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TNF-α (31-45), human is a potent NF-kB pathway activator. TNF-αis a proinflammatory cytokine that induces necrosis or apoptosis. TNF alpha stimulates NF-κB pathway via TNFR2 promotes cancer growth, invasion, and metastasis .
TNF-α (31-45), human TFA is a potent NF-kB pathway activator. TNF-αis a proinflammatory cytokine that induces necrosis or apoptosis. TNF alpha stimulates NF-κB pathway via TNFR2 promotes cancer growth, invasion, and metastasis .
TNF-α-IN-14 is a potent and selective TNFα inhibitor with an IC50 value of 1.1 µM. TNF-α-IN-14 shows antiinflammatory properties (WO2001072735A2; compound 12) .
TNF-α-IN-11 (Compound 10) is a TNF-α inhibitor with a KD value of 12.06 μM. TNF-α-IN-11 binds to TNF-α and blocks the activation of TNF-α-trigged caspase and NF-κB signaling pathway. TNF-α-IN-11 inhibits the phosphorylation of IκBα, as well as the nuclear translocation of NF κB p65. TNF-α-IN-11 can be used for research of TNF-α-mediated autoimmune diseases .
TNF-α-IN-2 is a potent and orally active inhibitor of tumor necrosis factor alpha (TNFα), with an IC50 of 25 nM in the HTRF assay. TNF-α-IN-2 distorts the TNFα trimer upon binding, leading to aberrant signaling when the trimer binds to TNFR1. TNF-α-IN-2 can be used for the research of rheumatoid arthritis .
TNF-α-IN-8 (compound I-42) is a TNF-α inhibitor. TNF-α-IN-8 is an isoindole-imide compound. TNF-α-IN-8 can be used for the research of cancer, heart disease, osteoporosis, inflammatory, allergic and autoimmune diseases . TNF-α-IN-8 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
PKC-IN-4 (compound 7l) is a potent and orally active aPKC inhibitor with an IC50 of 0.52 µM. PKC-IN-4 inhibits TNF-α induced NF-κB activity in vitro. PKC-IN-4 blocks VEGF- and TNFα-induced permeability across the retinal vasculature .
Infliximab (Avakine) is a chimeric monoclonal IgG1 antibody that specifically binds to TNF-α. Infliximab prevents the interaction of TNF-α with TNF-α receptor (TNFR1 and TNFR2). Infliximab has the potential for autoimmune, chronic inflammatory diseases and diabetic neuropathy research .
Benpyrine is a highly specific and orally active TNF-α inhibitor with a KD value of 82.1 μM. Benpyrine tightly binds to TNF-α and blocks its interaction with TNFR1, with an IC50 value of 0.109 µM. Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research .
(Rac)-Benpyrine, a racemate of Benpyrine, is a potent and orally active TNF-α inhibitor. (Rac)-Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research .
Aloeresin G is a chromone glycoside that can be isolated from Aloe. Aloeresin G has a weak inhibitory effect on TNFα-induced NF-κB transcriptional activity, with an IC 50 value of 40.02 μM .
DBM 1285 dihydrochloride is an orally active TNF-α production inhibitor with anti-inflammatory effects. DBM 1285 dihydrochloride inhibits Lipopolysaccharide (LPS)-induced TNF-α secretion in various cells of macrophage/monocyte lineage .
(R)-Benpyrine is the isomer of Benpyrine (HY-133807), and can be used as an experimental control. Benpyrine is a highly specific and orally active TNF-α inhibitor with a KD value of 82.1 μM. Benpyrine tightly binds to TNF-α and blocks its interaction with TNFR1, with an IC50 value of 0.109 μM. Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research .
SPD304 is a selective TNF-α inhibitor, which promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor. SPD304 has an IC50 of 22 µM for inhibiting in vitro TNF receptor 1 (TNFR1) binding to TNF-α .
SPD304 dihydrochloride is a selective TNF-α inhibitor, which promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor. SPD304 has an IC50 of 22 µM for inhibiting in vitro TNF receptor 1 (TNFR1) binding to TNF-α .
HS271 is a highly potent, orally active and selective IRAK4 inhibitor, with an IC50 of 7.2 μM. HS271 exhibits superior enzymatic and cellular activities, as well as excellent pharmacokinetic properties .
UTL-5g (GBL-5g), an anti-inflammatory TNF-α inhibitor, has chemoprotective and liver radioprotective effects. UTL-5g lowers hepatotoxicity, nephrotoxicity, and myelotoxicity induced by Cisplatin through TNF-α inhibition among other factors .
Licarin A ((+)-Licarin A), a neolignan, significantly and dose-dependently reduces TNF-α production (IC50=12.6 μM) in dinitrophenyl-human serum albumin (DNP-HSA)-stimulated RBL-2H3 cells. Anti-allergic effects. Licarin A reduces TNF-α and PGD2 production, and COX-2 expression .
Geraniin is a TNF-α releasing inhibitor with numerous activities including anticancer, anti-inflammatory, and anti-hyperglycemic activities, with an IC50 of 43 μM.
Myrtenal ((±)-Myrtenal) is a monoterpene that acts as an antineoplastic agent. Myrtenal inhibits liver cancer by preventing DEN-PB-induced upregulation of TNF-α protein expression.
Gnetifolin E is a resveratrol trimer derivative that can be isolated from Gnetum brunonianum. Gnetifolin E has anti-inflammatory activity, and inhibits TNF-α .
Boc-D-FMK is a cell-permeable, irreversible and broad spectrum caspase inhibitor. Boc-D-FMK inhibits apoptosis stimulated by TNF-α with an IC50 of 39 µM.
Hispidol ((Z)-Hispidol) is a potential therapeutic for inflammatory bowel disease; inhibits TNF-α induced adhesion of monocytes to colon epithelial cells with an IC50 of 0.50 µM.
Episappanol is a natural compound isolated from Caesalpinia sappan heartwood with anti-inflammatory activity. Episappanol significantly inhibits the IL-6 and TNF-α secretion .
Gnetumontanin B is a stilbenoid that can be found in Gnetum montanum f. megalocarpum. Gnetumontanin B inhibits TNF-α production with an IC50 value of 1.49 µM .
Glucocorticoid receptor agonist-4 (Compound Preparation 5) is a glucocorticoid receptor agonist that can be conjugated to TNF-α antibodies for the study of autoimmune and inflammatory diseases .
LEESGGGLVQPGGSMK, a proteolysis peptide, is a component of Infliximab. LEESGGGLVQPGGSMK can be used for quantitative analysis of Infliximab. Infliximab is a chimeric monoclonal IgG1 antibody that specifically binds to TNF-α .
LEESGGGLVQPGGSMK acetate, a proteolysis peptide, is a component of Infliximab. LEESGGGLVQPGGSMK acetate can be used for quantitative analysis of Infliximab. Infliximab is a chimeric monoclonal IgG1 antibody that specifically binds to TNF-α .
Teuclatriol is an NF-κB inhibitor can be isolated from salvia mirzayanii, has anti-inflammatory effects. Teuclatriol inhibits TNF-α secretion in a dose-dependent manner .
Ataquimast is a COX-2 inhibitor that inhibits the release of leukotrienes, TNF-α and GM-CSF. Ataquimast can be used in the study of advanced receptor-positive breast cancer .
Deoxyandrographolide suppresses LPS induced increase in mRNA levels of iNOS as well as production of proinflammatory mediators TNF-α and IL-6. Deoxyandrographolide potentiates NGF-induced neurite outgrowth .
CDC801 is a potent and orally active phosphodiesterase 4 (PDE4) and tumor necrosis factor-α (TNF-α) inhibitor with IC50 of 1.1 μM and 2.5 μM, respectively.
LEESGGGLVQPGGSMK TFA, a proteolysis peptide, is a component of Infliximab. LEESGGGLVQPGGSMK TFA can be used for quantitative analysis of Infliximab. Infliximab is a chimeric monoclonal IgG1 antibody that specifically binds to TNF-α .
Sinulatumolin E (compound 6), a terpenoid, displays significant TNF-α inhibitory activity with an IC50 of 3.6 μM. Sinulatumolin E (compound 6) exhibits anti-inflammatory activity .
Necrostatin 2 is a potent necroptosis inhibitor. EC50 for inhibition of necroptosis in FADD-deficient Jurkat T cells treated with TNF-α is 0.05 μM.
Necrostatin 2 is also a RIPK1 inhibitor.
GSK583 is a highly potent, orally active and selective inhibitor of RIP2 Kinase, with IC50 of 5 nM. GSK583 inhibits both TNF-α and IL-6 production with an IC50 value of 200 nM.
Homoplantaginin is a flavonoid from a traditional Chinese medicine Salvia plebeia with antiinflammatory and antioxidant properties. Homoplantaginin could inhibit TNF-α and IL-6 mRNA expression, IKKβ and NF-κB phosphorylation.
SIRT1 activator 3 is a potent activator of Sirt1 and suppresses TNF-α in a dose-dependent manner. SIRT1 activator 3 has the potential for anti-obesity or anti-diabetic researches .
Ataquimast free base is a COX-2 inhibitor that inhibits the release of leukotrienes, TNF-α and GM-CSF. Ataquimast free base can be used in the study of advanced receptor-positive breast cancer .
Oleaside A is a polar cardenolide monoglycoside isolated from Nerium oleander, inhibits the induction of ICAM-1 induced by IL-1α and TNF-α, and has anti-tumor activity .
QNZ (EVP4593) shows strong inhibitory effects on NF-κB transcriptional activation and TNF-α production with IC50s of 11 and 7 nM, respectively. QNZ (EVP4593) is a neuroprotective inhibitor of SOC channel.
IW927 is a potent small molecule antagonist that blocks the binding of TNF-α to TNFRc1 with an IC50 value of 50 nM and disrupts TNFα-induced IκB phosphorylation with an IC50 value of 600 nM .
Sibiricine (Compound 8) is an isoquinoline alkaloid derived from the medicinal plant Corydalis crispa. Sibiricine has significant anti-inflammatory activity on TNF-α production by LPS-activated THP-1 cells .
β-Anhydroicaritin is isolated from Boswellia carterii Birdware, has important biological and pharmacological effects, such as antiosteoporosis, estrogen regulation and antitumor properties . β-Anhydroicaritin ameliorates the degradation of periodontal tissue and inhibits the synthesis and secretion of TNF-α and MMP-3 in diabetic rats . β-Anhydroicaritin decreases the overproduction of NO, IL-10, TNF-α, MCP-1 and IL-6 in inperitonitis mice. β-Anhydroicaritin inhibits the elevation of intracellular Ca 2+, and markedly decreases iNOS protein expression .
Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM .
Ginsenoside Rc, one of major Ginsenosides from Panax ginseng, enhances GABA receptorA (GABAA)-mediated ion channel currents (IGABA). Ginsenoside Rc inhibits the expression of TNF-α and IL-1β.
RIP2 Kinase Inhibitor 4 is a potent and selective RIPK2 PROTAC. RIP2 Kinase Inhibitor 4 effectively degrades RIPK2 (pIC50 of 8) and inhibits the release of related TNF-α .
Necroptosis-IN-3 (Compound 69) is a necroptosis inhibitor that inhibits TNF-α induced necroptosis . Necroptosis-IN-3 (Compound STX1638) also inhibits 11β-HSD1 .
Methylenedihydrotanshinquinone is a natural product that can be isolated from the dried root of S. miltiorrhiza. Methylenedihydrotanshinquinone has anti-inflammatory effect by inhibiting expression of TNF-α, IL-1β, and IL-8 .
3-O-Methylviridicatin is an inhibitor of TNF-α.3-O-Methylviridicatin inhibits TNF-a synthesis instead of the activity. 3-O-Methylviridicatin can be used in study anti-in?ammatory agents .
Myrcene (β-Myrcene) is a type of aromatic compound that inhibits TNFα and NF-κB activity. Myrcene has anti-invasive action, inhibits cell cycle, and leads to cancer cell apoptosis. Myrcene has strong blood protection effect, anti-inflammation, and anti-inflammatory activity.
Golimumab (CNTO-148) is a potent human IgG1 TNFα antagonist monoclonal antibody. Golimumab has anti-inflammation activitity and inhibits IL-6 and IL-1β production. Golimumab acts via targeting and neutralizing TNF to prevent inflammation and destruction of cartilage and bone. Golimumab has the anticancer activity and induces cell apoptosis. Golimumab can be used for rheumatoid arthritis, Crohn's disease and cancer research .
TLR4 agonist-1 (TEA) (compound 17a) is a potent agonist of Toll-like Receptor 4 (TLR4), and induces the generation of MIP-1β in RAW 264.7 and MM6 cells .
Glucocorticoid receptor agonist-4 Ala-Ala-Mal (Compound Preparation 9) is an anti-human TNFα antibody-glucocorticoid receptor agonist (GC) conjugate. Glucocorticoid receptor agonist-4 Ala-Ala-Mal can be used in the study of autoimmune and inflammatory diseases .
