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. |
-
Redox Biol, 2024, 70:103072
-
J Exp Clin Cancer Res, 2023, 42(1):236
-
J Exp Clin Cancer Res, 2023, 42(1):236
|
|
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
|
|
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. |
-
iScience, 2024, 27(3):109125
-
Chem Biol Interact, 2023, 381:110574
-
Cancer Med, 2023, 10.1002/cam4.6508
|
|
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. |
-
Adv Sci (Weinh), 2023, 10(25):e2301059
-
Clin Transl Med, 2023, 13(8):e1364
-
Clin Transl Med, 2023, 13(8):e1364
|
|
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. |
-
Biology (Basel), 2023, 12(2)318
-
bioRxiv, 2023, 10.1101/2023.12.15.571909
-
Small, 2022, 18(4):e2103552
|
|
S6414 |
Apilimod
|
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. |
-
Nucleic Acids Res, 2023, 51(4):1583-1599
-
Front Immunol, 2023, 14:1128700
-
NPJ Digit Med, 2022, 5(1):18
|
|
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.
|
-
Cancer Commun -Lond), 2023, 43(10):1117-1142
-
Microbiol Res, 2023, 276:127480
-
Pathol Oncol Res, 2022, 28:1610273
|
|
S8301 |
Ossirene (AS101)
|
Ossirene (AS101), a potent in vitro and in vivo immunomodulator, is a novel inhibitor of IL-1beta converting enzyme. |
-
Cell Rep, 2023, 42(7):112660
-
Cells, 2022, 11(24)4013
-
Syst Biol Reprod Med, 2022, 1-15
|
|
S4267 |
Diacerein
|
Diacerein is an inhibitor of pro-inflammatory cytokine Interleukin-1B (IL-1B) production, prescribed for osteoarthritis and chronic inflammatory arthritis. |
-
Oral Dis, 2022, 10.1111/odi.14294
-
Free Radic Biol Med, 2021, 165:171-183
-
Cancer Res, 2020, canres.530.2020
|
|
S1733 |
Methylprednisolone
|
Methylprednisolone 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
|
|
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. |
-
Virulence, 2023, 14(1):2249779
-
Virulence, 2023, 14(1):2249779
|
|
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
|
|
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. |
-
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. |
-
J Exp Clin Cancer Res, 2022, 41(1):36
-
Free Radic Biol Med, 2021, 168:25-43
|
|
S3292 |
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. |
-
Front Cell Infect Microbiol, 2023, 13:1128000
-
Front Pharmacol, 2021, 12:656697
|
|
S9668 |
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. |
-
Exp Mol Med, 2024, 56(2):408-421.
-
EMBO J, 2024, 43(5):780-805.
-
Cell Chem Biol, 2021, S2451-9456(21)00303-2
|
|
S8879 |
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. |
-
Nat Commun, 2024, 15(1):1718
-
Nat Commun, 2024, 15(1):1337
-
Front Immunol, 2023, 10.3389/fimmu.2023.1263926
|
|
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. |
-
Biomedicine & Pharmacotherapy, 2023, 114638
-
Biomed Pharmacother, 2023, 162:114638
|
|
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
|
|
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. |
-
Cell Rep, 2023, 42(7):112696
|
|
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. |
-
Front Immunol, 2022, 13:863034
|
|
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
|
|
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
|
|
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). |
-
Plant Physiology, 2012, 81–94
|
|
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
|
|
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
|
|
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
|
|
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
|
|
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. |
-
Br J Cancer, 2021, 10.1038/s41416-021-01631-3
|
|
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. |
|
|
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. |
|
|
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.
|
|
|
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. |
|
|
E3568 |
Natural indigo Extract
|
Natural Indigo Extract is extracted from Polygonum tinctorium, which suppress sodium dextran sulfate-induced colitis through interleukin-10-related pathway. |
|
|
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. |
|
|
E2502 |
Tamarixetin
|
Tamarixetin (4'-O-Methyl Quercetin) is a natural flavonoid derivative of quercetin and has superior anti-inflammatory properties in bacterial sepsis by increasing the population of IL-10-secreting immune cells. |
|
|
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. 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. |
|
|
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. |
|
|
A2038 |
Dupilumab (anti-IL-4Rα)
|
Dupilumab (anti-IL-4Rα) is a fully human anti–interleukin-4 receptor α monoclonal antibody that inhibits both interleukin-4 (IL-4) and interleukin-13 (IL-13) signaling through blockade of the shared IL-4α subunit. |
|
|
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. |
|
|
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. |
|
|
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. |
|
|
E1383New |
Cp2-SO4
|
Cp2-SO4 is a phenylalanine derivative which reverses interleukin 4 induced 1 (IL4I1)-dependet inhibition of T-cell proliferation with Ki of 21.2 µM. |
|
|
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.
