TNF-alpha Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
S7942	Bioymifi	Bioymifi, a small-molecule death receptor 5 (DR5) agonist, binds to the extracellular domain(ECD) of DR5 with a Kd of 1.2 μM but showed little binding affinity to the DR4 ECD. It induces DR5 clustering and aggregation, leading to apoptosis.	Cell Death Dis, 2024, 15(1):27 Front Immunol, 2020, 11:1345
S3515	Benpyrine racemate	Benpyrine racemate ((Rac)-Benpyrine) is a potent, highly specific and orally active inhibitor of TNF-α and attenuates TNF-α-induced inflammation, thereby reducing liver and lung injury.	Theranostics, 2025, 15(7):2852-2869
S9396	Geraniin	Geraniin, a hydrolysable polyphenol derived from Nephelium lappaceum L. fruit rind, has been shown to possess significant antioxidant activity in vitro.The IC50 values of TNF-α release inhibition were 43 μM for geraniin.	Saudi J Biol Sci, 2022, 29(1):168-174
S9090	Corilagin	Corilagin, discovered in many medicinal plants such as Phyllanthus speices etc., has multiple activities including anti-oxidative, anti-inflammatory, anti-apoptotic, hepatoprotective and others. It is an inhibitor of TNF-α.	Int Immunopharmacol, 2025, 163:115245
S2465	CPI-1189	CPI-1189 (REN 1654, REN 1189) is the proapoptotic cytokine tumor necrosis factor (TNF) alpha inhibitor. This compound intracellularly inhibits the p38 mitogen-activated protein kinase phosphoactivation and shows neuroprotective effects.	Aging (Albany NY), 2021, 13(5):6712-6723
E3067	Trionycis Carapax Extract	Trionycis Carapax Extract is obtained from Carapax Trionycis, of which Carapax Trionycis extracts with molecular weight less than 6 KD (CT6) down-regulates TNF-α, IL-1β and IL-6 expression in TGF-β1-treated HSC-T6, indicating the potential therapeutic effect of these extracts against liver fibrosis.
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.
S3231	UCB-9260	UCB-9260 is an orally active inhibitor that inhibits TNF signalling by stabilising an asymmetric form of the trimer. This compound binds TNF with Kd of 13 nM. It also inhibits NF-κB with IC50 of 202 nM after TNF stimulation.
E3245	Piperis Kadsurae Caulis Extract	Piperis Kadsurae Caulis Extract is extracted from Piperis Kadsurae Caulis., which can reduce the expression level of IL-1β and TNF-α in cells.
E6029	Lenalidomide hemihydrate	Lenalidomide hemihydrate (CC-5013 hemihydrate) is a potent inhibitor of TNF-alpha with a IC50 of 13 nM. It induces tyrosine phosphorylation of CD28 on T cells, which subsequently activates NF-κB. It acts as a ligand for the ubiquitin E3 ligase cereblon (CRBN), leading to the selective ubiquitination and degradation of the lymphoid transcription factors IKZF1 and IKZF3 through the CRBN-CRL4 ubiquitin ligase complex.
E3310	Brassica Juncea Seed Extract	Brassica juncea seed Extract is obtained from seeds of Brassica juncea L., which confers a protective/therapeutic effect against thioacetamide-induced acute liver failure in experimental animal models, by markedly downregulating the expression levels of TNF-α and IL-6, and reversing DNA genotoxicity.
E3329	Centella Asiatica Extract	Centella Asiatica Extract is extrcated from Centella Asiatica, which inhibits TNF-alpha and can be used as a therapeutic agent for atopic dermatitis.
S3540	UTL-5g	UTL-5g (GBL-5g) is a novel small-molecule TNF-α inhibitor which can lower hepatotoxicity, nephrotoxicity and myelotoxicity induced by Cisplatin.
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. This compound 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.
S5584	Citronellol	Citronellol (Dihydrogeraniol, (±)-β-Citronellol), a constituent of rose and geranium oils, is used in perfumes and insect repellents. This compound can cause necrotic apoptosis of NCI-H1299 cells by up-regulating TNF-α, RIP1 / RIP3 activities, and down-regulating caspase-3 / caspase-8 activities. It also results in a biphasic increase in ROS production at 1 h and at 12 h in NCI-H1299 cells.
E0130	Apigenin-7-O-glucuronide	Apigenin-7-O-glucuronide (Apigenin-7-glucuronide) is the major flavonoid found in milk thistle. Apigenin 7-o-glucuronide inhibits tumor necrosis factor alpha (TNF-α) and total nitrite release in lipopolysaccharide-activated macrophages.