Glucocorticoid receptor agonist-3 Ala-Ala-Mal (Compound Preparation 8) is an anti-human TNFα antibody-glucocorticoid receptor agonist (GC) conjugate. Glucocorticoid receptor agonist-3 Ala-Ala-Mal can be used in the study of autoimmune and inflammatory diseases .
BIZ 114 (Example 11) is a fatty acid derivative and potent inhibits the TNF-α activated NF-κΒ pathway. BIZ 114 has the potential to prevent and / or treat ophthalmic disorders such as retinal degenerative disorders and ocular inflammatory diseases .
D-Trimannuronic acid, an alginate oligomer is extracted from seaweed. D-Trimannuronic acid can induce TNF‐α secretion by mouse macrophage cell lines. D-Trimannuronic acid can be used for the research of pain and vascular dementia .
Tengonermin (ARENEGYR) is a vascular-targeting agent consisting of the human Tumour Necrosis Factor-α (TNF-α) conjugated with the CNGRCG peptide. Tengonermin increases penetration of intratumoral chemotherapy and T-cell infiltration by modifying the tumour microenvironment .
Taurohyodeoxycholic acid (THDCA) sodium is the taurine-conjugated form of the secondary bile acid hyodeoxycholic acid. Taurohyodeoxycholic acid can also reduce the activity and expression of myeloperoxidase TNF-α and IL-6, as well as colonic damage in TNBS-induced ulcerative colitis mouse model.
Linderaspirone A is a natural compound that can be isolated from the roots of Lindera aggregate. Linderaspirone A shows significant inhibitory effects on the production of prostaglandin E2 (PGE2),TNF-α, and IL-6 .
Soyasapogenol A, a triterpene compound, isolated from soybean. Soyasapogenol A directly prevents apoptosis of hepatocytes, and secondly, inhibits the elevation of plasma TNF-α, which consequently results in the prevention of liver damage in the Concanavalin A-induced hepatitis model .
Lupeol acetate, a derivative of Lupeol, suppresses the progression of rheumatoid arthritis (RA) by inhibiting the activation of macrophages and osteoclastogenesis through downregulations of TNF-α, IL-1β, MCP-1, COX-2, VEGF and granzyme B .
HDMAPP triammonium is a potent phosphoantigen in the ammonium form and the pyrophosphate form of (E)-HDMAPP. HDMAPP is also a potent activator of γδ T cells and can induce T cell stimulation in vitro (EC50=0.39 nM, TNF-α) .
IMD-0354 (IKK2 Inhibitor V) is a selective IKKβ inhibitor which inhibits NF-κB activity . IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC50 of 1.2 uM .
Undecane has anti-allergic and anti-inflammatory activities on sensitized rat basophilic leukemia (RBL-2H3) mast cells and HaCaT keratinocytes. In sensitized mast cells, Undecane inhibits degranulation and the secretion of histamine and TNF-α[
Certolizumab pegol (Certolizumab) is a recombinant, polyethylene glycolylated, antigen-binding fragment of a humanized monoclonal antibody that selectively targets and neutralizes tumour necrosis factor-α (TNF-α). Certolizumab pegol can be used for rheumatoid arthritis and Crohn disease research .
Homouridine, is an uridine analogue. Homouridine serves as an intermediate to prepare MMP-2 inhibitor (compund I, IC50=150 μM). Homouridine derivate (compund I) also inhibits TNF-α binding to TNF-αR1 .
Anti-inflammatory agent 42 (Compound 10j) is an anti-inflammatory agent. Anti-inflammatory agent 42 shows excellent inhibition on the expression of TNF-α and IL-6 in LPS (HY-D1056)-stimulated macrophages .
Apremilast-d5 is a deuterium labeled Apremilast. Apremilast is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM[1].
Resiquimod-d5 is deuterium labeled Resiquimod. Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α[1][2].
PDE4-IN-10 (compound 7a) is a potent PDE4 inhibitor, with an IC50 of 7.01 μM for PDE4B. PDE4-IN-10 shows selectivity, microsomal stability, inhibition of TNF-α and no major toxicities in vitro .
Vialinin A (Terrestrin A) is a p-terphenyl compound with antioxidant properties . Vialinin A is a potent inhibitor of TNF-α, USP4, USP5, and sentrin/SUMO-specific protease 1 (SENP1). Vialinin A (Terrestrin A) can be used for autoimmune diseases and cancer research .
Ginsenoside Rh1 (Standard) is the analytical standard of Ginsenoside Rh1. This product is intended for research and analytical applications. Ginsenoside Rh1 (Prosapogenin A2) inhibits the expression of PPAR-γ, TNF-α, IL-6, and IL-1β.
(S)-(+)-Rolipram ((+)-Rolipram) is a cyclic AMP(cAMP)-specific phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 1100 nM. (S)-(+)-Rolipram can suppresse tumor necrosis factor-alpha (TNFα) production by human mononuclear cells .
MK2-IN-3 is a potent and selective inhibitor of MAPKAP-K2 (MK-2), with an IC50 of 8.5 nM. MK2-IN-3 shows selectivity for MK-2 over MK-3, MK-5, ERK2, MNK1, p38a (IC50s=0.21, 0.081, 3.44, 5.7, and >100 μM, respectively) and MSK1, MSK2, CDK2, JNK2, IKK2 (IC50s>200 μM). MK2-IN-3 can reduce TNFα production in both U937 cells and in vivo .
LG101506 is a selective and orally active RXR modulator with a Ki of 2.7 nM for RXRα. LG101506 can be used for the research of type 2 diabetes and cancer .
a-FABP-IN-1 (Compound 5g) is a potent and selective human adipocyte fatty acid-binding protein (a-FABP) inhibitor with a Ki below 1.0 nM. a-FABP-IN-1 inhibits the pro-inflammatory cytokine production .
RIPK1-IN-19 (compound 10b) is a selective RIPK1 inhibitor (IC50=15 nM). RIPK1-IN-19 displays potent protective activity in TNFα-induced systemic inflammatory response syndrome (SIRS) model and Imiquimod (IMQ)-induced psoriasis model. RIPK1-IN-19 can be used in research on inflammation and immune system diseases .
Catalposide, an iridoid glycoside that could be isolated from Catalpa ovate G. Don (Bignoniaceae), inhibits TNF-α, IL-1β, and IL-6 productions and NF-κB (p65) activation in lipopolysaccharide-activated RAW 264.7 macrophages .
Lacto-N-neotetraose (LNnT) is an endogenous metabolite. Lacto-N-neotetraose can inhibit TNF-α induced IL-8 secretion in immature epithelial cells. Lacto-N-neotetraose has anti-inflammatory avtivity, and can improve the wound closure .
Anti-inflammatory agent 64 (compound 4b) inhibits the secretion of IL-6 and TNF-α. Anti-inflammatory agent 64 has antioxidant and anti-inflammatory activity in vitro and in vivo. Anti-inflammatory agent 64 can effectively reduce paw edema .
Sauchinone is a diastereomeric lignan isolated from Saururus chinensis (Saururaceae). Sauchinone inhibits LPS-inducible iNOS, TNF-α and COX-2 expression through suppression of I-κBα phosphorylation and p65 nuclear translocation. Sauchinone has anti-inflammatory and antioxidant activity .
Loganic acid 6′-O-β-D-glucoside, a iridoidal glucoside, is isolated from the whole plant of Gentiana rhodantha (Gentianaceae). Loganic acid 6′-O-β-D-glucoside inhibits LPS-induced NO and TNF-α production in macrophage RAW264.7 cells .
CPI-1189 is an orally active TNF-α release inhibitor. CPI-1189 inhibits phosphorylation of p38. CPI-1189 can inhibit apoptosis. CPI-1189 can be used in the study of HIV and neurological diseases .
Anti-inflammatory agent 41 (13a) significantly inhibit lipopolysaccharide (LPS)-induced expression of the proinflammatory cytokines IL-6 and TNF-α on J774A.1, THP-1 and LX-2 cells, and inhibits the activation of the NF-κB pathway .
ONO-3403 is an orally active serine protease inhibitor. ONO-3403 inhibits the production of TNF-α and nitric oxide induced by LPS. ONO-3403 inhibits the cell growth and induces the apoptosis, and has an antitumor effect on malignant tumors .
Negletein is a neuroprotectant enhances the action of nerve growth factor and induces neurite outgrowth in PC12 cells. Negletein shows promising anti-inflammatory activity via inhibition of TNF-α and IL-1β with IC50 values of 16.4 and 10.8 μM, respectively .
Delmitide (RDP58) is an orally active d-isomer decapeptide with potent anti-inflammatory activity. Delmitide inhibits production of TNF-α, IFN-γ, and interleukin (IL)-12, and up-regulates heme oxygenase 1 activity. Delmitide can be used for the research of ulcerative colitis .
Hedycoronen A has inhibitory activity on the IL-6, IL-12 p40, and TNF-α production in LPS-Stimulated BMDCs, with IC50s of 9.1 μM, 5.6 μM, and 46.0 μM. Hedycoronen A can be isolated from Hedychium coronarium .
Delmitide (RDP58) acetate is an orally active d-isomer decapeptide with potent anti-inflammatory activity. Delmitide acetate inhibits production of TNF-α, IFN-γ, and interleukin (IL)-12, and up-regulates heme oxygenase 1 activity. Delmitide acetate can be used for the research of ulcerative colitis .
Cynaropicrin is a sesquiterpene lactone which can inhibit tumor necrosis factor(TNF-α) release with IC50s of 8.24 and 3.18 μM for murine and human macrophage cells, respectively. Cynaropicrin also inhibits the increase of cartilage degradation factor (MMP13) and suppresses NF-κB signaling.
(E)-C-HDMAPP ammonium, is a potent phosphoantigen in ammonium form as well as a pyrophosphonate form of (E)-HDMAPP. (E)-C-HDMAPP is also an effective activator of γδ-T cells, induces T-cell stimulatory responses in vitro (EC50=0.91 nM for TNF-α release) .
NCI126224 is a TLR4 signaling inhibitor. NCI126224 suppress LPS (HY-D1056)-induced production of NF-κB, TNF-α, IL-1β, and NO in the nanomolar-low micromolar range. NCI126224 can be used for the research of inflammatory diseases .
Mizolastine is an orally active, high affinity and specific peripheral histamine H1 receptor antagonist (second generation antihistamine). Mizolastine effectively inhibits mRNA expression of VEGF165, VEGF120, TNF-α and KC. Mizolastine can be used in studies of allergic rhinitis and chronic idiopathic urticarial .
Mizolastine dihydrochloride is an orally active, high affinity and specific peripheral histamine H1 receptor antagonist (second generation antihistamine). Mizolastine dihydrochloride effectively inhibits mRNA expression of VEGF165, VEGF120, TNF-α and KC. Mizolastine dihydrochloride can be used in studies of allergic rhinitis and chronic idiopathic urticarial .
Neochlorogenic acid is a natural polyphenolic compound found in dried fruits and other plants. Neochlorogenic acid inhibits the production of TNF-α and IL-1β. Neochlorogenic acid suppresses iNOS and COX-2 protein expression. Neochlorogenic acid also inhibits phosphorylated NF-κB p65 and p38 MAPK activation.
DCVC (S-[(1E)-1,2-Dichloroethenyl]-L-cysteine) is a bioactive metabolite of trichloroethylene (TCE). DCVC inhibits pathogen-stimulated pro-inflammatory cytokines IL-1β, IL-8, and TNF-α release from tissue cultures .
Muscone is the main active monomer of traditional Chinese medicine musk. Muscone inhibits NF-κB and NLRP3 inflammasome activation. Muscone remarkably decreases the levels of inflammatory cytokines (IL-1β, TNF-α and IL-6), and ultimately improves cardiac function and survival rate .
Reticuline shows anti-inflammatory effects through JAK2/STAT3 and NF-κB signaling pathways. Reticuline inhibits mRNA expressions of TNF-α, and IL-6 and reduces the phosphorylation levels of JAK2 and STAT3 . Reticuline exhibits cardiovascular effects .
CU-CPT 4a (TLR3-IN-1) is a potent, highly selective TLR3 signaling inhibitor. CU-CPT 4a represses the expression of downstream signaling pathways mediated by the TLR3/dsRNA complex, including TNF-α and IL-1β .
Alphitolic acid (Aophitolic acid) is an anti-inflammatory triterpene could found in quercus aliena. Alphitolic acid blocks Akt–NF-κB signaling to induce apoptosis. Alphitolic acid induces autophagy. Alphitolic acid has anti-inflammatory activity and down-regulates the NO and TNF-α production. Alphitolic acid can be used for cancer and inflammation research .
Koaburaside is a cytoprotective and anti-inflammatory natural compound. Koaburaside shows antioxidant activity with an IC50 of 9.0 μM for DPPH-free radical scavenging assay. Koaburaside inhibits histamine release and expressions of IL-6 and TNF-α in human mast cells. Koaburaside also effectively inhibits influenza A neuraminidase .
Citronellol ((±)-Citronellol) is a monoterpene Pelargonium graveolens. Citronellol ((±)-Citronellol) induces necroptosis of cancer cell via up-regulating TNF-α, RIP1/RIP3 activities, down-regulating caspase-3/caspase-8 activities and increasing ROS (reactive oxygen species) accumulation .
