Res, 2019, 25(1):301-309
S6850 NE 52-QQ57 NE 52-QQ57 is a selective, and orally available antagonist of G-protein coupled receptor 4 (GPR4) with IC50 of 0.07 μM. NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation with IC50 of 26.8 nM in HEK293 cells. The antagonism of GPR4 with NE 52-QQ57 significantly inhibits the AGE-induced increased expression of several key inflammatory cytokines and signaling molecules, including tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6, inducible nitric oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX2), and prostaglandin E2 (PGE2).
Exp Hematol Oncol, 2024, 13(1):13
S9417 Homoplantaginin Homoplantaginin (Hispidulin-7-glucoside), a main flavonoid from a traditional Chinese medicine Salvia plebeia, has anti-inflammatory and anti-oxidant properties. Homoplantaginin inhibits TNF-α and IL-6 mRNA expression, IKKβ and NF-κB phosphorylation.
Front Pharmacol, 2025, 16:1526107
S3745 Balsalazide disodium Balsalazide Disodium is the disodium salt form of balsalazide, an aminosalicylate and oral prodrug that is enzymatically cleaved in the colon to produce the anti-inflammatory agent mesalazine. Balsalazide Disodium suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway.
Front Microbiol, 2020, 10:2936
S9502 Madecassic acid Madecassic acid (Brahmic acid), a natural triterpene first isolated from C. asiatica, has diverse anti-inflammatory and anti-diabetic effects, blocking NF-κB activation in macrophages and causing by iNOS, COX-2, TNF-alpha, IL-1beta and IL-6 inhibition.
Drug Des Devel Ther, 2022, 16:3793-3804
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.
Cell Rep Med, 2025, S2666-3791(25)00231-9
S3261 Myrislignan Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan inhibits interleukin-6 (IL-6) and tumour necrosis factor-α (TNF-α). Myrislignan significantly inhibits the expressions of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2) dose-dependently in LPS-stimulated macrophage cells. Myrislignan inhibits the NF-κB signalling pathway activation.
Oxid Med Cell Longev, 2023, 2023:7098313
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).
S3312 Diethyl phosphate

Diethyl phosphate (DEP, DPF, Diethyl phosphoric acid, diethyl hydrogen phosphate), a non-specific metabolite of organophosphorus pesticides in the gut environment, significantly enriches opportunistic pathogens leading to a decrease in interleukin-6 (IL-6).

S5764 YM 90709 YM 90709 is a novel IL-5 inhibitor which selectively blocks the binding of IL-5 to the IL-5 receptor (IL-5R).
S4842 Balsalazide Balsalazide (Colazal, Giazo), an aminosalicylate and oral prodrug, is enzymatically cleaved in the colon to produce the anti-inflammatory agent mesalazine. Balsalazide suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway.
P1252New JNJ-77242113(Icotrokinra) Icotrokinra (JNJ-77242113, JNJ-2113, PN-235) is an orally available and selective antagonist of the IL-23 receptor. It also inhibits IL-23–induced STAT3 phosphorylation in peripheral blood mononuclear cells with an IC50 of 5.6 pM and suppresses IL-23–induced IFN-γ production in NK cells with an IC50 of 18.4 pM. It also exhibits anti-inflammatory activity in a TNBS-induced colitis model in rats and holds potential for studying psoriasis, psoriatic arthritis, and inflammatory bowel disease.
S3590 Triolein Triolein is an inhibitor of metalloproteinase-1 (MMP-1) and reduces both the expression of IL-6 and ROS generation in irradiated keratinocytes.
E0314 JTE-607 Dihydrochloride

JTE-607 Dihydrochloride is a prodrug compound that is converted to an active form by ester hydrolysis. JTE-607 is a multiple cytokine production inhibitor that targets CPSF3 and inhibits pre-mRNA processing. JTE-607 inhibits tumor necrosis factor (TNF)-alpha, interleukin (IL)-1beta, IL-6, IL-8 and IL-10, from LPS-stimulated human PBMCs, with IC50 values of 11 nM, 5.9 nM, 8.8 nM, 7.3 nM and 9.1 nM, respectively.

S3969 Veratric acid Veratric acid (3,4-Dimethoxybenzoic acid), a simple benzoic acid derived from plants and fruits, has anti-oxidant, anti-inflammation, and blood pressure-lowering effects. Veratric acid reduces upregulated COX-2 expression, and levels of PGE2, IL-6 after UVB irradiation.
S9236 α-Cyperone α-Cyperone (alpha-cyperone), a major active compound of Cyperus rotundus, exhibits biological activities, such as antivirulence, antigenotoxic, and antibacterial activities. α-Cyperone (alpha-cyperone) is associated with the down-regulation of COX-2, IL-6, Nck-2, Cdc42 and Rac1.