E3024	Ampelopsis Japonica Root Extract	Ampelopsis Japonica Root Extract is extracted from Ampelopsis japonica, may be a new therapeutic agent with the potential to reduce or replace corticosteroids and its mechanisms are closely related to regulation of TNF-α production.
S0248^New	Hispidol	Hispidol is a potent inhibitor of TNF-α–induced monocyte adhesion to colon epithelial cells with an IC50 of 0.50 μM, and effectively suppresses LPS-induced TNF-α gene expression. Its inhibition of TNF-α is linked to reduced AP-1 transcriptional activity, highlighting its potential as a therapeutic candidate for IBD.
S4902	QNZ (EVP4593)	QNZ (EVP4593) shows potent inhibitory activity toward both NF-κB activation and TNF-α production with IC50 of 11 nM and 7 nM in Jurkat T cells, respectively.	Cell Discov, 2025, 11(1):84 Nat Commun, 2025, 16(1):5912 Cell Rep Med, 2025, 6(1):101917
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. This compound downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF, and it also inhibits autophagy.	EMBO J, 2025, 10.1038/s44318-025-00515-z Carbohydr Polym, 2025, 350:122980 J Neuroinflammation, 2025, 22(1):38
S8279	(±)-Shikonin	(±)-Shikonin, a potent and specific Pyruvate kinase M2 (PKM2) inhibitor, is a major component of zicao (purple gromwell, the dried root of Lithospermum erythrorhizon), a Chinese herbal medicine with various biological activities. It is also an inhibitor of TMEM16A chloride channel activity using cell-based fluorescent-quenching assay. Shikonin exerts an anti-inflammatory effect by inhibiting tumor necrosis factor-α (TNF-α) and prevents activation of nuclear factor-κB (NF-κB) pathway via proteasome inhibition.	Signal Transduct Target Ther, 2025, 10(1):341 J Exp Clin Cancer Res, 2025, 44(1):299 Free Radic Biol Med, 2025, 237:65-75
S1193	Thalidomide	Thalidomide was introduced as a sedative drug, immunomodulatory agent and also is investigated for treating symptoms of many cancers. This compound inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1.	Nat Genet, 2025, 57(10):2468-2481 Biomed Pharmacother, 2025, 184:117878 Nat Commun, 2024, 15(1):9195
S7963	TIC10 (ONC201)	TIC10 (ONC201) inactivates Akt and ERK to induce TNF-related apoptosis-inducing ligand (TRAIL) through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. Phase 1/2.	Elife, 2023, 12e85898 J Biol Chem, 2023, S0021-9258(23)02442-0 Neoplasia, 2023, 39:100894
S8034	Apremilast	Apremilast (CC-10004) is a potent and orally active PDE4 and TNF-α inhibitor with IC50 of 74 nM and 77 nM, respectively.	Signal Transduct Target Ther, 2023, 8(1):40 Acta Pharm Sin B, 2022, 12(1):228-245 Int J Mol Sci, 2021, 22(23)12878
S8484	GSK2982772	GSK2982772 is an ATP competitive receptor-interacting protein-1 (RIP1) kinase (RIPK1) inhibitor with the IC50 value of 16 nM. It has exquisite kinase specificity and excellent activity in blocking many TNF-dependent cellular responses.	Antioxidants (Basel), 2021, 10(9)1347 Mol Cell Biochem, 2021, 10.1007/s11010-021-04136-y Exp Ther Med, 2021, 21(2):163
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. This compound significantly downregulats the levels of LPS-induced inflammatory cytokines and inhibits NF-κB and NLRP3 inflammasome activation in BMDMs. It 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
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
S8261	GSK583	GSK583 is a highly potent and selective inhibitor of RIP2 kinase with IC50 of 5 nM. This compound 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
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. This compound activates both the innate and the adaptive immune systems. It 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
S3865	Taurochenodeoxycholic acid	Taurochenodeoxycholic acid (Taurochenodeoxycholate, TCDCA, Chenodeoxycholyltaurine), a bile acid formed in the liver of most species, is used as a cholagogue and choleretic.	Nat Commun, 2021, 12(1):6479 Microbiome, 2019, 7(1):145
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. This compound inhibits LPS-induced NF-κB/AP1 transcriptional activity in THP1-Blue cells with IC50 of 1.4 μM. It also inhibits TNF-α and IL-6 production in vitro.	Int J Biol Sci, 2024, 20(6):2323-2338
S9374	2',5'-Dihydroxyacetophenone	2',5'-Dihydroxyacetophenone (DHAP, 2-Acetylhydroquinone, Quinacetophenone) is a mixture of dihydroxyacetophenone isomers is used in food flavouring. This compound significantly inhibits NO production via the suppression of iNOS expression. It 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. This compound effectively blocks GPR4-mediated cAMP accumulation with IC50 of 26.8 nM in HEK293 cells. The antagonism of GPR4 with this chemical 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. This compound inhibits TNF-α and IL-6 mRNA expression, IKKβ and NF-κB phosphorylation.	Front Pharmacol, 2025, 16:1526107
S8224	PF-3644022	PF-3644022 is a potent freely reversible ATP-competitive inhibitor of MAPKAPK2 (MK2) with an Ki of 3 nM. This compound also potently inhibits TNFα production with an IC50 of 160 nM.	iScience, 2024, 27(4):109339
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). This compound 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. This compound inhibits interleukin-6 (IL-6) and tumour necrosis factor-α (TNF-α). It significantly inhibits the expressions of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2) dose-dependently in LPS-stimulated macrophage cells. It also 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).
