Search Result
Results for "
TNF-α inhibitor
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
5
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-133807A
-
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TNF Receptor
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Inflammation/Immunology
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(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 .
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-
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- HY-133807
-
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TNF Receptor
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Inflammation/Immunology
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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 .
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- HY-118694
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- HY-149331
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TNF Receptor
Caspase
NF-κB
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Inflammation/Immunology
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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 .
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- HY-160436
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- HY-160433
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- HY-142069
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MMP
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Endocrinology
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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 .
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- HY-110343
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TNF Receptor
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Inflammation/Immunology
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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 .
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- HY-153330
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- HY-153329
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TNF Receptor
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Others
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TNF-α-IN-9 (compound 48) is a analog of NDM-1 inhibitor-3 (HY-150758). TNF-α-IN-9 is a TNF-α inhibitor. TNF-α-IN-9 shows low inhibitory activity .
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- HY-112275
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-
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- HY-133807B
-
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Others
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Inflammation/Immunology
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(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 .
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- HY-162599
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TNF Receptor
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Infection
Cancer
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Spirohypertone B is a potent Tumor necrosis factor-α (TNF-α) inhibitor. Spirohypertone B protects L929 cells from death induced by co-incubation with TNF-α and Actinomycin D (HY-17559) .
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- HY-123736
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MMP
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Others
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Ro 32-7315 is a TNF-α converting enzyme (TACE) inhibitor .
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- HY-20070
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TNF Receptor
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Others
Inflammation/Immunology
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BMS-566394 is a potent inhibitor of tumor necrosis factor-α (TNF-α) converting enzyme (TACE) that helps reduce the production of TNF-α, thereby alleviating inflammation and immune-mediated diseases and can be used in the study of inflammatory and autoimmune diseases .
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- HY-111255
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SPD304
5 Publications Verification
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TNF Receptor
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Cancer
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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 .
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- HY-111255A
-
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TNF Receptor
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Inflammation/Immunology
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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 .
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- HY-147078
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- HY-117082
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GBL-5g
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TNF Receptor
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Inflammation/Immunology
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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 .
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- HY-101041
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(E)-Tyrphostin AG 556
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EGFR
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Inflammation/Immunology
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(E)-AG 556 is a highly selective EGFR inhibitor and also blocks LPS-induced TNF-α production .
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- HY-156297
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Proteasome
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Inflammation/Immunology
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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 .
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- HY-N0472
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- HY-164102
-
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TNF Receptor
NF-κB
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Inflammation/Immunology
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TNF-α-IN-18 (Compound 61) is an inhibitor for TNF-α (IC50 of 1.8 μM), that inhibits TNF signaling pathway through block of NF-kB migration from cytoplasm to nucleus. TNF-α-IN-18 exhibits slight cytotoxicity to mouse fibroblast LM cell, with a CC50 >50 μM. TNF-α-IN-18 ameliorates the TNF- or Lipopolysaccharide (HY-D1056)-induced sepsis in mouse models. TNF-α-IN-18 protects mice from rheumatoid arthritis .
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- HY-N0358
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- HY-121401
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(±)-Myrtenal
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Others
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Cancer
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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.
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- HY-13229
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Caspase
Apoptosis
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Cancer
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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.
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- HY-N0604
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- HY-N9867
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TNF Receptor
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Inflammation/Immunology
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Gnetifolin E is a resveratrol trimer derivative that can be isolated from Gnetum brunonianum. Gnetifolin E has anti-inflammatory activity, and inhibits TNF-α .
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- HY-N1159
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NF-κB
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Inflammation/Immunology
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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 .
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- HY-108162A
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- HY-102040
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(Z)-Hispidol
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TNF Receptor
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Inflammation/Immunology
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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.
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- HY-N9315
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- HY-N10835
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Others
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Inflammation/Immunology
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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 .
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- HY-148908
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TNF Receptor
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-P10354
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- HY-14622
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RIP kinase
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Cancer
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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.
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- HY-110133
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JTE-607
2 Publications Verification
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Interleukin Related
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Inflammation/Immunology
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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 .
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- HY-U00179
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-
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- HY-100339
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GSK583
5 Publications Verification
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RIP kinase
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Endocrinology
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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.
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- HY-108162
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COX
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Inflammation/Immunology
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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 .
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- HY-110133A
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Interleukin Related
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Inflammation/Immunology
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JTE-607 free base, a highly selective inflammatory cytokine synthesis inhibitor, protects from endotoxin shock in mice. JTE-607 free base 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 free base .