Isoforskolin is the principle active component of C. forskohlii native to China. Isoforskolin reduces the secretion of lipopolysaccharide (LPS)-induced cytokines, namely TNF-α, IL-1β, IL-6 and IL-8, in human mononuclear leukocytes. Isoforskolin acts as an anti-inflammatory agent for the treatment of Lyme arthritis .
Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. Etanercept competitively inhibits the binding of both TNF-α and TNF-β to cell surface TNF receptors, rendering TNF biologically inactive. Etanercept shows efficacy against rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis .
KB-R7785 is a novel matrix metalloproteinase (MMP) inhibitor, which improves insulin sensitivity by inhibiting TNF-α production. KB-R7785 can be used for diabetes research. KB-R7785 has a protective efficacy against focal cerebral ischemia .
AMG-548, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε .
AMG-548 dihydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 dihydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 dihydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε .
Beclomethasone 17-propionate (Beclomethasone-17-monopropionate), an active metabolite of Beclomethasone dipropionate (HY-13571), is a glucocorticoid receptor (GR) agonist. Beclomethasone 17-propionate exhibits greater affinity for GR than Beclomethasone dipropionate. Beclomethasone 17-propionate effectively suppresses cytokine production in chronic obstructive pulmonary disease (COPD) lung macrophages .
β-Amyrenonol (11-Oxo-β-amyrin), an oleanolic-type triterpenoid in licorice roots, is a precursor of Glycyrrhetinic acid. β-Amyrenonol has anti-proliferative and anti-inflammatory activities, and β-Amyrenonol could function as the skeleton for the synthesis of many triterpenoids .
AMG-548 hydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 hydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 hydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε .
Direct Violet 1, an azo dye, is a textile dye. Direct Violet 1 is also the protein-protein interaction (PPI) between the SARS-CoV-2 spike protein and ACE2 inhibitor with IC50s of 1.47-2.63 μM .
RIPK1-IN-11 is a potent and orally active RIPK1 inhibitor (Kd=9.2 nM; IC50=67 nM). RIPK1-IN-11 inhibits necroptosis in both human and mouse cells (EC50=17-30 nM). Anti-inflammatory activity .
Cot inhibitor-2 is a potent, selective and orally active cot (Tpl2/MAP3K8) inhibitor with an IC50 of 1.6 nM. Cot inhibitor-2 inhibts TNF-α production in LPS-stimulated human whole blood with an IC50 of 0.3 μM .
LASSBio-1632 is a new anti-asthmatic lead candidate associated with selective inhibition of PDE4A and PDE4D isoenzymes and blockade of airway hyper-reactivity (AHR) and TNF-α production in the lung tissue. LASSBio-1632 (7j) displays high experimental BBB permeability across BBB through passive diffusion .
p38 MAP Kinase Inhibitor III (compound 7h) is a p38 MAPK inhibitor with an 50 of 0.9 μM. p38 MAP Kinase Inhibitor III also inhibits IL-1β and TNF-α release with 50 values of 0.37 μM and 0.044 μM, respectively .
Undecane-d24 is the deuterium labeled Undecane[1]. Undecane has anti-allergic and anti-inflammatory activities on sensitized rat basophilic leukemia (RBL-2H3) mast cells and HaCaT keratinocytes. In sensitized mast cells, Undecane inhibits degranulation and the secretion of histamine and TNF-α[2].
Rosolic Acid is an activator of Nrf2, as well as its downstream targets. Rosolic Acid increases the levels of angiogenic factors, decreases inflammation (TNF-α and IL-1β) and apoptotic markers (CXCL10 and CCL2). Rosolic Acid restores the function of pancreatic cells and protects endothelial cells (ECs) from endoplasmic reticulum stressed .
Tricin 7-O-β-D-glucopyranoside is a potent and orally active neuroprotective agent. Tricin 7-O-β-D-glucopyranoside induces Apoptosis. Tricin 7-O-β-D-glucopyranoside decreases the expression of TNF-α induced phosphor-κB-α, phosphor-NF-κB, HMGB1 .
Chlojaponilactone B is a lindenane-type sesquiterpenoid with anti-inflammatory properties. Chlojaponilactone B suppresses inflammatory responses by inhibiting TLR4 and subsequently decreasing reactive oxygen species (ROS) generation, downregulating the NF-κB, thus reducing the expression of the pro-inflammatory cytokines iNOS, NO, COX-2, IL-6 and TNF-α .
VEGFR-2-IN-40 is a VEGFR-2 inhibitor. VEGFR-2-IN-40 boosts early and late apoptosis. VEGFR-2-IN-40 decreases the levels immunomodulatory proteins TNF-α and IL-6 while showing a four-fold rise in an apoptotic marker caspase-3 .
VGX-1027 is an orally active isoxazole compound that exhibits various immunomodulatory properties. VGX-1027 targets macrophages, reducing the production of the proinflammatory mediators TNF-α, IL-1β, IL-10. VGX-1027 has antidiabetogenic effects by limiting cytokine-mediated immunoinflammatory events .
SKF-86002 is an orally active p38 MAPK inhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 inhibits lipopolysaccharide (LPS)-stimulate human monocyte IL-1 and TNF-α production (IC50 = 1 μM). SKF-86002 inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid .
FR 167653 free base, an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity. FR 167653 free base is effective in treating inflammation, relieving trauma and ischemia-reperfusion injury in vivo .
Asperulosidic Acid (ASPA), a bioactive iridoid glycoside, is extracted from the herbs of Hedyotis diffusa Willd. Asperulosidic Acid (ASPA) has anti-tumor, anti-oxidant, and anti-inflammatory activities .
ASPA is related to the inhibition of inflammatory cytokines (TNF-α, IL-6) and mediators via suppression of the NF-κB and mitogen-activated protein kinase (MAPK) signaling pathways .
α-Chaconine inhibits the expressions of COX-2, IL-1β, IL-6, and TNF-α at the transcriptional level. α-Chaconine inhibits the LPS-induced expressions of iNOS and COX-2 at the protein and mRNA levels and their promoter activities in RAW 264.7 macrophages. Anti-inflammatory effects .
SKF-86002 dihydrochloride is an orally active p38 MAPK inhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 dihydrochloride inhibits lipopolysaccharide (LPS)-stimulate human monocyte IL-1 and TNF-α production (IC50 = 1 μM). SKF-86002 dihydrochloride inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid .
Anti-inflammatory agent 20 (compound 5a) is a potent inhibitor of NO activity. Anti-inflammatory agent 20 shows anti-inflammatory activity. Anti-inflammatory agent 20 suppresses LPS-induced inflammation via inhibiting the activation of NF-κB and MAPK signaling and thereby reducing IL-6, TNF-α, iNOS, and COX-2 upregulation .
DHU-Se1 is a potent anti-inflammatory agent. DHU-Se1 can stimulate macrophages to release the reactive selenium compound and reduce the expression of cellular inflammatory factors (eg: iNOS and TNF-α). DHU-Se1 alleviate the process of inflammation by blocking the polarization of macrophages from M0 to M1 .
Anti-inflammatory agent 50 (compound a1) is a Fusidic acid derivative with anti-inflammatory effects. Anti-inflammatory agent 50 inhibits inflammatory factor NO, IL-6 and TNF-α. Anti-inflammatory agent 50 alleviates acute lung injury by regulating inflammatory mediators and suppressing the MAPK, NF-κB and NLRP3 inflammasome signaling pathways .
SIRT2/6-IN-1 (Compound 5) is a SIRT6/SIRT2 inhibitor, with IC50s of 106 μM and 114 μM. SIRT2/6-IN-1 increases H3K9 acetylation, increases glucose uptake and reduces TNF-α secretion in cells .
Taxamairin B is a potent anti-inflammatory agent. Taxamairin B decreases proinflammatory cytokines (TNF-α,IL-1β and IL-6) expression and the production of NO and ROS in LPS-induced RAW264.7 cells. Taxamairin B exhibits significant
protective effects in LPS-induced acute lung injury in mice .
Prostaglandin E2 Ethanolamide (PGE2-EA), an analog of PGE2, can be formed enzymatically following COX-2 oxygenation of endocannabinoids. Prostaglandin E2 Ethanolamide (PGE2-EA) could modulate the production of the proinflammatory cytokine TNF-α in human blood and human monocytic cells .
Naphazoline (Naphthazoline) hydrochloride is a potent α-adrenergic receptor agonist. Naphazoline hydrochloride reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline hydrochloride reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF。Naphazoline hydrochloride can be used for non-bacterial conjunctivitis research .
FR 167653 (FR 167653 sulfate), an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity. FR 167653 (FR 167653 sulfate) is effective in treating inflammation, relieving trauma and ischemia-reperfusion injury in vivo .
4-Hydroxychalcone is a chalcone metabolite with anti-angiogenic and anti-inflammatory activities. 4-Hydroxychalcone suppresses angiogenesis by suppression of growth factor pathway with no signs of cytotoxicity . 4-Hydroxychalcone inhibits TNF-α induced NF-κB pathway activation and activates BMP signaling, reduces resistant hypertension (RH) by attenuating hyperaldosteronism and renal injury in mice .
Tryptanthrin is an indole quinazoline that could be an alkaloid from indigo-bearing plants. Tryptanthrin is a potent and orally active cellular Leukotriene (LT) biosynthesis inhibitor. Tryptanthrin has anticancer activity. Tryptanthrin suppresses the expression levels of NOS1, COX-2, and NF-κB and regulates the expression levels of IL-2, IL-10, and TNF-α .
CU-115 is a potent TLR8 antagonist (IC50=1.04 µM), and shows selective for TLR8 over TLR7 (IC50=>50 µM). CU-115 decreases TNF-α and IL-1β production activated by R-848 in THP-1 cells .
CO delivery molecule 1 (compound 4) localizes to the endoplasmic reticulum, mitochondria, and lysosomes. Subcellular localization of CO delivery molecule 1 results in CO-induced toxicity effects. Anti-inflammatory effects of CO delivery molecule 1, as measured by TNF-α suppression, occur at the nanomolar level in the absence of CO release, and are enhanced with visible-light-induced CO release .
Anti-inflammatory agent 17 is a potent and orally active anti-inflammatory agent. Anti-inflammatory agent 17 inhibits the release of IL-6 and TNF-α in vitro experiments without cytotoxicity. Anti-inflammatory agent 17 exhibits anti-inflammatory activity in vivo. Anti-inflammatory agent 17 has the potential for the research of Acute lung injury (ALI) .
IKKβ-IN-1 is a potent and orally active IkappaB (IKK-β) inhibitor with IC50 of 0.20 μM. IKKβ-IN-1 can reduce PGE2 and TNF-α production in mouse macrophage cells. IKKβ-IN-1 has the ability to protect mice against septic shock induced mortality .
LSD1-IN-21 (compound 5a) is a potent and BBB-penetrated LSD1 (Lysine specific demethylase-1) inhibitor, with an IC50 of 0.956 µM. LSD1-IN-21 significantly reduces the pro-inflammatory cytokine TNF-α. LSD1-IN-21 shows good anticancer and anti-inflammatory activity .
AMS-17 is a potent NLRP3 inhibitor, inhibiting microglia activation in vitro and in vivo. AMS-17 also inhibits cytokines such as caspase-1, TNF-α, IL-1β and inducible nitric oxide synthase (iNOS) in N9 cells. AMS-17 can be used for researching inflammation-associated neurological disorders .
NOD2 antagonist 1 (compound 32) is a potent and selective NOD2 antagonist with an IC50 of 5.23 μM. NOD2 antagonist 1 inhibits Muramyl dipeptide (MDP)-induced IL-8 secretion in THP-1 cells and inhibits MDP-induced IL-6, IL-10, TNF-α release in PBMCs .
Naphazoline (Naphthazoline) is a potent α-adrenergic receptor agonist. Naphazoline reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF。Naphazoline can be used for non-bacterial conjunctivitis research .
2'-Fucosyllactose (2'-FL) is an oligosaccharide that could be derived from human milk. 2'-Fucosyllactose regulates the expression of CD14, alleviates colitis and regulates the gut microbiome. 2'-Fucosyllactose stimulates T cells to increase IFN-γ production and decreases IL-6, IL-17, and TNF-α production of cytokines .
Mca-PLAQAV-Dpa-RSSSR-NH2 is a fluorescent peptide and as one of fluorescent substrates of TNF-α converting enzyme (TACE; ADAM17), ADAM 9 and ADAM 10. Mca-PLAQAV-Dpa-RSSSR-NH2 is a substrate based on fluorescence resonance energy transfer, and its activity can be determined by the change of fluorescence intensity during pyrolysis .
Shizukaol B is a lindenane-type dimeric sesquiterpene, used to be isolated from the whole plant of Chloranthus henryi. Shizukaol B has anti-inflammatory effect against lipopolysaccharide (LPS)-induced activation of BV2 microglial cells. Shizukaol B inhibits iNOS and COX-2, and suppresses NO production, TNF-α, and IL-1β expression .