S0752 AUDA AUDA (compound 43) is a potent inhibitor of soluble epoxide hydrolase (sEH) with IC50 of 18 nM and 69 nM for the mouse sEH and human sEH, respectively. AUDA has anti-inflammatory activity that reduces the protein expression of MMP-9, IL-1β, TNF-α and TGF-β. AUDA downregulates Smad3 and p38 signaling pathways.
S0777 Isuzinaxib (APX-115 free base) APX-115 free base (Ewha-18278 free base) is a potent, orally active inhibitor of pan NADPH oxidase (pan-Nox) with Ki of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. APX-115 free base (Ewha-18278 free base) significantly suppresses the expression of inflammatory molecules including MCP-1/CCL2, IL-6, and TNFα in the diabetic kidney.
E0008 Atractylodin Atractylodin (Atractydin) is one of the major constituents of the rhizome of Atractylodes lancea and inhibits N-acylethanolamine-hydrolyzing acid amidase (NAAA) activity with an IC50 of 2.81 µM. Atractylodin also inhibits interleukin-6 (IL-6) by blocking NPM-ALK activation and MAPKs.
S6579 RCGD423 RCGD-423 is a modulator of Glycoprotein 130 (gp130, IL6ST, IL6-beta, CD130) signalling that regulates cartilage growth and differentiation.
S5973 Methylprednisolone Acetate Methylprednisolone (NSC-19987, Medrol) acetate is a synthetic glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation. Methylprednisolone activates ACE2 and reduces IL-6 levels, thus improves severe or critical COVID-19. Methylprednisolone markedly reduces autophagy and apoptosis.
S4966 4-Methylesculetin 4-methylesculetin is one of the coumarin derivatives with great anti-oxidant and anti-inflammatory activities. 4-Methylesculetin inhibits myeloperoxidase (MPO) activity and reduces IL-6 level.
S9054 Pectolinarin Pectolinarin is a major compound in Cirsium setidens with anti-inflammatory activity. Pectolinarin inhibits secretion of IL-6 and IL-8, as well as the production of PGE2 and NO. Pectolinarin induces apoptosis via inactivation of the PI3K/Akt pathway.
E1153 LMT-28 LMT-28 is a novel synthetic interleukin-6 (IL-6) inhibitor that functions through direct binding to gp130.
S3293 Gardenoside Gardenoside is a natural compound extracted from Gardenia fruits, with hepatoprotective properties. Gardenoside inhibits TNF-α, IL-1β, IL-6 and NFκB activation. Gardenoside also has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis. Gardenoside suppresses the pain in rats model of chronic constriction injury by regulating the P2X3 and P2X7 receptors.
S9660 Remibrutinib Remibrutinib is a potent, highly selective covalent inhibitor of bruton tyrosine kinase (BTK) with IC50 of 1.3 nM, 2.5 nM and 18 nM for BTK, FcγR-induced IL8 and anti-IgM/IL4-induced CD69, respectively. Remibrutinib (LOU064) exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for the treatment of autoimmune diseases.
S0139 MD2-TLR4-IN-1 MD2-TLR4-IN-1 (Compound 22m) is a potent inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4). MD2-TLR4-IN-1 (compound 22m) inhibits lipopolysaccharide (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 of 0.89 μM and 0.53 μM, respectively.
S9075 Mulberroside A Mulberroside A, isolated from the ethanol extract of Morus alba roots, is widely employed as an active ingredient in cosmetic products due to its anti-tyrosinase and anti-oxidant activities. Mulberroside A decreases the expressions of TNF-α, IL-1β and IL-6 and inhibits the activation of NALP3, caspase-1 and NF-κB and the phosphorylation of ERK, JNK and p38.
S5579 Chelidonic acid Chelidonic acid (Jerva acid, Jervaic acid, γ-Pyrone-2,6-dicarboxylic acid) is a secondary metabolite found in several plants with therapeutic potential in allergic disorders in experimental animals. Chelidonic acid inhibits IL-6 production by blocking NF-κB and caspase-1 in HMC-1 cells. Chelidonic acid is also an inhibitor of glutamate decarboxylase with Ki of 1.2 μM.
E2630 SKF-86002 SKF-86002 is an orally active p38 MAPK inhibitor, inhibits lipopolysaccharide (LPS)-stimulate human monocyte IL-1 and TNF-α production with IC50 of 1 μM, also inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid.
S6347 5'-N-Ethylcarboxamidoadenosine (NECA) 5'-N-Ethylcarboxamidoadenosine (NECA, 5'-(N-Ethylcarboxamido)adenosine, Adenosine-5'N-ethylcarboxamide, 5'-Ethylcarboxamidoadenosine) is a stable, nonselective adenosine receptor agonist. 5'-N-Ethylcarboxamidoadenosine acts via multiple mechanisms including: reducing diabetes-induced oxidative stress, inhibiting gene expression of IL-18, TNF-α and ICAM-1 (intercellular adhesion molecule 1 (CD54)), and blocking activation of the JNK-MAPK pathway.