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- HY-136010
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RIP kinase
PROTACs
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Inflammation/Immunology
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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 .
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- HY-148454
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- HY-N1949
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TNF Receptor
NF-κB
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Inflammation/Immunology
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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.
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- HY-N4275
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Others
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Cancer
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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 .
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- HY-12085
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- HY-13812
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- HY-N0472R
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TNF Receptor
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Metabolic Disease
Inflammation/Immunology
Cancer
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Geraniin (Standard) is the analytical standard of Geraniin. This product is intended for research and analytical applications. Geraniin is a TNF-α releasing inhibitor with numerous activities including anticancer, anti-inflammatory, and anti-hyperglycemic activities, with an IC50 of 43 μM.
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- HY-30235A
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PGE synthase
Bacterial
TNF Receptor
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Inflammation/Immunology
Cancer
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Benzydamine hydrochloride is an orally administered prostaglandin synthesis inhibitor that has anti-inflammatory, analgesic, antipyretic, and antibacterial properties. Benzydamine hydrochloride can inhibit TNF-α, stabilize cell membranes, and reduce oxidative stress within cells .
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- HY-30235
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PGE synthase
TNF Receptor
Bacterial
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Inflammation/Immunology
Cancer
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Benzydamine is an orally administered prostaglandin synthesis inhibitor that has anti-inflammatory, analgesic, antipyretic, and antibacterial properties. Benzydamine can inhibit TNF-α, stabilize cell membranes, and reduce oxidative stress within cells .
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- HY-N1940
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Cycloicaritin
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Interleukin Related
TNF Receptor
MMP
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Inflammation/Immunology
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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 .
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- HY-N0042
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- HY-126414
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Others
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Inflammation/Immunology
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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 .
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- HY-10172
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IKK2 inhibitor V
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IKK
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Cancer
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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 .
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- HY-135808
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NF-κB
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Inflammation/Immunology
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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 .
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- HY-154698
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Nucleoside Antimetabolite/Analog
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Cancer
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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 .
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- HY-N6073
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Apoptosis
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Inflammation/Immunology
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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 .
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- HY-169118
-
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TNF Receptor
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Inflammation/Immunology
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EGR-1-IN-2 (compound 2) is an EGR-1 inhibitor with anti-inflammatory activity. EGR-1-IN-2 inhibits the formation of EGR-1-DNA complexes induced by TNF-α in HaCaT cells .
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- HY-126114
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COX
Interleukin Related
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Inflammation/Immunology
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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 .
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- HY-123936
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NF-κB
IKK
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Neurological Disease
Inflammation/Immunology
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SR12343, an IKK/NF-κB inhibitor, is a NF-κB essential modulator (NEMO)-binding domain (NBD) mimetic. SR12343 inhibits TNF-α- and LPS-induced NF-κB activation by blocking the interaction between IKKβ and NEMO, with an IC50 of 37.02 μM for TNF-α-mediated NF-κB activation. SR12343 suppresses LPS-induced acute pulmonary inflammation in mice. SR12343 can be used for research of inflammatory and degenerative diseases .
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- HY-12085S
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CC-10004-d5
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Phosphodiesterase (PDE)
TNF Receptor
Apoptosis
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Inflammation/Immunology
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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].
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- HY-N2086
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- HY-N8593
-
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TNF Receptor
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Infection
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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 [
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- HY-100376
-
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TNF Receptor
Apoptosis
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Infection
Neurological Disease
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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 .
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- HY-123542
-
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Ser/Thr Protease
Apoptosis
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Cancer
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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 .
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- HY-149816
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-
- HY-147950
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- HY-103435
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Terrestrin A
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Deubiquitinase
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Inflammation/Immunology
Cancer
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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 .
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- HY-N3552
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NF-κB
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Inflammation/Immunology
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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 .
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- HY-N9445
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LNnT
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Endogenous Metabolite
TNF Receptor
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Inflammation/Immunology
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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 .
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- HY-155405
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ROS Kinase
Interleukin Related
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Inflammation/Immunology
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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 .
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- HY-12085R
-
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Phosphodiesterase (PDE)
Apoptosis
TNF Receptor
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Inflammation/Immunology
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Apremilast (Standard) is the analytical standard of Apremilast. This product is intended for research and analytical applications. 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 .
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- HY-N2350
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MMP
NF-κB
TNF Receptor
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Cancer
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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.
