Interleukins

Inhibitory Selectivity

Interleukins Products

Catalog No.	Information	Product Use Citations	Product Validations
S1189	Aprepitant Aprepitant (MK-0869, L-754030) 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.	Nat Commun, 2020, 29;11(1):2673 Neuron, 2019, 103(3):432-444 Cell Syst, 2019, 8(2):97-108	HepT1, HepG2, and HuH6 cells were treated with increasing doses of aprepitant or SP [100 nM] and Western blot analysis was performed for the apoptotic markers PARP, Caspase-3, and BID.
S1733	Methylprednisolone Methylprednisolone (NSC-19987) 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.	Drug Test Anal, 2020, 10.1002/dta.2917 Nat Med, 2017, 23(4):424-428 Trop J Pharm Res, 2014, 13 (1): 53-59	Motor disturbances of the rat hindlimbs after SCI, using an inclined plane test. Key: ◇ = PBS group; ■ = Sal B group; ▲ = methylprednisolone group.
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).
S3590^New	Triolein Triolein is an inhibitor of metalloproteinase-1 (MMP-1) and reduces both the expression of IL-6 and ROS generation in irradiated keratinocytes.
S3312^New	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).
S6898^New	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.
S3261^New	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.
S3299^New	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.
S3304^New	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.
S9668^New	PKR-IN-C16 PKR-IN-C16 (imoxin, 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.
S9660^New	Remibrutinib (LOU064) Remibrutinib (LOU064) 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.
S3293^New	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.
S3292^New	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. Falnidamol is a pyrimido-pyrimidine compound with anti-cancer activity.
S8966^New	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.	Nat Commun, 2020, 11(1):5079 Am J Cancer Res, 2020, 10(12):4325-4341 J Virol, 2020, JVI.02107-20
S8879^New	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.
S0787^New	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.	Free Radic Biol Med, 2021, 168:25-43
S0785^New	Apilimod mesylate Apilimod mesylate (STA-5326 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.	Hum Mol Genet, 2021, 29(22):3589-3605
S0781^New	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.
S0777^New	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.
S0752^New	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.
S0771^New	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).
S0437^New	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.
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).
S8301	AS101 AS101, a potent in vitro and in vivo immunomodulator, is a novel inhibitor of IL-1beta converting enzyme.	J Immunol, 2020, 205(10):2694-2706 World J Gastroenterol, 2020, 26(41):6361-6377 Cancer Lett, 2019, 10.1016/j.canlet.2019.07.016
S4267	Diacerein Diacerein is an inhibitor of pro-inflammatory cytokine Interleukin-1B (IL-1B) production, prescribed for osteoarthritis and chronic inflammatory arthritis.	Free Radic Biol Med, 2021, 165:171-183 Cancer Res, 2020, canres.530.2020 Free Radic Biol Med, 2020, 148:140-150	f, Intra-TG injection of IL-1β inhibitor, Diacerein 10 days after pIONL alleviated pIONL-induced mechanical allodynia from 1 to 6 h. P < 0.05, **P < 0.001. Two-way repeated measures ANOVA followed by Bonferroni test.
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.
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.	Cancer Res, 2020, canres.530.2020 J Neuroinflammation, 2020, 17(1):364
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.	Onco Targets Ther, 2021, 14:379-392 Onco Targets Ther, 2020, 12;13:2215-2224 Transl Oncol, 2020, 13(10):100825	Interleukin-6 (IL-6) secretion was inhibited by B7‐H4 silence through JAK2/signal transducer and activator of transcription 3 (STAT3) inactivation. (a) ELISA results showed that, compared with cells pretreated with control shRNA, B7‐H4 silence led to reduction of IL‐6 secretion. However, compared with cells pretreated with control shRNA and FLLL32, IL‐6 secretion in Eca109, TE1, and TE13 esophageal squamous cell carcinoma cells pretreated with B7‐H4 shRNA and FLLL32 was not significantly affected.
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.
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).
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.	FASEB J, 2021, 35(4):e21485 Front Pharmacol, 2021, 12:626949 Redox Biol, 2020, 37:101761
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.
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
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).	J Pharm Pharmacol, 2019, 71(11):1706-1713
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.
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.	Theranostics, 2019, 9(18):5332-5346
S6414	Apilimod Apilimod (STA-5326) 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.	Hum Mol Genet, 2021, 29(22):3589-3605 Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19
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.
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.
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) is an antithyroid agent. Methylthiouracil suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2.
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.
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.
S0228	SU 5201 SU 5201 (NSC 247030) is an interleukin-2 (IL-2) inhibitor.
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.
S1709	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.	J Steroid Biochem Mol Biol, 2021, 209:105826 Theranostics, 2020, 10(4):1833-1848 Life Sci, 2020, 1;248:117449
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.
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.
S6850^New	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).
S0826^New	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.
S8133	Resiquimod 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.	Pharmaceutics, 2021, 13(3)365 Vaccines (Basel), 2020, 15;8(2):E186 Nat Commun, 2020, 11(1):3521
S4842^New	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.
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.
S6579	RCGD423 RCGD-423 is a modulator of Glycoprotein 130 (gp130, IL6ST, IL6-beta, CD130) signalling that regulates cartilage growth and differentiation.
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