S9129 20(S)-Ginsenoside Rh1 20(S)-Ginsenoside Rh1 (Prosapogenin A2, Sanchinoside B2, Sanchinoside Rh1) is one of major bioactive compounds extracted from red ginseng, which has been increasingly used for enhancing cognition and physical health worldwide. It exhibits potent characteristics of anti-inflammatory, antioxidant, immunomodulatory effects, and positive effects on the nervous system. Ginsenoside Rh1 inhibits the expression of PPAR-γ, TNF-α, IL-6, and IL-1β.
S3138 Methylthiouracil Methylthiouracil (NSC-193526, NSC-9378,MTU) is an antithyroid agent. Methylthiouracil suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2.
E0177 Hydrocortisone sodium succinate Hydrocortisone sodium succinate (Hydrocortisone 21-hemisuccinate sodium salt) has significant inhibitory effects on the IL-6 bioactivity with IC50 of 6.7 μM. Hydrocortisone sodium succinate can bind to glucocorticoid receptor, initiating the transcription of anti-inflammatory and immunosuppressive mediators.
S0228 SU 5201 SU 5201 (NSC 247030) is an interleukin-2 (IL-2) inhibitor.
S3304 Stylopine Stylopine ((R,S)-Stylopine, Tetrahydrocoptisine) reduces nitric oxide (NO), prostaglandin E2 (PGE2), tumor necrosis factor-alpha (TNF-alpha) and interleukin-1beta (IL-1beta), and the IL-6 production and cyclooxygenase-2 (COX-2) activity caused by the LPS stimulation. Stylopine is a major component of the leaf of Chelidonium majus L.
S9184 Forsythoside B Forsythoside B is a phenylethanoid glycoside isolated from the leaves of Lamiophlomis rotata Kudo, a Chinese folk medicinal plant. Forsythoside B has potent neuroprotective effects and has anti-inflammation, antioxidant, and antisepsis properties. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB.
S3299 Demethyleneberberine Demethyleneberberine (DMB), a component of Cortex Phellodendri Chinensis (CPC), significantly alleviates the weight loss and diminishes myeloperoxidase (MPO) activity, while significantly reduces the production of pro-inflammatory cytokines, such as interleukin (IL)-6 and tumor necrosis factor-α (TNF-α), and inhibits the activation of NF-κB signaling pathway. Demethyleneberberine (DMB) potentially ameliorates NAFLD (Non-alcoholic fatty liver disease) by activating AMPK pathways.
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.
Nature, 2025, 644(8078):1058-1068
J Virol, 2025, e0128025.
Int J Nanomedicine, 2024, 19:3589-3605
S7455 Resatorvid (TAK-242) Resatorvid (TAK-242, CLI-095) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α and IL-6 in macrophages with IC50 of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy.
EMBO J, 2025, 10.1038/s44318-025-00515-z
Carbohydr Polym, 2025, 350:122980
J Neuroinflammation, 2025, 22(1):38
S1189 Aprepitant Aprepitant is a potent and selective neurokinin-1 receptor antagonist with IC50 of 0.1 nM. Aprepitant reduces levels of pro-inflammatory cytokines including G-CSF, IL-6, IL-8 and TNFα. Aprepitant inhibits HIV infection of human macrophages.
Br J Cancer, 2024, 10.1038/s41416-024-02608-8
Inflammation, 2023, 46(1):256-269
Nat Commun, 2022, 13(1):4995
Aprepitant-S118901W0220161031.gif
S8966 T-5224 T-5224 is a selective inhibitor of transcription factor c-Fos/activator protein (AP)-1 with anti-inflammatory effects. T-5224 specifically inhibits the DNA binding activity of c-Fos/c-Jun and the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription.
MedComm (2020), 2025, 6(4):e70154
MedComm (2020), 2025, 6(4):e70154
Cells, 2025, 14(7)474
S7124 SC144 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.
Cell Rep Med, 2025, S2666-3791(25)00102-8
Respir Res, 2025, 26(1):285
bioRxiv, 2025, 2025.01.20.633954
SC144-S712401Y0220161118.gif
S6414 Apilimod (STA-5326) Apilimod 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. Apilimod (STA-5326) 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. Apilimod (STA-5326) is also a cell permeable small molecule that specifically inhibits PIKfyve with IC50 of 14 nM.
Nat Commun, 2025, 16(1):8123
Nat Commun, 2025, 16(1):6397
J Cell Biol, 2025, 224(6)e202408158
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.