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- HY-N0613
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NF-κB
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Inflammation/Immunology
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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 .
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- HY-N9000
-
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TNF Receptor
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Inflammation/Immunology
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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 .
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- HY-16658C
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Z-VA-DL-D(OH)-FMK
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Caspase
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Infection
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Z-VA-DL-D-FMK (Z-VA-DL-D(OH)-FMK) is an inhibitor for caspase . Z-VA-DL-D-FMK binds irreversibly to caspases, increases the sensitivity of TNF-α, and activates HIV replication in infected T cell ACH-2 .
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- HY-N1949R
-
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TNF Receptor
NF-κB
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Inflammation/Immunology
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Homoplantaginin (Standard) is the analytical standard of Homoplantaginin. This product is intended for research and analytical applications. 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.
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- HY-N0722
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trans-5-O-Caffeoylquinic acid
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NF-κB
Interleukin Related
TNF Receptor
COX
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Inflammation/Immunology
Cancer
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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.
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- HY-147712
-
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PKC
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Inflammation/Immunology
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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 .
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- HY-N3421
-
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Interleukin Related
TNF Receptor
Influenza Virus
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Infection
Inflammation/Immunology
Cancer
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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 .
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- HY-142618
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-
- HY-32018
-
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MAP3K
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Cancer
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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 .
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- HY-106359
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-
- HY-106359A
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RDP-58 acetate
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TNF Receptor
IFNAR
Reactive Oxygen Species
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Cancer
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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 .
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- HY-112389
-
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p38 MAPK
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Inflammation/Immunology
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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 .
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- HY-108847
-
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TNF Receptor
Bacterial
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Inflammation/Immunology
Cancer
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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 .
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- HY-B1615
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NAB-365
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Adrenergic Receptor
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Inflammation/Immunology
|
Clenbuterol (NAB-365) is a β2-adrenergic receptor agonist with an EC50 of 31.9 nM . Clenbuterol is a very potent inhibitor of the lipopolysaccharide (LPS)-induced release of TNF-α and IL-1β. Clenbuterol can inhibit the inflammatory process. Clenbuterol is a bronchodilator .
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- HY-160437
-
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TNF Receptor
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Inflammation/Immunology
|
TNF-α-IN-16 is a potent TNFα inhibitor with an IC50 of <0.6 μM. TNF-α-IN-16 has antiinflammatory properties (WO2001072735A2; example 18) .
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- HY-160434
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-
- HY-134471
-
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TNF Receptor
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Inflammation/Immunology
|
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 .
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- HY-156060
-
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Toll-like Receptor (TLR)
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Inflammation/Immunology
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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 .
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- HY-126211
-
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HDAC
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Inflammation/Immunology
|
KBH-A42 is a novel histone deacetylase (HDAC) inhibitor with significant anti-inflammatory properties. KBH-A42 against TNF-α and NO production with IC50 values of 1.10 and 2.71 µM, respectively, in the LPS-induced murine macrophage RAW 264.7 cells .
|
-
- HY-160435
-
|
TNF Receptor
|
Inflammation/Immunology
|
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) .
|
-
- HY-B0164
-
|
Histamine Receptor
|
Inflammation/Immunology
|
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 .
|
-
- HY-B0164A
-
|
Histamine Receptor
|
Inflammation/Immunology
|
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 .
|
-
- HY-19717
-
S-[(1E)-1,2-Dichloroethenyl]-L-cysteine
|
TNF Receptor
|
Inflammation/Immunology
|
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 .
|
-
- HY-N0633
-
-
- HY-N1356
-
-
- HY-108473
-
TLR3-IN-1
|
Toll-like Receptor (TLR)
|
Cancer
|
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 .
|
-
- HY-160027
-
|
TNF Receptor
|
Inflammation/Immunology
|
TNF-alpha-IN-1 (compound 202) is an orally active inhibitor of TNF-alpha. TNF-alpha-IN-1 has anti-inflammatory activity which can used in study rheumatoid arthritis, psoriasis, and asthma .
|
-
- HY-P99148
-
-
- HY-12511
-
|
p38 MAPK
|
Inflammation/Immunology
|
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 .
|
-
- HY-108641
-
|
p38 MAPK
|
Inflammation/Immunology
|
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 .