Mca-PLAQAV-Dpa-RSSSR-NH2 is a fluorescent peptide and as one of fluorescent substrates of TNF-α converting enzyme (TACE); ADAM17, ADAM 9 and ADAM 10. Mca-PLAQAV-Dpa-RSSSR-NH2 is a substrate based on fluorescence resonance energy transfer, and its activity can be determined by the change of fluorescence intensity during pyrolysis .
Semapimod, an inhibitor of proinflammatory cytokine production, can inhibit TNF-α, IL-1β, and IL-6. Semapimod inhibits TLR4 signaling (IC50≈0.3 μM). Semapimod inhibits p38 MAPK and nitric oxide production in macrophages. Semapimod has potential in a variety of inflammatory and autoimmune disorders .
Anti-inflammatory agent 74 (B5) is an anti-inflammatory agent that can inhibit NO, IL-6, and TNF-α, with IC50 values of 10.88 μM and 4.93 μM for NO and IL-6, respectively. Anti-inflammatory agent 74 alleviates acute lung injury (ALI) by regulating inflammatory mediators and inhibiting the MAPK and NF-κB signaling pathways .
Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively .
BIIB068 is a potent, selective, reversible and orally active BTK inhibitor with an IC50 of 1 nM and a Kd of 0.3 nM. BIIB068 shows more >400-fold selective for BTK than other kinases. BIIB068 has the potential for autoimmune diseases research .
Coixol (6-Methoxy-2-benzoxazolinone; 6-MBOA) is a potent and orally active anti-inflammatory agent. Coixol decreases the iNOS protein expression. Coixol inhibits the production of TNF-α, IL-6, and IL-1β. Coixol improves glucose tolerance and plasma insulin. Coixol decreases the blood glucose level .
LTβR-IN-1 is a potent, selective lymphotoxin β receptor (LTβR) inhibitor. LTβR-IN-1 also selectively inhibits the nuclear translocation of p52 depended on TNF12A, instead of the nuclear translocation of p65 mediated by TNF-α receptor. LTβR-IN-1 regulates the NF-kB signaling pathway IN a ligand-independent manner .
Cucurbitacin IIb is an active component isolated from Hemsleya amabilis, induces apoptosis with anti-inflammatory activity. Cucurbitacin IIb inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB (p65), blocks nuclear translocation of NF-κB (p65) and decreases mRNA levels of IκBα and TNF-α .
LEO 39652 is a dual-soft PDE4 inhibitor with IC50s of 1.2 nM, 1.2 nM, 3.0 nM and 3.8 nM for PDE4A, PDE4B, PDE4C and PDE4D, respectively. LEO 39652 also inhibits TNF-α with an IC50 value of 6.0 nM. LEO 39652 is used for topical research of Atopic dermatitis (AD) .
TMI-1 is a potent inhibitor of disintegrin metalloenzyme 17 (ADAM17) and other MMPs. TMI-1 inhibits LPS-induced TNF-α secretion in human primary monocytes, and human whole blood . TMI-1 selectively induces caspase-dependent apoptosis in triple negative (TN) and ERBB2-overexpressing breast tumor cell lines .
Anti-inflammatory agent 22 (compound 14a) is an orally active anti-inflammatory agent. Anti-inflammatory agent 22 inhibits LPS-induced TNF-α production with an IC50 value of 14.6 μM. Anti-inflammatory agent 22 has preventive effects on lymphedematous tissue via suppression of adipogenesis. Anti-inflammatory agent 22 suppresses limb lymphedema volume in mice .
BET-IN-13 is a potent BET inhibitor with an IC50 value of 1.6 nM. BET-IN-13 reduces LPS-induced TNF-α, IL-1β, IL-6, and NOS2 mRNA expression levels. BET-IN-13 shows anti-inflammatory activity. BET-IN-13 has the potential for the research of acute liver injury .
Maceneolignan A is a natural product that can be isolated from mace, the aril of Myristica fragrans (Myristicaceae). Maceneolignan A inhibits the release of β-hexosaminidase in RBL-2H3 cells, with an IC50 of 48.4 μM. Maceneolignan A inhibits the release of TNF-α in antigen stimulated RBL-2H3 cells, with an IC50 of 63.7 μM .
Apratastat (TMI-005) is an orally active, non-selective and reversible TACE/MMPs inhibitor, can inhibit inhibit the release of TNF-α. Apratastat has the potential to overcome radiotherapy-resistance in non-small cell lung cancer (NSCLC) . Apratastat is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Naphazoline (Naphthazoline) nitrate is an α-adrenergic receptor agonist. Naphazoline nitrate reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline nitrate reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF。Naphazoline nitrate can be used for non-bacterial conjunctivitis research .
Glucocorticoid receptor modulator 1 is a highly potent and orally active non-steroidal selective glucocorticoid receptor modulator with an IC50 value of 9 nM and 130 nM for NF-κB and AP-1, respectively. Glucocorticoid receptor modulator 1 can effectively reduce the expression of inflammatory factors IL-6, IL-1β, TNF-α, also can relieve dermatitis in mice .
Citronellol (Standard) is the analytical standard of Citronellol. This product is intended for research and analytical applications. Citronellol ((±)-Citronellol) is a monoterpene Pelargonium graveolens. Citronellol ((±)-Citronellol) induces necroptosis of cancer cell via up-regulating TNF-α, RIP1/RIP3 activities, down-regulating caspase-3/caspase-8 activities and increasing ROS (reactive oxygen species) accumulation .
1V209 (TLR7 agonist T7) is a Toll-like receptor 7 (TLR7) agonist and has anti-tumor effects. 1V209 can be conjugated with various polysaccharides to improve its water solubility, and enhance its efficacy, and maintain low toxicity .
PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect .
GW1929 hydrochloride is an orally active peroxisome proliferator-activated receptor-γ (PPARγ) agonist with a pKi of 8.84 for human PPAR-γ, and pEC50s of 8.56 and 8.27 for human PPAR-γ and murine PPAR-γ, respectively. GW1929 hydrochloride has antidiabetic efficacy and neuroprotective potential. GW1929 hydrochloride suppresses neuronal apoptosis and shows anti-inflammatory potential .
Triptohypol C, a Tripterin (HY-13067) derivative, is a potent Nur77-targeting anti-inflammatory agent with an Kd value of 0.87 μM. Triptohypol C inhibits inflammatory response by promoting the interactions of Nur77 with TRAF2 and p62/SQSTM1 .
PGN-9856 is a selective and high affinity (pKi ≥ 8.3) ligand at EP2 receptor. PGN-9856 is a potetn and non-prostanoid EP2 receptor agonist (pEC50 ≥ 8.5). PGN-9856 shows anti-inflammatory and anti-glaucoma activities .
Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor. Resatorvid inhibits NO, TNF-α and IL-6 production with IC50s 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 and plays pivotal role in various inflammatory diseases .
Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM . Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway . Shikonin decreases exosome secretion through the inhibition of glycolysis . Shikonin inhibits AIM2 inflammasome activation .
SR-318 is a potent and highly selective p38 MAPK inhibitor with IC50s of 5 nM, 32 nM and 6.11 μM for p38α, p38β and p38α/β, respectively. SR-318 potently inhibits the TNF-α release in whole blood with an IC50 of 283 nM. SR-318 has anti-cancer and anti-inflammatory activity .
Orientin is a neuroprotective agentinhibits which has anti-inflammation, anti-oxidative, anti-tumor, and cardio protection properties. Orientin inhibits the levels of IL-6, IL-1β and TNF-α. Orientin increases IL-10 level. Orientin exhibits neuroprotective effect by inhibits TLR4 and NF-kappa B signaling pathway. Orientin can used in study neuropathic pain .
Adenosine-2'-monophosphate (2'-AMP) is converted by extracellular 2’,3'-CAMP. Adenosine-2'-monophosphate is further metabolized to extracellular adenosine (a mechanism called the extracellular 2’,3’-cAMP-adenosine pathway). Adenosine-2'-monophosphate inhibits LPS-induced TNF-α and CXCL10 production via A2A receptor activation .
KAG-308 is a potent selective and orally active agonist of EP4 receptor (a prostaglandin E2 receptor subtype), suppresses colitis and promotes histological mucosal healing, potently inhibits TNF-α production. KAG-308 shows a Ki and an EC50 of 2.57 nM and 17 nM for human EP4 receptor, respectively, more selective over EP1, EP2, EP3 and IP receptor .
MAO-B-IN-21 is an excellent MAO-B inhibitor with antioxidant activity and anti-Aβ aggregation activity. MAO-B-IN-21 also exhibits metal-ion chelating ability, anti-neuroinflammation (NO, TNF-α), neuroprotective activity and BBB permeability. MAO-B-IN-21 significantly improves the memory and cognitive impairment in Aβ1-42 induced Alzheimer's disease mice model .
Tylvalosin-d9 (Acetylisovaleryltylo?sin-d9)is the deuterium labeledTylvalosin(HY-128423A) . Tylvalosin is a third-generation macrolide, with anti-inflammatory property. Tylvalosin decreases the levels of IL-8, IL-6, IL-1β, PGE2, TNF-α and NO, and reduces the inflammatory cells recruitment and activation in mouse acute lung injury model .
TPNA10168 is an Nrf-2 activator that activates the Keap1-Nrf2-ARE pathway. TPNA10168 is neuroprotective against oxidative stress-induced damage. TPNA10168 significantly reduces the transcription of inflammatory genes, including TNF-α, IL-1β, IL-6, and iNOS. TPNA10168 can be used in research on anti-inflammatory and neurological diseases .
Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.) . 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, exhibiting anti-inflammatory antiapoptotic effects . Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC50 of 53.6 μM .
Semapimod tetrahydrochloride (CNI-1493), an inhibitor of proinflammatory cytokine production, can inhibit TNF-α, IL-1β, and IL-6. Semapimod tetrahydrochloride inhibits TLR4 signaling (IC50≈0.3 μM). Semapimod tetrahydrochloride inhibits p38 MAPK and nitric oxide production in macrophages. Semapimod tetrahydrochloride has potential in a variety of inflammatory and autoimmune disorders .
Quin C1 is a highly specific and potent agonist for formyl peptide receptor 2 (FPR2/ALX). Quin-C1 significantly reduces the neutrophil and lymphocyte counts in BALF, diminishes expression of TNF-α, IL-1β, KC, and TGF-β1, and decreases collagen deposition in lung tissue. Quin C1 has the potential for the research of lung injury .
β5i-IN-1 is a potent and selective inhibitor of β5i with a IC50 of 8.463 nM. β5i-IN-1 releases TNF-α and IL-6 and influences the transcriptional activity of NF-κB. β5i-IN-1 can be used in study idiopathic pulmonary fibrosis .
AX-024 hydrochloride is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 hydrochloride modulates cell signaling by targeting SH3 domains. AX-024 hydrochloride has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
AX-024 is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 modulates cell signaling by targeting SH3 domains. AX-024 has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
MD2-TLR4-IN-1 (compound 22m) is an inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex, inhibiting lipopolysaccharides (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively .
Santamarine (Santamarin), a sesquiterpene lactone, increases HO-1 expression through Nrf2 translocation and suppresses NO, PGE2, TNF-α, and IL-1β production through inhibition of NF-κB translocation in LPS-induced macrophages. Santamarine shows anti-photoaging properties via inhibition of MAPK/AP-1 and stimulation of TGF-β/Smad signaling in UVA-irradiated human dermal fibroblasts (HDFs). Antioxidant activities .
Diprovocim is a potent TLR1/TLR2 agonist. Diprovocim elicits full agonist activity in human THP-1 cells (EC50=110 pM). Diprovocim stimulates the release of TNF-α from mouse macrophages (EC50=1.3 nM). Diprovocim activates downstream MAPK and NF-κB signaling pathway. Diprovocim displays strong adjuvant activity in mice, particularly abetting cellular immune responses .
JNK2-IN-1 (Compound J27) is a JNK2 inhibitor (Kds: 79.2 μM). JNK2-IN-1 has anti-inflammatory activity. JNK2-IN-1 decreases the release of TNF-α and IL-6 through inhibiting the activation of NF-κB/MAPK pathway. JNK2-IN-1 alleviates the symptoms of LPS-induced acute lung injury (ALI) and sepsis .
HDAC6-IN-34 (compound 21) is an oral active and selective HDAC6 inhibitor with the IC50 of 18 nM. HDAC6-IN-34 increases the acetylation level of tubulin without affecting histone acetylation in cutaneous T-cell lymphoma cells and inhibits TNF-α secretion in LPS (HY-D1056)-stimulated macrophage cells. HDAC6-IN-34 shows excellent anti-arthritic efficacy in rat .
J-113863 is a potent and selective CCR1 antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively. J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect .
cis-Mulberroside A (Mulberroside D) is the cis-isomer of Mulberroside A. Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.) . 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, exhibiting anti-inflammatory and anti-apoptotic effects . Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC50 of 53.6 μM .