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|
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. |
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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. |
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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. |
|
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A2030 |
Siltuximab (anti-IL-6)
|
Siltuximab (anti-IL-6) (CNTO 328) is a human-mouse chimeric monoclonal antibody that binds human interleukin-6 (IL-6). |
|
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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. |
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A2038 |
Dupilumab (anti-IL-4Rα)
|
Dupilumab (anti-IL-4Rα) is a fully human anti–interleukin-4 receptor α monoclonal antibody that inhibits both interleukin-4 (IL-4) and interleukin-13 (IL-13) signaling through blockade of the shared IL-4α subunit. |
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A2030 |
Siltuximab (anti-IL-6)
|
Siltuximab (anti-IL-6) (CNTO 328) is a human-mouse chimeric monoclonal antibody that binds human interleukin-6 (IL-6). |
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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. |
- Redox Biol, 2024, 70:103072
- J Exp Clin Cancer Res, 2023, 42(1):236
- J Exp Clin Cancer Res, 2023, 42(1):236
|
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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
|
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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. |
- Adv Sci (Weinh), 2023, 10(25):e2301059
- Clin Transl Med, 2023, 13(8):e1364
- Clin Transl Med, 2023, 13(8):e1364
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S6414 |
Apilimod
|
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. |
- Nucleic Acids Res, 2023, 51(4):1583-1599
- Front Immunol, 2023, 14:1128700
- NPJ Digit Med, 2022, 5(1):18
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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.
|
- Cancer Commun -Lond), 2023, 43(10):1117-1142
- Microbiol Res, 2023, 276:127480
- Pathol Oncol Res, 2022, 28:1610273
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S8301 |
Ossirene (AS101)
|
Ossirene (AS101), a potent in vitro and in vivo immunomodulator, is a novel inhibitor of IL-1beta converting enzyme. |
- Cell Rep, 2023, 42(7):112660
- Cells, 2022, 11(24)4013
- Syst Biol Reprod Med, 2022, 1-15
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S4267 |
Diacerein
|
Diacerein is an inhibitor of pro-inflammatory cytokine Interleukin-1B (IL-1B) production, prescribed for osteoarthritis and chronic inflammatory arthritis. |
- Oral Dis, 2022, 10.1111/odi.14294
- Free Radic Biol Med, 2021, 165:171-183
- Cancer Res, 2020, canres.530.2020
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S1733 |
Methylprednisolone
|
Methylprednisolone 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
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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. |
- Virulence, 2023, 14(1):2249779
- Virulence, 2023, 14(1):2249779
|
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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
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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. |
- Stem Cell Reports, 2022, 17(2):397-412
- Hum Mol Genet, 2021, 29(22):3589-3605
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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. |
- J Exp Clin Cancer Res, 2022, 41(1):36
- Free Radic Biol Med, 2021, 168:25-43
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S3292 |
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. |
- Front Cell Infect Microbiol, 2023, 13:1128000
- Front Pharmacol, 2021, 12:656697
|
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S9668 |
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. |
- Exp Mol Med, 2024, 56(2):408-421.
- EMBO J, 2024, 43(5):780-805.
- Cell Chem Biol, 2021, S2451-9456(21)00303-2
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S8879 |
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. |
- Nat Commun, 2024, 15(1):1718
- Nat Commun, 2024, 15(1):1337
- Front Immunol, 2023, 10.3389/fimmu.2023.1263926
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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. |
- Cell Rep, 2023, 42(7):112696
|
|
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. |
- Front Immunol, 2022, 13:863034
|
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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
|
|
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). |
- Plant Physiology, 2012, 81–94
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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
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|
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
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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
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|
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
|
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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
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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. |
- Br J Cancer, 2021, 10.1038/s41416-021-01631-3
|
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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
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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). |
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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). |
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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). |
|
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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. |
|
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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. |
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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.
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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. |
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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. |
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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. |
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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. 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. |
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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. |
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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. |
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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. |
|
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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. |
|
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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. |
|
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E1153 |
LMT-28
|
LMT-28 is a novel synthetic interleukin-6 (IL-6) inhibitor that functions through direct binding to gp130. |
|
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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. |
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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. |
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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. |
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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. |
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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
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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. |
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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. |
|
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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. |
|
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E1383New |
Cp2-SO4
|
Cp2-SO4 is a phenylalanine derivative which reverses interleukin 4 induced 1 (IL4I1)-dependet inhibition of T-cell proliferation with Ki of 21.2 µM. |
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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. |
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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. |
|
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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. |
|
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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.
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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. |
|
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S0228 |
SU 5201
|
SU 5201 (NSC 247030) is an interleukin-2 (IL-2) inhibitor. |
|
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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. |
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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. |
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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. |
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