|
-
- HY-161757
-
|
Others
|
Inflammation/Immunology
|
Anti-inflammatory agent 86 is a Chrysin (HY-14589) derivative with anti-inflammatory effects. Anti-inflammatory agent 86 inhibits monocyte adhesion to colon epithelium induced by TNF-α, with an IC50 of 4.71 μM. Anti-inflammatory agent 86 has the potential for the inflammatory bowel disease (IBD) research .
|
-
- HY-N0042R
-
-
- HY-N6073R
-
|
Apoptosis
|
Inflammation/Immunology
|
Soyasapogenol A (Standard) is the analytical standard of Soyasapogenol A. This product is intended for research and analytical applications. 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 .
|
-
- HY-162850
-
-
- HY-15509
-
CNI-1493 free base; CPSI-2364
|
Interleukin Related
TNF Receptor
p38 MAPK
|
Inflammation/Immunology
Cancer
|
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 .
|
-
- HY-129113
-
|
COX
|
Inflammation/Immunology
|
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 .
|
-
- HY-146419
-
|
NF-κB
COX
TNF Receptor
|
Inflammation/Immunology
|
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 .
|
-
- HY-146765
-
|
NOD-like Receptor (NLR)
|
Neurological Disease
Inflammation/Immunology
|
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 .
|
-
- HY-N8593S
-
|
TNF Receptor
|
Infection
|
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].
|
-
- HY-N8413
-
|
Toll-like Receptor (TLR)
Reactive Oxygen Species
NF-κB
|
Inflammation/Immunology
|
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 .
|
-
- HY-157546
-
-
- HY-N8593R
-
|
TNF Receptor
|
Infection
|
Undecane (Standard) is the analytical standard of Undecane. This product is intended for research and analytical applications. 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[
|
-
- HY-147506
-
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
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 .
|
-
- HY-157809
-
|
Interleukin Related
TNF Receptor
NF-κB
p38 MAPK
|
Inflammation/Immunology
|
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 .
|
-
- HY-163998
-
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
TLR4-IN-1 (compound 3k) inhibits the cell viability of RAW264.7 with an IC50 of 1.02 μM. TLR4-IN-1 inhibits the release of cytokine TNF-α, IL-1β and IL-6, and exhibits anti-inflammatory efficacy in rats rheumatoid arthritis models .
|
-
- HY-18754
-
|
p38 MAPK
Autophagy
|
Endocrinology
|
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 .
|
-
- HY-155753
-
|
NF-κB
COX
|
Inflammation/Immunology
|
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 .
|
-
- HY-123194
-
|
Histone Demethylase
Sirtuin
|
Metabolic Disease
|
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 .
|
-
- HY-161620
-
|
IRAK
|
Inflammation/Immunology
|
DW18134 is an inhibitor for interleukin receptor-associated kinase 4 (IRAK 4) with an IC50 of 11.2 nM. DW18134 inhibits phosphorylation of IRAK4 and IKK, downregulates the secretion of TNF-α and IL-6. DW18134 attenuates the Lipopolysaccharides (HY-D1056)-induced peritonitis and DSS-induced colitis in mouse models, and protects the intestinal barrier function .
|
-
- HY-123984
-
|
NF-κB
|
Metabolic Disease
|
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 .
|
-
- HY-131707
-
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
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) .
|
-
- HY-N12116
-
|
TNF Receptor
|
Cancer
|
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 .
|
-
- HY-N0722R
-
|
NF-κB
Interleukin Related
TNF Receptor
COX
|
Inflammation/Immunology
Cancer
|
Neochlorogenic acid (Standard) is the analytical standard of Neochlorogenic acid. This product is intended for research and analytical applications. 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.
|
-
- HY-N2350R
-
|
MMP
NF-κB
TNF Receptor
|
Cancer
|
Cynaropicrin (Standard) is the analytical standard of Cynaropicrin. This product is intended for research and analytical applications. 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.
|
-
- HY-119307
-
TMI-005
|
MMP
TNF Receptor
|
Cancer
|
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.
|
-
- HY-117569
-
|
TNF Receptor
|
Inflammation/Immunology
|
KF24345 free base is an orally active adenosine uptake inhibitor. KF24345 free base inhibits adenosine uptake by human, mouse, rabbit and hamster erythrocytes with IC50 values ??of 59.5, 130.1, 104.2 and 30.9 nM, respectively. KF24345 free base has anti-inflammatory activity and can inhibit LPS-induced TNF-α production and leukopenia in mice .
|
-
- HY-N0822
-
C.I. 75535; Isoarnebin 4
|
Chloride Channel
Pyruvate Kinase
NF-κB
TNF Receptor
HIV
AIM2
|
Cancer
|
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 .