PDE4-IN-6 is a potent, safe and moderately selective PDE4 inhibitor with IC50s of 0.125 and 0.43 µM for PDE4B and PDE4D, respectively. PDE4-IN-6 can downregulate the expression level of TNF-α and IL-6. PDE4-IN-6 has potent immunomodulatory activity thereby its potential against rheumatoid arthritis. Anti-inflammatory and anti-arthritic effects .
COX-2-IN-10 is a potent COX-2 inhibitor. COX-2-IN-10 inhibits the production of PGE2 in concentration dependent manner (IC50=2.54 µM). COX-2-IN-10 inhibits the expression of iNOS and COX-2 on mRNA and protein level . COX-2-IN-10 inhibits the production of IL-6, TNF-α and IL-1β .
Lucidone, an anti-inflammatory agent that can be isolated from the fruit of Lindera erythrocarpa Makino. Lucidone inhibits LPS-induced NO and PGE2 production in RAW 264.7 mouse macrophages. Lucidone also decreases TNF-α secretion, iNOS and COX-2 expression. Lucidone prevents NF-κB translocation and inhibits JNK and p38MAPK signals. Lucidone also has inhibitory activity against Dengue virus (DENV) (EC50=25 μM) .
STING agonist-23 (CF502) is a non-nucleotide small-molecule STING agonist. STING agonist-23 activates STING, increases phosphorylation of STING, TBK1 and IRF3. STING agonist-23 promotes the levels of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells. STING agonist-23 exhibits activity against SARS-CoV series strains .
STING agonist-24 (CF504) is a non-nucleotide small-molecule STING agonist. STING agonist-23 activates STING, increases phosphorylation of STING, TBK1 and IRF3. STING agonist-23 promotes the levels of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells. STING agonist-23 exhibits activity against SARS-CoV series strains .
STING agonist-25 (CF505) is a non-nucleotide small-molecule STING agonist. STING agonist-23 activates STING, increases phosphorylation of STING, TBK1 and IRF3. STING agonist-23 promotes the levels of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells. STING agonist-23 exhibits activity against SARS-CoV series strains .
STING agonist-26 (CF508) is a non-nucleotide small-molecule STING agonist. STING agonist-23 activates STING, increases phosphorylation of STING, TBK1 and IRF3. STING agonist-23 promotes the levels of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells. STING agonist-23 exhibits activity against SARS-CoV series strains .
STING agonist-28 (CF510) is a non-nucleotide small-molecule STING agonist. STING agonist-23 activates STING, increases phosphorylation of STING, TBK1 and IRF3. STING agonist-23 promotes the levels of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells. STING agonist-23 exhibits activity against SARS-CoV series strains .
Anti-inflammatory agent 54 (compound 9c) is a derivative of Coixol and has anti-inflammatory activity. Anti-inflammatory agent 54 inhibits the NF-κB pathway and downregulates the expression of iNOS, TNF-α, IL-6 and IL-1β. Anti-inflammatory agent 54 inhibits LPS-induced nitric oxide (NO) production in RAW264.7 macrophages (IC50: 2.4 μM) and exerts in vivo anti-inflammatory activity in a mouse auricular edema model .
Anti-inflammatory agent 55 (compound 9j) is a derivative of Coixol and has anti-inflammatory activity. Anti-inflammatory agent 54 inhibits the NF-κB pathway and downregulates the expression of iNOS, TNF-α, IL-6 and IL-1β. Anti-inflammatory agent 54 inhibits LPS-induced nitric oxide (NO) production in RAW264.7 macrophages (IC50: 0.8 μM) and exerts in vivo anti-inflammatory activity in a mouse auricular edema model .
RIPK2-IN-5 (compound 14) is a high affinity and excellent selectivity RIPK2 inhibitor with an IC50 value of 5.1nM. RIPK2-IN-5 has cellular anti-inflammatory effect and can reduce the secretion of MDP-induced TNF-α with a dose-dependent manner. RIPK2-IN-5 shows moderate stability in human liver microsome. RIPK2-IN-5 can be used for the research of immune diseases .
Celastramycin A is an antibiotic isolated from Streptomyces MaB-QuH-8, which exhibits antimicrobial activity against series of gram-negative bacteria and mycobacteria, with MICs between 0.05-3.1 μg/ml . Celastramycin A exhibits immunosuppressing efficacy in ex vivo Drosophila through immune deficiency pathway (IC50 of 0.008 μg/ml), inhibits the immunoresponse in human innate immunity through TNF-α signaling, inhibits IL-8 production in HUEVCs with IC50 of 0.06 μg/ml .
LM-021 is a coumarin-chalcone derivative with anti-aggregatory, antioxidant, neuroprotective and anti-inflammatory properties which suppresses nitric oxide (NO), IL-1β, IL-6, TNF-α production, CD68 antigen (CD68) and histocompatibility-2 (MHCII) expression. LM-021 also attenuates the increase of caspase 1 activity, lactate dehydrogenase release and ROS level. LM-021 can be used for neurological research .
Gamma-glutamylcysteine (γ-Glutamylcysteine) TFA, an intermediate in glutathione (GSH) synthesis, is a dipeptide served as an essential cofactor for the antioxidant enzyme glutathione peroxidase (GPx). Gamma-glutamylcysteine TFA also upregulates the level of the anti-inflammatory cytokine IL-10 and reduces the levels of the pro-inflammatory cytokines (TNF-α,IL-6, and IL-1β). Gamma-glutamylcysteine TFA attenuates the changes in metalloproteinase activity in oligomeric Aβ40-treated astrocytes .
YQ128 is a potent and selective second-generation NLRP3 (NOD-like receptor P3) inflammasome inhibitor with an IC50 of 0.30 μM. YQ128 significantly and selectively suppresses the production of IL-1β, but not TNF-α, and it can cross the BBB to reach the CNS. YQ128 has anti-inflammatory activity . YQ128 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
CU-T12-9 is a specific TLR1/2 agonist 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 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS .
Anti-inflammatory agent 11 (compound 16) is a potent antimycobacterial and anti-inflammatory agent. Anti-inflammatory agent 11 inhibits Mtb H37Rv and M299 growth, with MIC50 (minimum inhibitory concentration 50%) of 1.3 and 6.9 μM, respectively. Anti-inflammatory agent 11 inhibits NO through the suppression of iNOS expression, and also inhibited the production of TNF-α and IL-1β. Anti-inflammatory agent 11 can be used for tuberculosis (TB) research .
Anti-inflammatory agent 15 (compound 29) is a potent antimycobacterial and anti-inflammatory agent. Anti-inflammatory agent 15 inhibits Mtb H37Rv and M299 growth, with MIC50 (minimum inhibitory concentration 50%) of 2.3 and 7.8 μM, respectively. Anti-inflammatory agent 15 inhibits NO through the suppression of iNOS expression, and also inhibited the production of TNF-α and IL-1β. Anti-inflammatory agent 15 can be used for tuberculosis (TB) research .
HCAR2 agonist 1 (Compound 9n) is a Gi protein-biased allosteric modulator of HCAR2. HCAR2 agonist 1 activates the Gi protein signaling pathway. HCAR2 agonist 1 shows anti-inflammatory effect, and reduces mRNA level of pro-inflammatory cytokine (TNF-α, IL-1β, IL-6, and MCP-1). HCAR2 agonist 1 enhances anti-inflammatory effects of orthosteric agonists in the mouse model of colitis .
TLR7 agonist 18 (Compound 21a) is a selective Toll-like receptor 7 (TLR7) agonist with an EC50 of 7.8 μM. TLR7 agonist 18 is not cytotoxic to hTLR7 cotransfected HEK293 cell lines and can induce the secretion of several cytokines, including IL-1β, IL-12p70, IL-8, and TNF-α. TLR7 agonist 18 can be used in vaccine, asthma, allergy and anti-cancer research .
NF-κB-IN-15 (compound 14r) is a potent NF-κB inhibitor. NF-κB-IN-15 decreases the NO levels and inhibits the release of IL-6, TNF-α, and IL-1β in LPS (HY-D1056) -induced cells. NF-κB-IN-15 inhibits LPS-induced phosphorylation of p65 and degradation of IκBα. NF-κB-IN-15 shows anti-inflammatory activity has the potential for the research of acute lung injury (ALI) .
JTE-607, a highly selective inflammatory cytokine synthesis inhibitor, protects from endotoxin shock in mice. JTE-607 inhibits inflammatory cytokine production, including TNF-α, IL-1β, IL-6, IL-8 and IL-10, from LPS-stimulated human PBMCs, with IC50s of 11, 5.9, 8.8, 7.3 and 9.1 nM, respectively . Cleavage and Polyadenylation Specificity Factor 3 (CPSF3) is the target of JTE-607 .
Keap1-Nrf2-IN-11 (compound 6k) is a Keap1-Nrf2 inhibitor with KD2 value of 0.21 nM. Keap1-Nrf2-IN-11 inhibits the productions of ROS and NO and the expression of TNF-α. Keap1-Nrf2-IN-11 relieves inflammations by increasing the Nrf2 nuclear translocation. Keap1-Nrf2-IN-11 can be used for anti-inflammatory research .
Cetrelimab (JNJ 63723283; JNJ 3283) is a human IgG4κ mAb targeting PD-1. Cetrelimab binds PD-1 (Kd=1.72 nM, HEK293) to block the interaction of PD-1 with PD-L1 and PD-L2 (IC50s=111.7 ng/mL and 138.6 ng/mL, respectively). Cetrelimab stimulates peripheral T cells, increases IFN-γ, IL-2, TNF-α level and inhibits tumor growth in vivo .
Narchinol B (Compound 4) is a sesquiter penoid
compound. Narchinol B has anti-inflammatory effects. Narchinol B works by
inhibiting proinflammatory mediators, including prostaglandin E2 (PGE2),
inducible nitric oxide synthase (iNOS), and cyclooxygenase-2 (COX-2) proteins,
as well as proinflammatory cytokines, such as interleukin-1b, IL-6, and tumor
necrosis factor-α (TNF-α). Narchinol B significantly inhibits LPS-induced
overproduction of NO in BV2 cells (IC50=2.43 μM)
.
DPP-4-IN-8 (compound 27) is a potent and selective DPP4 (dipeptidyl peptidase 4) inhibitor, with a Ki of 0.96 μM. DPP-4-IN-8 blocks the dipeptidase activity of DPP4 in both Caco-2 and HepG-2 cells. DPP-4-IN-8 also dose-dependently suppresses the expression levels of the chemokines tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), and interleukin-1β (IL-1β) .
RN-1734 is selective antagonist of the TRPV4 channel, completely antagonizes 4αPDD-mediated activation of TRPV4 with comparable, low micromolar IC50s for all three species (hTRPV4: 2.3 μM, mTRPV4: 5.9 μM, rTRPV4: 3.2 μM) . RN-1734 clearly decreases the production of tumor necrosis factor α (TNF-α) and interleukin 1β (IL-1β) without altering the number of olig2-positive cells .
T6167923 is a selective inhibitor of MyD88-dependent signaling pathways. T6167923 directly binds to Toll/IL1 receptor (TIR) domain of MyD88 and disrupts MyD88 homodimeric formation. T6167923 inhibits NF-κB driven Staphylococcus enterotoxin AP (SEAP) activity, and improves anti-inflammatory activity with IC50s of 2.7 μM, 2.9 μM, 2.66 μM and 2.66 μM for IFN-γ, IL-1β, IL-6 and TNF-α, respectively .
Anti-Aβ agent 1A (compound M15) has potent activity against amyloid-β. Anti-Aβ agent 1A possesses can significantly inhibit LPS-induced levels of IL-1β, IL-6 and TNF-α, and reduces the apoptosis of SH-SY5Y induced by H2O2 through mitochondria pathway. Anti-Aβ agent 1A possesses antioxidant, anti-inflammatory, anti-Aβ toxicity and neuroprotective activities. Anti-Aβ agent 1A can be used for researching Alzheimer’s disease (AD) .
PDE1-IN-5 (Compound 10c) is a selective PDE1C inhibitor (IC50: 15 nM). PDE1-IN-5 has anti- inflammatory activity, and inhibits expression of iNOS, TNF-α, IL-1α, IL-1β, and IL-6 induced by LPS. PDE1-IN-5 has anti-inflammatory bowel disease (IBD) effects in the dextran sodium sulfate (DSS)-Induced colitis mice model. PDE1-IN-5 can be used for research of IBD .
12R-LOX-IN-1 (Compound 4a) is a 12R-LOX inhibitor (IC50: 28.25 μM). 12R-LOX-IN-1 inhibits the hyper-proliferative state and colony forming potential of Imiquimod (HY-B0180)-induced psoriatic keratinocytes. 12R-LOX-IN-1 inhibits reactive oxygen species, Ki67, IL-17A, TNF-α and IL-6 production. 12R-LOX-IN-1 can be used for antipsoriatic research .
GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK-J4 hydrochloride is a cell permeable proagent of GSK-J1 .
CAY10789 (compound 6) is a potent CysLT1R (cysteinyl leukotriene receptor 1) antagonist (IC50=2.80 μM) and GPBAR1 (G-protein-coupled bile acid receptor 1) agonist (EC50=3 μM). CAY10789 significantly reduces the adhesion of U937 cells to HAEC, reduces the expression of TNF-α. CAY10789 shows very promising metabolic stability and excellent pharmacokinetics. CAY10789 can be used for the research of colitis, metabolic syndromes, and other GPBAR1/CysLT1R-related diseases .