Stem Cell Reports, 2025, 20(10):102673
Cancer Commun -Lond), 2023, 43(10):1117-1142
Microbiol Res, 2023, 276:127480
FLLL32-S725901Z0520161121.gif
S8301 Ossirene (AS101) Ossirene (AS101), a potent in vitro and in vivo immunomodulator, is a novel inhibitor of IL-1beta converting enzyme.
Mol Neurodegener, 2025, 20(1):5
Cell Biosci, 2025, 15(1):18
Stem Cell Rev Rep, 2025, none
S9668 PKR-IN-C16 PKR-IN-C16 (C16, Imidazolo-oxindole PKR inhibitor C16) is a specific inhibitor of RNA-dependent protein kinase (PKR, Protein Kinase R, EIF2AK2). PKR-IN-C16 prevents apoptosis and IL-1β production in an acute excitotoxic rat model with a neuroinflammatory component.
Immunity, 2025, 58(10):2489-2504.e8
Exp Mol Med, 2024, 56(2):408-421.
EMBO J, 2024, 43(5):780-805.
S8879 BMS-986165 (Deucravacitinib) 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
S4267 Diacerein Diacerein is an inhibitor of pro-inflammatory cytokine Interleukin-1B (IL-1B) production, prescribed for osteoarthritis and chronic inflammatory arthritis.
MedComm (2020), 2024, 5(8):e668
Oral Dis, 2022, 10.1111/odi.14294
Free Radic Biol Med, 2021, 165:171-183
Diacerein-S426701Z0720161110.gif
S6898 RCM-1 RCM-1 is a nontoxic inhibitor of Forkhead box M1 (FOXM1) that suppresses goblet cell metaplasia and prevents IL-13 and STAT6 signaling in allergen-exposed mice. RCM-1 decreases carcinogenesis and nuclear β-catenin.
Gut, 2025, gutjnl-2025-335163
Parasit Vectors, 2025, 18(1):100
bioRxiv, 2025, 2025.05.25.655133
S9727 Ac-YVAD-cmk 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.
Cell Commun Signal, 2024, 22(1):368
J Transl Med, 2024, 22(1):1139
Int J Mol Sci, 2024, 25(4)2185
S1733 Methylprednisolone Methylprednisolone (NSC-19987,U 7532) is a synthetic glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation. Methylprednisolone activates ACE2 and reduces IL-6 levels, thus improves severe or critical COVID-19. Methylprednisolone markedly reduces autophagy and apoptosis.
Food Chem Toxicol, 2024, 188:114665
Drug Test Anal, 2020, 10.1002/dta.2917
Nat Med, 2017, 23(4):424-428
Methylprednisolone-S173301X0220161108.gif
S3871 Muscone Muscone (3-Methylcyclopentadecanone, Methylexaltone), a flavouring ingredient, is an organic compound that is the primary contributor to the odor of musk and also a potent anti-inflammatory agent. Muscone significantly downregulats the levels of LPS-induced inflammatory cytokines and inhibits NF-κB and NLRP3 inflammasome activation in BMDMs. Muscone remarkably decreases the levels of inflammatory cytokines (IL-1β, TNF-α and IL-6).
Ecotoxicol Environ Saf, 2025, 292:117961
Invest Ophthalmol Vis Sci, 2025, 66(5):21
Toxicol Appl Pharmacol, 2025, 503:117494
S8261 GSK583 GSK583 is a highly potent and selective inhibitor of RIP2 kinase with IC50 of 5 nM. GSK583 also inhibits both TNF-α and IL-6 production with IC50 of ~200 nM in explant cultures.
J Invest Dermatol, 2025, S0022-202X(25)00494-4
Cancer Res, 2020, canres.530.2020
J Neuroinflammation, 2020, 17(1):364
S0785 Apilimod mesylate 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. Apilimod mesylate (STA-5326 mesylate) 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. Apilimod mesylate (STA-5326 mesylate) is also a cell permeable small molecule that specifically inhibits PIKfyve with IC50 of 14 nM.
bioRxiv, 2024, 2024.02.28.582543
Stem Cell Reports, 2022, 17(2):397-412
Hum Mol Genet, 2021, 29(22):3589-3605
S0787 3-Deazaadenosine hydrochloride 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.
Virus Res, 2025, 358:199590
J Exp Clin Cancer Res, 2022, 41(1):36
Free Radic Biol Med, 2021, 168:25-43
S3292 (3R,8S)-Falcarindiol Falcarindiol (FAD, (3R,8S)-Falcarindiol, FaDOH) is a natural polyacetylene compound found rich in many plants of the Umbelliferae family. Falcarindiol suppresses LPS-stimulated expression of inducible nitric oxide synthase (iNOS), tumor necrosis factor alpha (TNFα), interleukin-6 (IL-6), and interleukin-1 beta (IL-1β). Falcarindiol attenuates the LPS-induced activation of JNK, ERK, STAT1, and STAT3 signaling molecules.