Catalog No.	Information	Product Use Citations	Product Validations
S1189	Aprepitant Aprepitant (MK-0869, L-754030) 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.	Nat Commun, 2020, 29;11(1):2673 Neuron, 2019, 103(3):432-444 Cell Syst, 2019, 8(2):97-108	HepT1, HepG2, and HuH6 cells were treated with increasing doses of aprepitant or SP [100 nM] and Western blot analysis was performed for the apoptotic markers PARP, Caspase-3, and BID.
S1733	Methylprednisolone Methylprednisolone (NSC-19987) 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.	Drug Test Anal, 2020, 10.1002/dta.2917 Nat Med, 2017, 23(4):424-428 Trop J Pharm Res, 2014, 13 (1): 53-59	Motor disturbances of the rat hindlimbs after SCI, using an inclined plane test. Key: ◇ = PBS group; ■ = Sal B group; ▲ = methylprednisolone group.
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).
S3590^New	Triolein Triolein is an inhibitor of metalloproteinase-1 (MMP-1) and reduces both the expression of IL-6 and ROS generation in irradiated keratinocytes.
S3312^New	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).
S6898^New	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.
S3261^New	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.
S3299^New	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.
S3304^New	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.
S9668^New	PKR-IN-C16 PKR-IN-C16 (imoxin, 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.
S9660^New	Remibrutinib (LOU064) Remibrutinib (LOU064) 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.
S3293^New	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.
S3292^New	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. Falnidamol is a pyrimido-pyrimidine compound with anti-cancer activity.
S8966^New	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.	Nat Commun, 2020, 11(1):5079 Am J Cancer Res, 2020, 10(12):4325-4341 J Virol, 2020, JVI.02107-20
S8879^New	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.
S0787^New	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.	Free Radic Biol Med, 2021, 168:25-43
S0785^New	Apilimod mesylate Apilimod mesylate (STA-5326 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.	Hum Mol Genet, 2021, 29(22):3589-3605
S0781^New	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.
S0777^New	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.
S0752^New	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.
S0771^New	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).
S0437^New	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.
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).
S8301	AS101 AS101, a potent in vitro and in vivo immunomodulator, is a novel inhibitor of IL-1beta converting enzyme.	J Immunol, 2020, 205(10):2694-2706 World J Gastroenterol, 2020, 26(41):6361-6377 Cancer Lett, 2019, 10.1016/j.canlet.2019.07.016
S4267	Diacerein Diacerein is an inhibitor of pro-inflammatory cytokine Interleukin-1B (IL-1B) production, prescribed for osteoarthritis and chronic inflammatory arthritis.	Free Radic Biol Med, 2021, 165:171-183 Cancer Res, 2020, canres.530.2020 Free Radic Biol Med, 2020, 148:140-150	f, Intra-TG injection of IL-1β inhibitor, Diacerein 10 days after pIONL alleviated pIONL-induced mechanical allodynia from 1 to 6 h. P < 0.05, **P < 0.001. Two-way repeated measures ANOVA followed by Bonferroni test.
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.
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.	Cancer Res, 2020, canres.530.2020 J Neuroinflammation, 2020, 17(1):364
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.	Onco Targets Ther, 2021, 14:379-392 Onco Targets Ther, 2020, 12;13:2215-2224 Transl Oncol, 2020, 13(10):100825	Interleukin-6 (IL-6) secretion was inhibited by B7‐H4 silence through JAK2/signal transducer and activator of transcription 3 (STAT3) inactivation. (a) ELISA results showed that, compared with cells pretreated with control shRNA, B7‐H4 silence led to reduction of IL‐6 secretion. However, compared with cells pretreated with control shRNA and FLLL32, IL‐6 secretion in Eca109, TE1, and TE13 esophageal squamous cell carcinoma cells pretreated with B7‐H4 shRNA and FLLL32 was not significantly affected.
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.
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).
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.	FASEB J, 2021, 35(4):e21485 Front Pharmacol, 2021, 12:626949 Redox Biol, 2020, 37:101761
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.
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
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).	J Pharm Pharmacol, 2019, 71(11):1706-1713
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.
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.	Theranostics, 2019, 9(18):5332-5346
S6414	Apilimod Apilimod (STA-5326) 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.	Hum Mol Genet, 2021, 29(22):3589-3605 Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19
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.
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.
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) is an antithyroid agent. Methylthiouracil suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2.
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.
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.
S0228	SU 5201 SU 5201 (NSC 247030) is an interleukin-2 (IL-2) inhibitor.
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.

Catalog No.	Information	Product Use Citations	Product Validations
S1709	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.	J Steroid Biochem Mol Biol, 2021, 209:105826 Theranostics, 2020, 10(4):1833-1848 Life Sci, 2020, 1;248:117449
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.

Catalog No.

Information

Product Use Citations

Product Validations

S1709

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.

J Steroid Biochem Mol Biol, 2021, 209:105826

Theranostics, 2020, 10(4):1833-1848

Life Sci, 2020, 1;248:117449

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.

Catalog No.	Information	Product Use Citations	Product Validations
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.
S6850^New	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).
S0826^New	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.

Catalog No.

Information

Product Use Citations

Product Validations

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.

S6850^New

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).

S0826^New

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.

Catalog No.	Information	Product Use Citations	Product Validations
S8133	Resiquimod 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.	Pharmaceutics, 2021, 13(3)365 Vaccines (Basel), 2020, 15;8(2):E186 Nat Commun, 2020, 11(1):3521

Catalog No.

Information

Product Use Citations

Product Validations

S8133

Resiquimod

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.

Pharmaceutics, 2021, 13(3)365

Vaccines (Basel), 2020, 15;8(2):E186

Nat Commun, 2020, 11(1):3521

Catalog No.	Information	Product Use Citations
S4842^New	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.
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.
S6579	RCGD423 RCGD-423 is a modulator of Glycoprotein 130 (gp130, IL6ST, IL6-beta, CD130) signalling that regulates cartilage growth and differentiation.
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

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