NF-κB-IN-11 (Compound 3i) is a NF-κB inhibitor. NF-κB-IN-11 inhibits TNF-α induced activation of NF-κB pathway, and inhibits nuclear translocation of NF-κB. NF-κB-IN-11 down-regulates the expression levels of phosphor-IKK, IκBα, and NF-κB p65. NF-κB-IN-11 has anti-inflammatory activity, and alleviates dextran sulfate sodium-induced colitis in mice. NF-κB-IN-11 (p.o.) shows a MTD more than 1852 mg/kg in mice acute toxicity assay .
(R)-STU104 is a potent and orally active TAK1-MKK3 interaction inhibitor with IC50s of 0.58 μM and 4.0 μM for TNF-α and MKK3 phosphorylation. (R)-STU104 suppresses the TAK1/MKK3/p38/MnK1/MK2/elF4E signal pathways through binding with MKK3 and disrupting the TAK1 phosphorylating MKK3. (R)-STU104 can be used for researching ulcerative colitis .
PDE4-IN-11 is an inhibitor of phosphodiesterase isoenzyme 4 (PDE4). PDE4-IN-11 displays highly effective bronchodilatory and anti-inflammatory properties, can be used for obstructive or inflammatory airway diseases research .
GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable proagent of GSK-J1 . GSK-J4 induces endoplasmic reticulum stress-related apoptosis .
Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1ß, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research .
CB2R/FAAH modulator-1 is a cannabinoid type 2 receptor (CB2R) full agonist with Kis of 14.8 nM and 241.3 nM for CB2R and CB1R, respectively. CB2R/FAAH modulator-1 is a fatty acid amide hydrolase (FAAH) inhibitor with an IC50 of 4 μM. CB2R/FAAH modulator-1 decreases pro-inflammatory and increases anti-inflammatory cytokines production .
Z-Asp-CH2-DCB is an irreversible broad spectrum caspase inhibitor. Z-Asp-CH2-DCB also inhibits proteases with caspase-like activity. Z-D-CH2-DCB blocks the production of IL-1β, TNF-α, IL-6, and IFN-γ in staphylococcal enterotoxin B (SEB)-stimulated peripheral blood mononuclear cells (PBMC), and reduces SEB-1-stimulated T-cell proliferation in a dose-dependent manner. Z-Asp-CH2-DCB prevents SU5416-induced septal cell apoptosis and emphysema development .
1,11b-Dihydro-11b-hydroxymedicarpin (11b-Hydroxy-11b,1-dihydromedicarpin) is a pterocarpan from Ononis viscosa subsp. breviflora is a Medicarpin derivative . Medicarpin, a natural pterocarpan, heals cortical bone defect by activation of Notch and Wnt canonical signaling pathways . Medicarpin prevents arthritis in post-menopausal conditions by arresting the expansion of TH17 cells and pro-inflammatory cytokines. Medicarpin down-regulates pro-inflammatory cytokines like TNF-α, IL-6 and IL-17A, while up-regulates anti-inflammatory cytokine IL-10 in arthritis (CIA) model of mice .
L6H21, a Chalcone (HY-121054) derivative, is an orally active, potent and specific myeloid differentiation 2 (MD-2) inhibitor. L6H21 directly binds to MD-2 protein with a high affinity and low KD value of 33.3 μM, blocking the formation of the LPS-TLR4/MD-2 complex. L6H21 inhibits LPS-induced expression of TNF-α and IL-6 in RAW264.7 macrophages, with IC50 values of 6.58 and 8.59 μM, respectively. L6H21 can be used for alcoholic liver disease, metabolic disturbance and neuroinflammation research .
ADS032 is a dual inhibitor of NLRP1 and NLRP3 that can rapidly, reversibly and stably inhibit inflammasome formation. ADS032 can reduce NLPR1 and NLRP3 activation of human macrophages and bronchial epithelial cells to secrete and mature IL-1β and TNF-α, and reduce NLRP3-induced ASC speck formation. ADS032 protected mice against the deadly influenza A virus, reducing inflammation in the lungs and improving survival. ADS032 inhibits Nigericin (HY-127019)-induced IL-1β secretion with IC50s of 94.6 μM (No wash out) and 354 μM (Wash out) respectively .
HMGB1-IN-2 (compound 15) is an inhibitor of highly conserved nuclear protein (HMGB1), showing NO inhibitory effect with IC50 value of 20.2 μM in RAW264.7 cells. HMGB1-IN-2 (30 μM) decreases the level of IL-1 β, TNF-α, caspase-1 p20, inhibits the phosphorylation of NF-κB p65, exhibits anti-apoptotic activity. HMGB1-IN-2 (15 mg/kg; ip) relives kidney injury in septic acute kidney injury mouse. HMGB1-IN-2 inhibits Huh7 cells and A549 cells with IC50s of 77.0 μM, and 82.0 μM, respectively .
C18 Phytoceramide (t18:0/18:0) (Cer(t18:0/18:0)) is a bioactive sphingolipid found in the stratum corneum of Saccharomyces cerevisiae, wheat grain, and mammalian epidermis. Cer(t18:0/18:0) consists of a phytosphingosine backbone amine linked to a C18 fatty acid chain. Cer(t18:0/18:0) has the function of regulating apoptosis, cell differentiation, proliferation of smooth muscle cells and inhibition of mitochondrial respiratory chain. It also suppresses the expression of allergic cytokines IL-4, TNF-α, and transcription factors c-Jun and NF-κB in histone-stimulated mouse skin tissue. Formulations containing cer(t18:0/18:0) have been used as skin protectants in cosmetics as they reduce water loss and prevent epidermal dehydration and irritation.
Penfluridol (R-16341) is a potent, long-acting, first-generation, oral diphenylbutylpiperidine antipsychotic agent by targeting D2-like dopamine receptor. Penfluridol effectively inhibits TNFα-induced NF-κB activation and alleviates the severity of arthritis and colitis in vivo. Penfluridol is a Ca 2+-calmodulin inhibitor. Penfluridol induces apoptosis and autophagy. Penfluridol is used for chronic schizophrenia, acute psychosis, Tourette syndrome and autoimmune diseases. Penfluridol inhibites the growth of E. faecalis planktonic cells with the MIC of 7.81 µg/ml .
Antibody inhibitors are compounds with the same activity as the original therapeutic antibodies, which can be used as positive controls for drug efficacy evaluation and other studies. Antibody inhibitors can also assist in verifying the functional activity of the target protein. These antibody inhibitors are active in vivo and can achieve certain physiological functions by blocking or neutralizing target proteins, such as CD20, HER2, EGFR, VEGFR, TNF-α, etc. In drug screening, antibody inhibitor-based screening can be carried out to identify active compounds targeting target proteins and target diseases.
MCE can provide 21 antibody inhibitors that can be used for drug development in cancer, immunity, infection and other hot research areas.
Direct Violet 1, an azo dye, is a textile dye. Direct Violet 1 is also the protein-protein interaction (PPI) between the SARS-CoV-2 spike protein and ACE2 inhibitor with IC50s of 1.47-2.63 μM .
Taurohyodeoxycholic acid (THDCA) sodium is the taurine-conjugated form of the secondary bile acid hyodeoxycholic acid. Taurohyodeoxycholic acid can also reduce the activity and expression of myeloperoxidase TNF-α and IL-6, as well as colonic damage in TNBS-induced ulcerative colitis mouse model.
Rosolic Acid is an activator of Nrf2, as well as its downstream targets. Rosolic Acid increases the levels of angiogenic factors, decreases inflammation (TNF-α and IL-1β) and apoptotic markers (CXCL10 and CCL2). Rosolic Acid restores the function of pancreatic cells and protects endothelial cells (ECs) from endoplasmic reticulum stressed .
C18 Phytoceramide (t18:0/18:0) (Cer(t18:0/18:0)) is a bioactive sphingolipid found in the stratum corneum of Saccharomyces cerevisiae, wheat grain, and mammalian epidermis. Cer(t18:0/18:0) consists of a phytosphingosine backbone amine linked to a C18 fatty acid chain. Cer(t18:0/18:0) has the function of regulating apoptosis, cell differentiation, proliferation of smooth muscle cells and inhibition of mitochondrial respiratory chain. It also suppresses the expression of allergic cytokines IL-4, TNF-α, and transcription factors c-Jun and NF-κB in histone-stimulated mouse skin tissue. Formulations containing cer(t18:0/18:0) have been used as skin protectants in cosmetics as they reduce water loss and prevent epidermal dehydration and irritation.
TNF-α (31-45), human is a potent NF-kB pathway activator. TNF-αis a proinflammatory cytokine that induces necrosis or apoptosis. TNF alpha stimulates NF-κB pathway via TNFR2 promotes cancer growth, invasion, and metastasis .
TNF-α (31-45), human TFA is a potent NF-kB pathway activator. TNF-αis a proinflammatory cytokine that induces necrosis or apoptosis. TNF alpha stimulates NF-κB pathway via TNFR2 promotes cancer growth, invasion, and metastasis .
LEESGGGLVQPGGSMK, a proteolysis peptide, is a component of Infliximab. LEESGGGLVQPGGSMK can be used for quantitative analysis of Infliximab. Infliximab is a chimeric monoclonal IgG1 antibody that specifically binds to TNF-α .
LEESGGGLVQPGGSMK acetate, a proteolysis peptide, is a component of Infliximab. LEESGGGLVQPGGSMK acetate can be used for quantitative analysis of Infliximab. Infliximab is a chimeric monoclonal IgG1 antibody that specifically binds to TNF-α .
LEESGGGLVQPGGSMK TFA, a proteolysis peptide, is a component of Infliximab. LEESGGGLVQPGGSMK TFA can be used for quantitative analysis of Infliximab. Infliximab is a chimeric monoclonal IgG1 antibody that specifically binds to TNF-α .
Delmitide (RDP58) is an orally active d-isomer decapeptide with potent anti-inflammatory activity. Delmitide inhibits production of TNF-α, IFN-γ, and interleukin (IL)-12, and up-regulates heme oxygenase 1 activity. Delmitide can be used for the research of ulcerative colitis .
Delmitide (RDP58) acetate is an orally active d-isomer decapeptide with potent anti-inflammatory activity. Delmitide acetate inhibits production of TNF-α, IFN-γ, and interleukin (IL)-12, and up-regulates heme oxygenase 1 activity. Delmitide acetate can be used for the research of ulcerative colitis .
Mca-PLAQAV-Dpa-RSSSR-NH2 is a fluorescent peptide and as one of fluorescent substrates of TNF-α converting enzyme (TACE; ADAM17), ADAM 9 and ADAM 10. Mca-PLAQAV-Dpa-RSSSR-NH2 is a substrate based on fluorescence resonance energy transfer, and its activity can be determined by the change of fluorescence intensity during pyrolysis .
Mca-PLAQAV-Dpa-RSSSR-NH2 is a fluorescent peptide and as one of fluorescent substrates of TNF-α converting enzyme (TACE); ADAM17, ADAM 9 and ADAM 10. Mca-PLAQAV-Dpa-RSSSR-NH2 is a substrate based on fluorescence resonance energy transfer, and its activity can be determined by the change of fluorescence intensity during pyrolysis .
Citrullinated LL-37 5cit is a citrullinated LL-37 (HY-P1222) peptide. The antiviral and antibacterial effects of Citrullinated LL-37 5cit are significantly reduced compared to native LL-37. Citrullinated LL-37 5cit is unable to reduce LPS-mediated release of TNF-α due to a lack of LPS-binding capacity .
Infliximab (Avakine) is a chimeric monoclonal IgG1 antibody that specifically binds to TNF-α. Infliximab prevents the interaction of TNF-α with TNF-α receptor (TNFR1 and TNFR2). Infliximab has the potential for autoimmune, chronic inflammatory diseases and diabetic neuropathy research .
Golimumab (CNTO-148) is a potent human IgG1 TNFα antagonist monoclonal antibody. Golimumab has anti-inflammation activitity and inhibits IL-6 and IL-1β production. Golimumab acts via targeting and neutralizing TNF to prevent inflammation and destruction of cartilage and bone. Golimumab has the anticancer activity and induces cell apoptosis. Golimumab can be used for rheumatoid arthritis, Crohn's disease and cancer research .
Tengonermin (ARENEGYR) is a vascular-targeting agent consisting of the human Tumour Necrosis Factor-α (TNF-α) conjugated with the CNGRCG peptide. Tengonermin increases penetration of intratumoral chemotherapy and T-cell infiltration by modifying the tumour microenvironment .
Certolizumab pegol (Certolizumab) is a recombinant, polyethylene glycolylated, antigen-binding fragment of a humanized monoclonal antibody that selectively targets and neutralizes tumour necrosis factor-α (TNF-α). Certolizumab pegol can be used for rheumatoid arthritis and Crohn disease research .
Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. Etanercept competitively inhibits the binding of both TNF-α and TNF-β to cell surface TNF receptors, rendering TNF biologically inactive. Etanercept shows efficacy against rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis .
Cetrelimab (JNJ 63723283; JNJ 3283) is a human IgG4κ mAb targeting PD-1. Cetrelimab binds PD-1 (Kd=1.72 nM, HEK293) to block the interaction of PD-1 with PD-L1 and PD-L2 (IC50s=111.7 ng/mL and 138.6 ng/mL, respectively). Cetrelimab stimulates peripheral T cells, increases IFN-γ, IL-2, TNF-α level and inhibits tumor growth in vivo .
Geraniin is a TNF-α releasing inhibitor with numerous activities including anticancer, anti-inflammatory, and anti-hyperglycemic activities, with an IC50 of 43 μM.
Aloeresin G is a chromone glycoside that can be isolated from Aloe. Aloeresin G has a weak inhibitory effect on TNFα-induced NF-κB transcriptional activity, with an IC 50 value of 40.02 μM .
Myrtenal ((±)-Myrtenal) is a monoterpene that acts as an antineoplastic agent. Myrtenal inhibits liver cancer by preventing DEN-PB-induced upregulation of TNF-α protein expression.
Gnetifolin E is a resveratrol trimer derivative that can be isolated from Gnetum brunonianum. Gnetifolin E has anti-inflammatory activity, and inhibits TNF-α .
Episappanol is a natural compound isolated from Caesalpinia sappan heartwood with anti-inflammatory activity. Episappanol significantly inhibits the IL-6 and TNF-α secretion .
Gnetumontanin B is a stilbenoid that can be found in Gnetum montanum f. megalocarpum. Gnetumontanin B inhibits TNF-α production with an IC50 value of 1.49 µM .
Teuclatriol is an NF-κB inhibitor can be isolated from salvia mirzayanii, has anti-inflammatory effects. Teuclatriol inhibits TNF-α secretion in a dose-dependent manner .
Deoxyandrographolide suppresses LPS induced increase in mRNA levels of iNOS as well as production of proinflammatory mediators TNF-α and IL-6. Deoxyandrographolide potentiates NGF-induced neurite outgrowth .
Sinulatumolin E (compound 6), a terpenoid, displays significant TNF-α inhibitory activity with an IC50 of 3.6 μM. Sinulatumolin E (compound 6) exhibits anti-inflammatory activity .
Homoplantaginin is a flavonoid from a traditional Chinese medicine Salvia plebeia with antiinflammatory and antioxidant properties. Homoplantaginin could inhibit TNF-α and IL-6 mRNA expression, IKKβ and NF-κB phosphorylation.
Oleaside A is a polar cardenolide monoglycoside isolated from Nerium oleander, inhibits the induction of ICAM-1 induced by IL-1α and TNF-α, and has anti-tumor activity .
Sibiricine (Compound 8) is an isoquinoline alkaloid derived from the medicinal plant Corydalis crispa. Sibiricine has significant anti-inflammatory activity on TNF-α production by LPS-activated THP-1 cells .
Ginsenoside Rc, one of major Ginsenosides from Panax ginseng, enhances GABA receptorA (GABAA)-mediated ion channel currents (IGABA). Ginsenoside Rc inhibits the expression of TNF-α and IL-1β.
Methylenedihydrotanshinquinone is a natural product that can be isolated from the dried root of S. miltiorrhiza. Methylenedihydrotanshinquinone has anti-inflammatory effect by inhibiting expression of TNF-α, IL-1β, and IL-8 .
Myrcene (β-Myrcene) is a type of aromatic compound that inhibits TNFα and NF-κB activity. Myrcene has anti-invasive action, inhibits cell cycle, and leads to cancer cell apoptosis. Myrcene has strong blood protection effect, anti-inflammation, and anti-inflammatory activity.
D-Trimannuronic acid, an alginate oligomer is extracted from seaweed. D-Trimannuronic acid can induce TNF‐α secretion by mouse macrophage cell lines. D-Trimannuronic acid can be used for the research of pain and vascular dementia .
Linderaspirone A is a natural compound that can be isolated from the roots of Lindera aggregate. Linderaspirone A shows significant inhibitory effects on the production of prostaglandin E2 (PGE2),TNF-α, and IL-6 .
Soyasapogenol A, a triterpene compound, isolated from soybean. Soyasapogenol A directly prevents apoptosis of hepatocytes, and secondly, inhibits the elevation of plasma TNF-α, which consequently results in the prevention of liver damage in the Concanavalin A-induced hepatitis model .
Lupeol acetate, a derivative of Lupeol, suppresses the progression of rheumatoid arthritis (RA) by inhibiting the activation of macrophages and osteoclastogenesis through downregulations of TNF-α, IL-1β, MCP-1, COX-2, VEGF and granzyme B .
Undecane has anti-allergic and anti-inflammatory activities on sensitized rat basophilic leukemia (RBL-2H3) mast cells and HaCaT keratinocytes. In sensitized mast cells, Undecane inhibits degranulation and the secretion of histamine and TNF-α[
Ginsenoside Rh1 (Standard) is the analytical standard of Ginsenoside Rh1. This product is intended for research and analytical applications. Ginsenoside Rh1 (Prosapogenin A2) inhibits the expression of PPAR-γ, TNF-α, IL-6, and IL-1β.
Catalposide, an iridoid glycoside that could be isolated from Catalpa ovate G. Don (Bignoniaceae), inhibits TNF-α, IL-1β, and IL-6 productions and NF-κB (p65) activation in lipopolysaccharide-activated RAW 264.7 macrophages .
Lacto-N-neotetraose (LNnT) is an endogenous metabolite. Lacto-N-neotetraose can inhibit TNF-α induced IL-8 secretion in immature epithelial cells. Lacto-N-neotetraose has anti-inflammatory avtivity, and can improve the wound closure .
Sauchinone is a diastereomeric lignan isolated from Saururus chinensis (Saururaceae). Sauchinone inhibits LPS-inducible iNOS, TNF-α and COX-2 expression through suppression of I-κBα phosphorylation and p65 nuclear translocation. Sauchinone has anti-inflammatory and antioxidant activity .
Loganic acid 6′-O-β-D-glucoside, a iridoidal glucoside, is isolated from the whole plant of Gentiana rhodantha (Gentianaceae). Loganic acid 6′-O-β-D-glucoside inhibits LPS-induced NO and TNF-α production in macrophage RAW264.7 cells .
Negletein is a neuroprotectant enhances the action of nerve growth factor and induces neurite outgrowth in PC12 cells. Negletein shows promising anti-inflammatory activity via inhibition of TNF-α and IL-1β with IC50 values of 16.4 and 10.8 μM, respectively .
Hedycoronen A has inhibitory activity on the IL-6, IL-12 p40, and TNF-α production in LPS-Stimulated BMDCs, with IC50s of 9.1 μM, 5.6 μM, and 46.0 μM. Hedycoronen A can be isolated from Hedychium coronarium .
Cynaropicrin is a sesquiterpene lactone which can inhibit tumor necrosis factor(TNF-α) release with IC50s of 8.24 and 3.18 μM for murine and human macrophage cells, respectively. Cynaropicrin also inhibits the increase of cartilage degradation factor (MMP13) and suppresses NF-κB signaling.
Neochlorogenic acid is a natural polyphenolic compound found in dried fruits and other plants. Neochlorogenic acid inhibits the production of TNF-α and IL-1β. Neochlorogenic acid suppresses iNOS and COX-2 protein expression. Neochlorogenic acid also inhibits phosphorylated NF-κB p65 and p38 MAPK activation.
Muscone is the main active monomer of traditional Chinese medicine musk. Muscone inhibits NF-κB and NLRP3 inflammasome activation. Muscone remarkably decreases the levels of inflammatory cytokines (IL-1β, TNF-α and IL-6), and ultimately improves cardiac function and survival rate .
Reticuline shows anti-inflammatory effects through JAK2/STAT3 and NF-κB signaling pathways. Reticuline inhibits mRNA expressions of TNF-α, and IL-6 and reduces the phosphorylation levels of JAK2 and STAT3 . Reticuline exhibits cardiovascular effects .
Alphitolic acid (Aophitolic acid) is an anti-inflammatory triterpene could found in quercus aliena. Alphitolic acid blocks Akt–NF-κB signaling to induce apoptosis. Alphitolic acid induces autophagy. Alphitolic acid has anti-inflammatory activity and down-regulates the NO and TNF-α production. Alphitolic acid can be used for cancer and inflammation research .
Koaburaside is a cytoprotective and anti-inflammatory natural compound. Koaburaside shows antioxidant activity with an IC50 of 9.0 μM for DPPH-free radical scavenging assay. Koaburaside inhibits histamine release and expressions of IL-6 and TNF-α in human mast cells. Koaburaside also effectively inhibits influenza A neuraminidase .
Citronellol ((±)-Citronellol) is a monoterpene Pelargonium graveolens. Citronellol ((±)-Citronellol) induces necroptosis of cancer cell via up-regulating TNF-α, RIP1/RIP3 activities, down-regulating caspase-3/caspase-8 activities and increasing ROS (reactive oxygen species) accumulation .
Isoforskolin is the principle active component of C. forskohlii native to China. Isoforskolin reduces the secretion of lipopolysaccharide (LPS)-induced cytokines, namely TNF-α, IL-1β, IL-6 and IL-8, in human mononuclear leukocytes. Isoforskolin acts as an anti-inflammatory agent for the treatment of Lyme arthritis .
β-Amyrenonol (11-Oxo-β-amyrin), an oleanolic-type triterpenoid in licorice roots, is a precursor of Glycyrrhetinic acid. β-Amyrenonol has anti-proliferative and anti-inflammatory activities, and β-Amyrenonol could function as the skeleton for the synthesis of many triterpenoids .
Tricin 7-O-β-D-glucopyranoside is a potent and orally active neuroprotective agent. Tricin 7-O-β-D-glucopyranoside induces Apoptosis. Tricin 7-O-β-D-glucopyranoside decreases the expression of TNF-α induced phosphor-κB-α, phosphor-NF-κB, HMGB1 .
Chlojaponilactone B is a lindenane-type sesquiterpenoid with anti-inflammatory properties. Chlojaponilactone B suppresses inflammatory responses by inhibiting TLR4 and subsequently decreasing reactive oxygen species (ROS) generation, downregulating the NF-κB, thus reducing the expression of the pro-inflammatory cytokines iNOS, NO, COX-2, IL-6 and TNF-α .
Asperulosidic Acid (ASPA), a bioactive iridoid glycoside, is extracted from the herbs of Hedyotis diffusa Willd. Asperulosidic Acid (ASPA) has anti-tumor, anti-oxidant, and anti-inflammatory activities .
ASPA is related to the inhibition of inflammatory cytokines (TNF-α, IL-6) and mediators via suppression of the NF-κB and mitogen-activated protein kinase (MAPK) signaling pathways .
α-Chaconine inhibits the expressions of COX-2, IL-1β, IL-6, and TNF-α at the transcriptional level. α-Chaconine inhibits the LPS-induced expressions of iNOS and COX-2 at the protein and mRNA levels and their promoter activities in RAW 264.7 macrophages. Anti-inflammatory effects .
Taxamairin B is a potent anti-inflammatory agent. Taxamairin B decreases proinflammatory cytokines (TNF-α,IL-1β and IL-6) expression and the production of NO and ROS in LPS-induced RAW264.7 cells. Taxamairin B exhibits significant
protective effects in LPS-induced acute lung injury in mice .
4-Hydroxychalcone is a chalcone metabolite with anti-angiogenic and anti-inflammatory activities. 4-Hydroxychalcone suppresses angiogenesis by suppression of growth factor pathway with no signs of cytotoxicity . 4-Hydroxychalcone inhibits TNF-α induced NF-κB pathway activation and activates BMP signaling, reduces resistant hypertension (RH) by attenuating hyperaldosteronism and renal injury in mice .
Tryptanthrin is an indole quinazoline that could be an alkaloid from indigo-bearing plants. Tryptanthrin is a potent and orally active cellular Leukotriene (LT) biosynthesis inhibitor. Tryptanthrin has anticancer activity. Tryptanthrin suppresses the expression levels of NOS1, COX-2, and NF-κB and regulates the expression levels of IL-2, IL-10, and TNF-α .
2'-Fucosyllactose (2'-FL) is an oligosaccharide that could be derived from human milk. 2'-Fucosyllactose regulates the expression of CD14, alleviates colitis and regulates the gut microbiome. 2'-Fucosyllactose stimulates T cells to increase IFN-γ production and decreases IL-6, IL-17, and TNF-α production of cytokines .
Shizukaol B is a lindenane-type dimeric sesquiterpene, used to be isolated from the whole plant of Chloranthus henryi. Shizukaol B has anti-inflammatory effect against lipopolysaccharide (LPS)-induced activation of BV2 microglial cells. Shizukaol B inhibits iNOS and COX-2, and suppresses NO production, TNF-α, and IL-1β expression .