Antioxidants (Basel), 2024, 13(12)1533
Front Cell Infect Microbiol, 2023, 13:1128000
Front Pharmacol, 2021, 12:656697
S0826 A-740003 A-740003 is a potent, selective and competitive antagonist of P2X7 receptor with IC50 of 18 nM and 40 nM for rat and human P2X7 receptors, respectively. A-740003 potently blocks agonist-evoked IL-1β release and pore formation with IC50 of 156 nM and 92 nM in differentiated human THP-1 cells.
Am J Cancer Res, 2024, 14(2):585-600
Cell Rep, 2023, 42(7):112696
S9052 Auraptene Auraptene (7-geranyloxycoumarin) is a natural coumarin derived from citrus plants and possesses valuable pharmacological properties, including anticarcinogenic, anti-inflammatory, antihelicobacter, antigenotoxic, and neuroprotective effects. Auraptene inhibits matrix metalloproteinase 2 (MMP-2) as well as key inflammatory mediators, including IL-6, IL-8 and chemokine (C-C motif) ligand-5(CCL5).
Neuropharmacology, 2025, 269:110352
Plant Physiology, 2012, 81–94
S6620 Danirixin (GSK1325756) Danirixin (GSK1325756) is a small molecule, non-peptide, high affinity (IC50 for CXCL8 (IL-8) binding = 12.5 nM), selective, and reversible CXCR2 antagonist.
Redox Biol, 2024, 76:103323
Theranostics, 2019, 9(18):5332-5346
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.
Cancer Discov, 2023, 13(2):410-431
Cancer Discov, 2023, 13(2):410-431
S0472 EC330 EC330 is a steroidal inhibitor of leukemia inhibitory factor (LIF, an interleukin 6 class cytokine). EC330 inhibits the LIF/LIF-R signaling and blocks the promoting effects of LIF on growth and migration of cancer cells.
NPJ Precis Oncol, 2024, 8(1):246
Br J Cancer, 2021, 10.1038/s41416-021-01631-3
S0781 IQ 3 IQ 3 is a specific c-Jun N-terminal kinase (JNK) inhibitor with Kd of 66 nM, 240 nM and 290 nM for JNK3, JNK1 and JNK2, respectively. IQ 3 inhibits LPS-induced NF-κB/AP1 transcriptional activity in THP1-Blue cells with IC50 of 1.4 μM. IQ 3 also inhibits TNF-α and IL-6 production in vitro.
Int J Biol Sci, 2024, 20(6):2323-2338
S5972 Hydrocortisone hemisuccinate Hydrocortisone hemisuccinate (A-hydrocort, Hydrocortisone 21-hemisuccinate), a physiological glucocorticoid with anti-inflammatory properties, is an inhibitor of proinflammatory cytokine with IC50 of 6.7 μM and 21.4 μM for Interleukin-6 (IL-6) and IL-3, respectively.
J Transl Med, 2023, 21(1):50
S9374 2',5'-Dihydroxyacetophenone 2',5'-Dihydroxyacetophenone (DHAP, 2-Acetylhydroquinone, Quinacetophenone) is a mixture of dihydroxyacetophenone isomers is used in food flavouring. 2',5'-Dihydroxyacetophenone significantly inhibits NO production via the suppression of iNOS expression. 2',5'-Dihydroxyacetophenone significantly decreases levels of the pro-inflammatory cytokines TNF-α and IL-6 by blocking the ERK1/2 and NF-κB signaling pathways.
Pathol Oncol Res, 2019, 25(1):301-309
S6850 NE 52-QQ57 NE 52-QQ57 is a selective, and orally available antagonist of G-protein coupled receptor 4 (GPR4) with IC50 of 0.07 μM. NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation with IC50 of 26.8 nM in HEK293 cells. The antagonism of GPR4 with NE 52-QQ57 significantly inhibits the AGE-induced increased expression of several key inflammatory cytokines and signaling molecules, including tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6, inducible nitric oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX2), and prostaglandin E2 (PGE2).
Exp Hematol Oncol, 2024, 13(1):13
S9417 Homoplantaginin Homoplantaginin (Hispidulin-7-glucoside), a main flavonoid from a traditional Chinese medicine Salvia plebeia, has anti-inflammatory and anti-oxidant properties. Homoplantaginin inhibits TNF-α and IL-6 mRNA expression, IKKβ and NF-κB phosphorylation.