|
-
- HY-18754A
-
FR 167653 sulfate
|
p38 MAPK
Autophagy
|
Endocrinology
|
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 .
|
-
- HY-107818
-
|
NF-κB
|
Cardiovascular Disease
Inflammation/Immunology
|
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 .
|
-
- HY-N6607
-
-
- HY-146547
-
|
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
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) .
|
-
- HY-146723
-
|
IKK
|
Inflammation/Immunology
|
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 .
|
-
- HY-147697
-
|
Histone Demethylase
TNF Receptor
|
Inflammation/Immunology
Cancer
|
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 .
|
-
- HY-N8371
-
|
NO Synthase
COX
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
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 .
|
-
- HY-N0613R
-
|
NF-κB
|
Inflammation/Immunology
|
Sauchinone (Standard) is the analytical standard of Sauchinone. This product is intended for research and analytical applications. 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 .
|
-
- HY-159669
-
|
HIV Protease
|
Infection
Inflammation/Immunology
|
Stercobilin hydrochloride (amixture of isomers) is a bile pigment metabolized by gut bacteria, and it's also an HIV protease inhibitor, with a Ki of 4 μM. Stercobilin hydrochloride (a mixture of isomers) can induce pro-inflammatory activity in mouse macrophage RAW264 cells, including the production of TNF-α and IL-1β. Stercobilin hydrochloride (a mixture of isomers) can be used in studies of inflammation and viral infections .
|
-
- HY-159516
-
-
- HY-11109
-
Resatorvid
Maximum Cited Publications
376 Publications Verification
TAK-242; CLI-095
|
Toll-like Receptor (TLR)
TNF Receptor
Interleukin Related
Autophagy
|
Inflammation/Immunology
Cancer
|
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 .
|
-
- HY-15509A
-
CNI-1493; CPSI-2364 tetrahydrochloride
|
TNF Receptor
Interleukin Related
p38 MAPK
|
Inflammation/Immunology
Cancer
|
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 .
|
-
- HY-N0936
-
Coixol
1 Publications Verification
6-Methoxy-2-benzoxazolinone; 6-MBOA
|
Others
|
Inflammation/Immunology
|
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 .
|
-
- HY-N1987
-
|
Apoptosis
|
Inflammation/Immunology
|
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 .
|
-
- HY-146435
-
|
TNF Receptor
|
Inflammation/Immunology
|
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 .
|
-
- HY-152213
-
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
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 .
|
-
- HY-B0164R
-
|
Histamine Receptor
|
Inflammation/Immunology
|
Mizolastine (Standard) is the analytical standard of Mizolastine. This product is intended for research and analytical applications. 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 .
|
-
- HY-N0633R
-
-
- HY-135674
-
|
p38 MAPK
TNF Receptor
|
Inflammation/Immunology
Cancer
|
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 .
|
-
- HY-N0405
-
|
TNF Receptor
Interleukin Related
|
Neurological Disease
Cancer
|
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 .
|
-
- HY-N12905
-
|
Antibiotic
Bacterial
|
Infection
|
Celastramycin A isomer is an isomer of Celastramycin A (HY-122292), an antibiotic against Gram-negative bacteria and Mycobacterium tuberculosis with an MIC of 0.05-3.1 μg/mL. Celastramycin A exerts immunosuppressive effects in Drosophila ex vivo via the immunodeficiency pathway (IC50 of 8 ng/mL), inhibits human innate immune responses via the TNF-α pathway, and inhibits IL-8 production in HUEVC with an IC50 of 60 ng/mL .
|
-
- HY-161936
-
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
Z21115 is an orally active inhibitor for phosphodiesterase 4 (PDE4), that inhibits PDE4D7 with IC50 of 10.5 nM. Z21115 inhibits Lipopolysaccharide (HY-D1056)-induced expression of IL-6, TNF-α and iNOS. Z21115 exhibits anti-inflammatory activity in DSS (HY-116282)-induced mouse colitis models without significant toxicity (1 g/kg) .
|
-
- HY-19717S
-
S-[(1E)-1,2-Dichloroethenyl]-L-cysteine-13C3,15N
|
Isotope-Labeled Compounds
|
Inflammation/Immunology
|
DCVC- 13C3, 15N is 15N and 13C labeled DCVC. 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 .
|
-
- HY-107390A
-
|
TNF Receptor
Interleukin Related
IFNAR
|
Inflammation/Immunology
|
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.