Coixol (6-Methoxy-2-benzoxazolinone; 6-MBOA) is a potent and orally active anti-inflammatory agent. Coixol decreases the iNOS protein expression. Coixol inhibits the production of TNF-α, IL-6, and IL-1β. Coixol improves glucose tolerance and plasma insulin. Coixol decreases the blood glucose level .
Maceneolignan A is a natural product that can be isolated from mace, the aril of Myristica fragrans (Myristicaceae). Maceneolignan A inhibits the release of β-hexosaminidase in RBL-2H3 cells, with an IC50 of 48.4 μM. Maceneolignan A inhibits the release of TNF-α in antigen stimulated RBL-2H3 cells, with an IC50 of 63.7 μM .
Citronellol (Standard) is the analytical standard of Citronellol. This product is intended for research and analytical applications. Citronellol ((±)-Citronellol) is a monoterpene Pelargonium graveolens. Citronellol ((±)-Citronellol) induces necroptosis of cancer cell via up-regulating TNF-α, RIP1/RIP3 activities, down-regulating caspase-3/caspase-8 activities and increasing ROS (reactive oxygen species) accumulation .
Triptohypol C, a Tripterin (HY-13067) derivative, is a potent Nur77-targeting anti-inflammatory agent with an Kd value of 0.87 μM. Triptohypol C inhibits inflammatory response by promoting the interactions of Nur77 with TRAF2 and p62/SQSTM1 .
Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM . Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway . Shikonin decreases exosome secretion through the inhibition of glycolysis . Shikonin inhibits AIM2 inflammasome activation .
Orientin is a neuroprotective agentinhibits which has anti-inflammation, anti-oxidative, anti-tumor, and cardio protection properties. Orientin inhibits the levels of IL-6, IL-1β and TNF-α. Orientin increases IL-10 level. Orientin exhibits neuroprotective effect by inhibits TLR4 and NF-kappa B signaling pathway. Orientin can used in study neuropathic pain .
Adenosine-2'-monophosphate (2'-AMP) is converted by extracellular 2’,3'-CAMP. Adenosine-2'-monophosphate is further metabolized to extracellular adenosine (a mechanism called the extracellular 2’,3’-cAMP-adenosine pathway). Adenosine-2'-monophosphate inhibits LPS-induced TNF-α and CXCL10 production via A2A receptor activation .
Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.) . 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, exhibiting anti-inflammatory antiapoptotic effects . Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC50 of 53.6 μM .
Santamarine (Santamarin), a sesquiterpene lactone, increases HO-1 expression through Nrf2 translocation and suppresses NO, PGE2, TNF-α, and IL-1β production through inhibition of NF-κB translocation in LPS-induced macrophages. Santamarine shows anti-photoaging properties via inhibition of MAPK/AP-1 and stimulation of TGF-β/Smad signaling in UVA-irradiated human dermal fibroblasts (HDFs). Antioxidant activities .
cis-Mulberroside A (Mulberroside D) is the cis-isomer of Mulberroside A. Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.) . 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, exhibiting anti-inflammatory and anti-apoptotic effects . Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC50 of 53.6 μM .
Lucidone, an anti-inflammatory agent that can be isolated from the fruit of Lindera erythrocarpa Makino. Lucidone inhibits LPS-induced NO and PGE2 production in RAW 264.7 mouse macrophages. Lucidone also decreases TNF-α secretion, iNOS and COX-2 expression. Lucidone prevents NF-κB translocation and inhibits JNK and p38MAPK signals. Lucidone also has inhibitory activity against Dengue virus (DENV) (EC50=25 μM) .
Celastramycin A is an antibiotic isolated from Streptomyces MaB-QuH-8, which exhibits antimicrobial activity against series of gram-negative bacteria and mycobacteria, with MICs between 0.05-3.1 μg/ml . Celastramycin A exhibits immunosuppressing efficacy in ex vivo Drosophila through immune deficiency pathway (IC50 of 0.008 μg/ml), inhibits the immunoresponse in human innate immunity through TNF-α signaling, inhibits IL-8 production in HUEVCs with IC50 of 0.06 μg/ml .
Gamma-glutamylcysteine (γ-Glutamylcysteine) TFA, an intermediate in glutathione (GSH) synthesis, is a dipeptide served as an essential cofactor for the antioxidant enzyme glutathione peroxidase (GPx). Gamma-glutamylcysteine TFA also upregulates the level of the anti-inflammatory cytokine IL-10 and reduces the levels of the pro-inflammatory cytokines (TNF-α,IL-6, and IL-1β). Gamma-glutamylcysteine TFA attenuates the changes in metalloproteinase activity in oligomeric Aβ40-treated astrocytes .
Narchinol B (Compound 4) is a sesquiter penoid
compound. Narchinol B has anti-inflammatory effects. Narchinol B works by
inhibiting proinflammatory mediators, including prostaglandin E2 (PGE2),
inducible nitric oxide synthase (iNOS), and cyclooxygenase-2 (COX-2) proteins,
as well as proinflammatory cytokines, such as interleukin-1b, IL-6, and tumor
necrosis factor-α (TNF-α). Narchinol B significantly inhibits LPS-induced
overproduction of NO in BV2 cells (IC50=2.43 μM)
.
Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1ß, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research .
1,11b-Dihydro-11b-hydroxymedicarpin (11b-Hydroxy-11b,1-dihydromedicarpin) is a pterocarpan from Ononis viscosa subsp. breviflora is a Medicarpin derivative . Medicarpin, a natural pterocarpan, heals cortical bone defect by activation of Notch and Wnt canonical signaling pathways . Medicarpin prevents arthritis in post-menopausal conditions by arresting the expansion of TH17 cells and pro-inflammatory cytokines. Medicarpin down-regulates pro-inflammatory cytokines like TNF-α, IL-6 and IL-17A, while up-regulates anti-inflammatory cytokine IL-10 in arthritis (CIA) model of mice .
Tumour Necrosis Factor alpha (TNF alpha) is a potent pro-inflammatory cytokine. TNF alpha binds to its receptors, mainly TNFR1 and TNFR2, and then transmits molecular signals for biological functions such as inflammation and cell death. TNF alpha stimulates NF-κB pathway via TNFR2 promotes cancer growth, invasion, and metastasis. Anti-TNF-α MAb significantly suppresses the tumor development in colitis-associated cancer (CAC) mouse. TNF alpha as a proneurogenic factor activates the SAPK/JNK Pathway and can facilitate neuronal replacement and brain repair in response to brain injury. TNF-alpha/TNFSF2 Protein, Human (Biotinylated, HEK293, His-Avi) is a biotinylated recombinant protein with a C-Terminal Avi and a His label, It consists of 157 amino acids (V77-L233) and is produced in HEK293 cells.
Tumour Necrosis Factor alpha (TNF alpha) is a potent pro-inflammatory cytokine. TNF alpha binds to its receptors, mainly TNFR1 and TNFR2, and then transmits molecular signals for biological functions such as inflammation and cell death. TNF alpha stimulates NF-κB pathway via TNFR2 promotes cancer growth, invasion, and metastasis. Anti-TNF-α MAb significantly suppresses the tumor development in colitis-associated cancer (CAC) mouse. TNF alpha as a proneurogenic factor activates the SAPK/JNK Pathway and can facilitate neuronal replacement and brain repair in response to brain injury. TNF-alpha/TNFSF2 Protein, Human (HEK293, His-Avi) is a recombinant protein with a C-Terminal Avi and a His label, It consists of 157 amino acids (V77-L233) and is produced in HEK293 cells.
TNF-α/TNFSF2 protein is a cytokine that binds to TNFRSF1A/TNFR1 and TNFRSF1B/TNFBR. It is mainly secreted by macrophages and has multiple biological functions. It has the ability to induce cell death in specific tumor cell lines, serves as a potent pyrogen, can cause fever through direct action or stimulation of interleukin-1 secretion, and is involved in the induction of cachexia. Animal-Free TNF-alpha/TNFSF2 Protein, Pig (His) is the recombinant pig-derived animal-FreeTNF-alpha/TNFSF2 protein, expressed by E. coli , with C-His labeled tag. The total length of Animal-Free TNF-alpha/TNFSF2 Protein, Pig (His) is 156 a.a., with molecular weight of ~18.1 kDa.
TNF-alpha/TNFSF2 protein binds to TNFRSF1A/TNFR1 and TNFRSF1B/TNFBR, inducing cell death in specific tumors and causing fever. It can also stimulate cell proliferation, induce insulin resistance, promote angiogenesis, and mediate bone resorption. TNF-alpha's intracellular domain induces IL12 production, highlighting its diverse physiological impact. TNF-alpha/TNFSF2 Protein, Guinea (N-His) is the recombinant TNF-alpha/TNFSF2 protein, expressed by E. coli , with N-6*His labeled tag. The total length of TNF-alpha/TNFSF2 Protein, Guinea (N-His) is 156 a.a., with molecular weight of ~19 kDa.
TNF-alpha/TNFSF2 protein binds to TNFRSF1A/TNFR1 and TNFRSF1B/TNFBR. It induces tumor cell death, fever, cachexia, cell proliferation, and cell differentiation. It also causes insulin resistance and GKAP42 protein degradation in adipocytes. Additionally, it plays a role in angiogenesis, osteoclastogenesis, and IL12 production in dendritic cells. TNF-alpha/TNFSF2 Protein, Equine is the recombinant equine-derived TNF-alpha/TNFSF2 protein, expressed by E. coli , with tag free. The total length of TNF-alpha/TNFSF2 Protein, Equine is 157 a.a., with molecular weight of ~19.36 kDa.
Tumour Necrosis Factor alpha (TNF alpha) is a potent pro-inflammatory cytokine. TNF alpha binds to its receptors, mainly TNFR1 and TNFR2, and then transmits molecular signals for biological functions such as inflammation and cell death. TNF alpha stimulates NF-κB pathway via TNFR2 promotes cancer growth, invasion, and metastasis. Anti-TNF-α MAb significantly suppresses the tumor development in colitis-associated cancer (CAC) mouse. TNF alpha as a proneurogenic factor activates the SAPK/JNK Pathway and can facilitate neuronal replacement and brain repair in response to brain injury. TNF-alpha/TNFSF2 Protein, Rhesus macaque is a recombinant protein consisting of 157 amino acids (V77-L233) and is produced in E. coli.
Tumour Necrosis Factor alpha (TNF alpha) is a potent pro-inflammatory cytokine. TNF alpha binds to its receptors, mainly TNFR1 and TNFR2, and then transmits molecular signals for biological functions such as inflammation and cell death. TNF alpha stimulates NF-κB pathway via TNFR2 promotes cancer growth, invasion, and metastasis. Anti-TNF-α MAb significantly suppresses the tumor development in colitis-associated cancer (CAC) mouse. TNF alpha as a proneurogenic factor activates the SAPK/JNK Pathway and can facilitate neuronal replacement and brain repair in response to brain injury. TNF-alpha/TNFSF2 Protein, Bovine is a recombinant protein consisting of 157 amino acids (L78-L234) and is produced in E. coli.
Tumour Necrosis Factor alpha (TNF alpha) is a potent pro-inflammatory cytokine. TNF alpha binds to its receptors, mainly TNFR1 and TNFR2, and then transmits molecular signals for biological functions such as inflammation and cell death. TNF alpha stimulates NF-κB pathway via TNFR2 promotes cancer growth, invasion, and metastasis. Anti-TNF-α MAb significantly suppresses the tumor development in colitis-associated cancer (CAC) mouse. TNF alpha as a proneurogenic factor activates the SAPK/JNK Pathway and can facilitate neuronal replacement and brain repair in response to brain injury. TNF-alpha/TNFSF2 Protein, Human is a recombinant protein consisting of 157 amino acids (V77-L233) and is produced in E. coli.
Resiquimod-d5 is deuterium labeled Resiquimod. Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α[1][2].
Tylvalosin-d9 (Acetylisovaleryltylo?sin-d9)is the deuterium labeledTylvalosin(HY-128423A) . Tylvalosin is a third-generation macrolide, with anti-inflammatory property. Tylvalosin decreases the levels of IL-8, IL-6, IL-1β, PGE2, TNF-α and NO, and reduces the inflammatory cells recruitment and activation in mouse acute lung injury model .
Undecane-d24 is the deuterium labeled Undecane[1]. Undecane has anti-allergic and anti-inflammatory activities on sensitized rat basophilic leukemia (RBL-2H3) mast cells and HaCaT keratinocytes. In sensitized mast cells, Undecane inhibits degranulation and the secretion of histamine and TNF-α[2].
YQ128 is a potent and selective second-generation NLRP3 (NOD-like receptor P3) inflammasome inhibitor with an IC50 of 0.30 μM. YQ128 significantly and selectively suppresses the production of IL-1β, but not TNF-α, and it can cross the BBB to reach the CNS. YQ128 has anti-inflammatory activity . YQ128 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
TNF-α-IN-8 (compound I-42) is a TNF-α inhibitor. TNF-α-IN-8 is an isoindole-imide compound. TNF-α-IN-8 can be used for the research of cancer, heart disease, osteoporosis, inflammatory, allergic and autoimmune diseases . TNF-α-IN-8 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
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