Front Pharmacol, 2025, 16:1526107
S9502 Madecassic acid Madecassic acid (Brahmic acid), a natural triterpene first isolated from C. asiatica, has diverse anti-inflammatory and anti-diabetic effects, blocking NF-κB activation in macrophages and causing by iNOS, COX-2, TNF-alpha, IL-1beta and IL-6 inhibition.
Drug Des Devel Ther, 2022, 16:3793-3804
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.
Cell Rep Med, 2025, S2666-3791(25)00231-9
S3261 Myrislignan Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan inhibits interleukin-6 (IL-6) and tumour necrosis factor-α (TNF-α). Myrislignan significantly inhibits the expressions of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2) dose-dependently in LPS-stimulated macrophage cells. Myrislignan inhibits the NF-κB signalling pathway activation.
Oxid Med Cell Longev, 2023, 2023:7098313
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).
S3312 Diethyl phosphate

Diethyl phosphate (DEP, DPF, Diethyl phosphoric acid, diethyl hydrogen phosphate), a non-specific metabolite of organophosphorus pesticides in the gut environment, significantly enriches opportunistic pathogens leading to a decrease in interleukin-6 (IL-6).

S5764 YM 90709 YM 90709 is a novel IL-5 inhibitor which selectively blocks the binding of IL-5 to the IL-5 receptor (IL-5R).
S3590 Triolein Triolein is an inhibitor of metalloproteinase-1 (MMP-1) and reduces both the expression of IL-6 and ROS generation in irradiated keratinocytes.
E0314 JTE-607 Dihydrochloride

JTE-607 Dihydrochloride is a prodrug compound that is converted to an active form by ester hydrolysis. JTE-607 is a multiple cytokine production inhibitor that targets CPSF3 and inhibits pre-mRNA processing. JTE-607 inhibits tumor necrosis factor (TNF)-alpha, interleukin (IL)-1beta, IL-6, IL-8 and IL-10, from LPS-stimulated human PBMCs, with IC50 values of 11 nM, 5.9 nM, 8.8 nM, 7.3 nM and 9.1 nM, respectively.

S3969 Veratric acid Veratric acid (3,4-Dimethoxybenzoic acid), a simple benzoic acid derived from plants and fruits, has anti-oxidant, anti-inflammation, and blood pressure-lowering effects. Veratric acid reduces upregulated COX-2 expression, and levels of PGE2, IL-6 after UVB irradiation.
S9236 α-Cyperone α-Cyperone (alpha-cyperone), a major active compound of Cyperus rotundus, exhibits biological activities, such as antivirulence, antigenotoxic, and antibacterial activities. α-Cyperone (alpha-cyperone) is associated with the down-regulation of COX-2, IL-6, Nck-2, Cdc42 and Rac1.
S0752 AUDA AUDA (compound 43) is a potent inhibitor of soluble epoxide hydrolase (sEH) with IC50 of 18 nM and 69 nM for the mouse sEH and human sEH, respectively. AUDA has anti-inflammatory activity that reduces the protein expression of MMP-9, IL-1β, TNF-α and TGF-β. AUDA downregulates Smad3 and p38 signaling pathways.
S0777 Isuzinaxib (APX-115 free base) APX-115 free base (Ewha-18278 free base) is a potent, orally active inhibitor of pan NADPH oxidase (pan-Nox) with Ki of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. APX-115 free base (Ewha-18278 free base) significantly suppresses the expression of inflammatory molecules including MCP-1/CCL2, IL-6, and TNFα in the diabetic kidney.
E0008 Atractylodin Atractylodin (Atractydin) is one of the major constituents of the rhizome of Atractylodes lancea and inhibits N-acylethanolamine-hydrolyzing acid amidase (NAAA) activity with an IC50 of 2.81 µM. Atractylodin also inhibits interleukin-6 (IL-6) by blocking NPM-ALK activation and MAPKs.
S5973 Methylprednisolone Acetate Methylprednisolone (NSC-19987, Medrol) acetate is a synthetic glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation. Methylprednisolone activates ACE2 and reduces IL-6 levels, thus improves severe or critical COVID-19. Methylprednisolone markedly reduces autophagy and apoptosis.
S4966 4-Methylesculetin 4-methylesculetin is one of the coumarin derivatives with great anti-oxidant and anti-inflammatory activities. 4-Methylesculetin inhibits myeloperoxidase (MPO) activity and reduces IL-6 level.
S9054 Pectolinarin Pectolinarin is a major compound in Cirsium setidens with anti-inflammatory activity. Pectolinarin inhibits secretion of IL-6 and IL-8, as well as the production of PGE2 and NO. Pectolinarin induces apoptosis via inactivation of the PI3K/Akt pathway.
E1153 LMT-28 LMT-28 is a novel synthetic interleukin-6 (IL-6) inhibitor that functions through direct binding to gp130.