E5778^New	CU-CPT 4a	CU-CPT 4a (TLR3-IN-1) is a potent small molecule antagonist of TLR3 with an IC50 of 3.44 µM that also inhibits TLR3/dsRNA-mediated signaling, including TNF-α and IL-1β expression. It is a valuable tool for studying protein-RNA complexes.
S3236	Mesaconitine	Mesaconitine, one of the aconite alkaloids in Aconiti tuber, increases the [Ca2+]i level in endothelial cells by influx of Ca2+ from extracellular spaces.
S0949	Cucurbitacin IIb	Cucurbitacin IIb (CuIIb, Dihydrocucurbitacin F, 25-deacetyl hemslecin A) inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB, blocks nuclear translocation of NF-κB and decreases mRNA levels of IκBα and TNF-α. This compound exhibits anti-inflammatory activity and induces apoptosis. It is isolated from Hemsleya amabilis.
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. This compound has anti-inflammatory activity that reduces the protein expression of MMP-9, IL-1β, TNF-α and TGF-β. It downregulates Smad3 and p38 signaling pathways.
S0777	Isuzinaxib (APX-115 free base)	Isuzinaxib (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. This compound significantly suppresses the expression of inflammatory molecules including MCP-1/CCL2, IL-6, and TNFα in the diabetic kidney.
E3633	Ginger Extract	Ginger Extract is extracted from Zingiber officinale Roscoe, which has antioxidant potential and regulates STAT6 and TNF- α pathways.
E3634	Ginger Extract(1%)	Ginger Extract(1%) is extracted from Zingiber officinale Roscoe, which has antioxidant potential and regulates STAT6 and TNF- α pathways.
S3293	Gardenoside	Gardenoside is a natural compound extracted from Gardenia fruits, with hepatoprotective properties. It inhibits TNF-α, IL-1β, IL-6 and NFκB activation. This compound also has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis. It suppresses the pain in rats model of chronic constriction injury by regulating the P2X3 and P2X7 receptors.
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). This compound 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.
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. It 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. This compound suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2.
S5851	4'-Methoxychalcone	4'-Methoxychalcone, found in citrus, is chalcone derivative that has shown diverse pharmacological properties, including anti-tumor and anti-inflammatory activities. This compound significantly enhanced adipocyte differentiation, in part, by its potent effects on PPARγ activation and by its reverse effect on TNF-α.
S1273	Amarogentin	Amarogentin (AG), a secoiridoid glycoside mainly extracted from Swertia and Gentiana roots, exhibits anti-oxidative, anti-tumour, and anti-diabetic activities. This compound is an agonist for the bitter taste receptor TAS2R1 and inhibits in LAD-2 cells substance P-induced production of newly synthesized TNF-α. It induces apoptosis in human gastric cancer cells (SNU-16) through G2/M cell cycle arrest and PI3K/Akt signalling pathway. This chemical interacts with the α2 subunit of AMP-activated protein kinase (AMPK) and activates the trimeric kinase with EC50 of 277 pM.
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. This compound 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. This compound has potent neuroprotective effects and has anti-inflammation, antioxidant, and antisepsis properties. It 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. This compound potentially ameliorates NAFLD (Non-alcoholic fatty liver disease) by activating AMPK pathways.