S3293 Gardenoside Gardenoside is a natural compound extracted from Gardenia fruits, with hepatoprotective properties. Gardenoside inhibits TNF-α, IL-1β, IL-6 and NFκB activation. Gardenoside also has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis. Gardenoside suppresses the pain in rats model of chronic constriction injury by regulating the P2X3 and P2X7 receptors.
S9660 Remibrutinib Remibrutinib is a potent, highly selective covalent inhibitor of bruton tyrosine kinase (BTK) with IC50 of 1.3 nM, 2.5 nM and 18 nM for BTK, FcγR-induced IL8 and anti-IgM/IL4-induced CD69, respectively. Remibrutinib (LOU064) exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for the treatment of autoimmune diseases.
S0139 MD2-TLR4-IN-1 MD2-TLR4-IN-1 (Compound 22m) is a potent inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4). MD2-TLR4-IN-1 (compound 22m) inhibits lipopolysaccharide (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 of 0.89 μM and 0.53 μM, respectively.
S9075 Mulberroside A Mulberroside A, isolated from the ethanol extract of Morus alba roots, is widely employed as an active ingredient in cosmetic products due to its anti-tyrosinase and anti-oxidant activities. Mulberroside A decreases the expressions of TNF-α, IL-1β and IL-6 and inhibits the activation of NALP3, caspase-1 and NF-κB and the phosphorylation of ERK, JNK and p38.
S5579 Chelidonic acid Chelidonic acid (Jerva acid, Jervaic acid, γ-Pyrone-2,6-dicarboxylic acid) is a secondary metabolite found in several plants with therapeutic potential in allergic disorders in experimental animals. Chelidonic acid inhibits IL-6 production by blocking NF-κB and caspase-1 in HMC-1 cells. Chelidonic acid is also an inhibitor of glutamate decarboxylase with Ki of 1.2 μM.
E2630 SKF-86002 SKF-86002 is an orally active p38 MAPK inhibitor, inhibits lipopolysaccharide (LPS)-stimulate human monocyte IL-1 and TNF-α production with IC50 of 1 μM, also inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid.
S6347 5'-N-Ethylcarboxamidoadenosine (NECA) 5'-N-Ethylcarboxamidoadenosine (NECA, 5'-(N-Ethylcarboxamido)adenosine, Adenosine-5'N-ethylcarboxamide, 5'-Ethylcarboxamidoadenosine) is a stable, nonselective adenosine receptor agonist. 5'-N-Ethylcarboxamidoadenosine acts via multiple mechanisms including: reducing diabetes-induced oxidative stress, inhibiting gene expression of IL-18, TNF-α and ICAM-1 (intercellular adhesion molecule 1 (CD54)), and blocking activation of the JNK-MAPK pathway.
S9129 20(S)-Ginsenoside Rh1 20(S)-Ginsenoside Rh1 (Prosapogenin A2, Sanchinoside B2, Sanchinoside Rh1) is one of major bioactive compounds extracted from red ginseng, which has been increasingly used for enhancing cognition and physical health worldwide. It exhibits potent characteristics of anti-inflammatory, antioxidant, immunomodulatory effects, and positive effects on the nervous system. Ginsenoside Rh1 inhibits the expression of PPAR-γ, TNF-α, IL-6, and IL-1β.
S3138 Methylthiouracil Methylthiouracil (NSC-193526, NSC-9378,MTU) is an antithyroid agent. Methylthiouracil suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2.
E0177 Hydrocortisone sodium succinate Hydrocortisone sodium succinate (Hydrocortisone 21-hemisuccinate sodium salt) has significant inhibitory effects on the IL-6 bioactivity with IC50 of 6.7 μM. Hydrocortisone sodium succinate can bind to glucocorticoid receptor, initiating the transcription of anti-inflammatory and immunosuppressive mediators.
S0228 SU 5201 SU 5201 (NSC 247030) is an interleukin-2 (IL-2) inhibitor.
S3304 Stylopine Stylopine ((R,S)-Stylopine, Tetrahydrocoptisine) reduces nitric oxide (NO), prostaglandin E2 (PGE2), tumor necrosis factor-alpha (TNF-alpha) and interleukin-1beta (IL-1beta), and the IL-6 production and cyclooxygenase-2 (COX-2) activity caused by the LPS stimulation. Stylopine is a major component of the leaf of Chelidonium majus L.
S9184 Forsythoside B Forsythoside B is a phenylethanoid glycoside isolated from the leaves of Lamiophlomis rotata Kudo, a Chinese folk medicinal plant. Forsythoside B has potent neuroprotective effects and has anti-inflammation, antioxidant, and antisepsis properties. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB.
S3299 Demethyleneberberine Demethyleneberberine (DMB), a component of Cortex Phellodendri Chinensis (CPC), significantly alleviates the weight loss and diminishes myeloperoxidase (MPO) activity, while significantly reduces the production of pro-inflammatory cytokines, such as interleukin (IL)-6 and tumor necrosis factor-α (TNF-α), and inhibits the activation of NF-κB signaling pathway. Demethyleneberberine (DMB) potentially ameliorates NAFLD (Non-alcoholic fatty liver disease) by activating AMPK pathways.
S1709 17β-Estradiol 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.
Cancer Cell, 2025, 43(5):891-904.e10
Nat Commun, 2025, 16(1):758
Cell Rep Med, 2025, 6(7):102192
S2979 CU-T12-9 CU-T12-9 is a specific agonist of Toll-like receptor (TLR) 1/2 with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.
Nat Commun, 2025, 16(1):2743
Biomedicine & Pharmacotherapy, 2023, 114638
Biomed Pharmacother, 2023, 162:114638
S0771 BRD6989 BRD6989 is a selective inhibitor of CDK8 and CDK19. BRD6989 upregulates IL-10. BRD6989 is an analog of the natural product cortistatin A (dCA).
Infect Drug Resist, 2021, 14:3135-3143
S0094 SR 0987 SR 0987, a SR 1078 analog, is an agonist for T cell-specific RORγ (RORγt) with EC50 of 800 nM. SR 0987 represses PD-1, produces IL17 and is potential for the treatment of cancer.
Evid Based Complement Alternat Med, 2022, 2022:8315503.
S2015 Suplatast Tosylate Suplatast Tosylate (IPD-1151T, Suplatast Tosilate) is a novel capsular anti-asthmatic agent that suppresses both IgE production, IL-4 and IL-5 synthesis with IC50 above 100 μM.
J Transl Med, 2022, 20(1):615
P1235 Raleukin Anakinra (Raleukin, AMG-719) is an exogenous antagonist of recombinant human interleukin-1 receptor that also inhibits caspase-1 and caspase-9 activity with Ki of 0.201 μM and 0.31 μM respectively. It is used in research to study IL-1 blockade in inflammation, tumor growth, islet transplantation, and cardiac injury models.
Inflammation, 2025, 10.1007/s10753-025-02315-3
P1252New JNJ-77242113(Icotrokinra) Icotrokinra (JNJ-77242113, JNJ-2113, PN-235) is an orally available and selective antagonist of the IL-23 receptor. It also inhibits IL-23–induced STAT3 phosphorylation in peripheral blood mononuclear cells with an IC50 of 5.6 pM and suppresses IL-23–induced IFN-γ production in NK cells with an IC50 of 18.4 pM. It also exhibits anti-inflammatory activity in a TNBS-induced colitis model in rats and holds potential for studying psoriasis, psoriatic arthritis, and inflammatory bowel disease.
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.
Nature, 2025, 644(8078):1058-1068
J Virol, 2025, e0128025.
Int J Nanomedicine, 2024, 19:3589-3605
S6281 Sodium Thiocyanate Sodium Thiocyanate (NaSCN, Sodium rhodanide, Sodium sulfocyanate, Sodium rhodanate), one of the main sources of the thiocyanate anion, is used as a precursor for the synthesis of pharmaceuticals and other specialty chemicals. Sodium thiocyanate (NaSCN) reduces IL-6, whereas increases IL-10 levels. Sodium thiocyanate also reduces ROS.
Evid Based Complement Alternat Med, 2022, 2022:8315503
S3745 Balsalazide disodium Balsalazide Disodium is the disodium salt form of balsalazide, an aminosalicylate and oral prodrug that is enzymatically cleaved in the colon to produce the anti-inflammatory agent mesalazine. Balsalazide Disodium suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway.
Front Microbiol, 2020, 10:2936
S4842 Balsalazide Balsalazide (Colazal, Giazo), an aminosalicylate and oral prodrug, is enzymatically cleaved in the colon to produce the anti-inflammatory agent mesalazine. Balsalazide suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway.
S6579 RCGD423 RCGD-423 is a modulator of Glycoprotein 130 (gp130, IL6ST, IL6-beta, CD130) signalling that regulates cartilage growth and differentiation.
P1252New JNJ-77242113(Icotrokinra) Icotrokinra (JNJ-77242113, JNJ-2113, PN-235) is an orally available and selective antagonist of the IL-23 receptor. It also inhibits IL-23–induced STAT3 phosphorylation in peripheral blood mononuclear cells with an IC50 of 5.6 pM and suppresses IL-23–induced IFN-γ production in NK cells with an IC50 of 18.4 pM. It also exhibits anti-inflammatory activity in a TNBS-induced colitis model in rats and holds potential for studying psoriasis, psoriatic arthritis, and inflammatory bowel disease.