|
-
- HY-107390
-
AX-024
1 Publications Verification
|
TNF Receptor
Interleukin Related
IFNAR
|
Inflammation/Immunology
|
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.
|
-
- HY-124151
-
2'-AMP; Adenosine 2'-phosphate; AMP 2'-phosphate
|
Adenosine Receptor
Endogenous Metabolite
|
Neurological Disease
|
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 .
|
-
- HY-128686
-
KAG-308
1 Publications Verification
|
Prostaglandin Receptor
|
Inflammation/Immunology
Endocrinology
|
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 .
|
-
- HY-149984
-
|
Monoamine Oxidase
|
Neurological Disease
Inflammation/Immunology
|
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 .
|
-
- HY-128598
-
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
Cancer
|
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 .
|
-
- HY-149485
-
|
JNK
|
Inflammation/Immunology
|
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 .
|
-
- HY-163368
-
|
HDAC
|
Inflammation/Immunology
|
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 .
|
-
- HY-129113R
-
|
COX
|
Inflammation/Immunology
|
α-Chaconine (Standard) is the analytical standard of α-Chaconine. This product is intended for research and analytical applications. 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 .
|
-
- HY-115351
-
|
TNF Receptor
MMP
|
Inflammation/Immunology
|
GW-3333 is a potent and orally active TNF-alpha-converting enzyme (TACE) and matrix metalloproteinases (MMP) inhibitor. GW-3333 inhibits tumor necrosis factor-alpha (TNF-alpha) production. GW-3333 can be used in research of arthritis .
|
-
- HY-115976
-
|
COX
|
Inflammation/Immunology
|
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 .
|
-
- HY-N0822R
-
|
Chloride Channel
Pyruvate Kinase
NF-κB
TNF Receptor
HIV
AIM2
|
Cancer
|
Shikonin (Standard) is the analytical standard of Shikonin. This product is intended for research and analytical applications. 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 .
|
-
- HY-N0619
-
|
TNF Receptor
Interleukin Related
Tyrosinase
|
Inflammation/Immunology
|
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 .
|
-
- HY-10320A
-
BIRB 796 hydrochloride
|
Autophagy
Raf
p38 MAPK
|
Inflammation/Immunology
|
Doramapimod hydrochloride (BIRB 796 hydrochloride) is an anti-inflammatory compound with biological activity through inhibition of p38 MAPK. Doramapimod hydrochloride can significantly inhibit the activities of TNF-α and IL-1β induced by LPS, LTA and PGN. Doramapimod hydrochloride showed a stronger inhibitory effect on inflammation induced by all three bacterial toxins, which was more significant compared with the effects of other compounds. Doramapimod hydrochloride can be used in the research of autoimmune diseases .
|
-
- HY-162649
-
|
Toll-like Receptor (TLR)
NF-κB
p38 MAPK
|
Inflammation/Immunology
|
TIC10g is a dual inhibitor for toll-like receptor 7 and 9 (TLR7 and TLR9), which inhibits TLR7 and TLR9 mediated TNF-α release in mouse macrophages (IC50 is 14.5 μM and 6.5 μM) and human B lymphocytes (IC50 is 7.69 μM and 11.5 μM). TIC10g inhibits the activation of NF-κB and MAPK, and exhibits anti-inflammatory activity against systemic lupus erythematosus and rheumatoid arthritis .
|
-
- HY-161674
-
|
Monoamine Oxidase
|
Neurological Disease
|
Monoamine Oxidase B inhibitor 4 (compound 1l) is a selective inhibitor of human monoamine oxidase-B (hMAO-B) (IC50=8.3 nM). Monoamine Oxidase B inhibitor 4 also has anti-neuroinflammatory and low neurotoxicity. Monoamine Oxidase B inhibitor 4 can inhibit the release of NO, TNF-α and IL-1β stimulated by LPS and Aβ1-42, and can also attenuate Aβ(1-42)-induced cytotoxicity .
|
-
- HY-N6607R
-
|
Leukotriene Receptor
NO Synthase
NF-κB
COX
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
Cancer
|
Tryptanthrin (Standard) is the analytical standard of Tryptanthrin. This product is intended for research and analytical applications. 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 .
|
-
- HY-N3364
-
|
Flavivirus
Dengue virus
TNF Receptor
NF-κB
NO Synthase
COX
JNK
p38 MAPK
IKK
|
Infection
Inflammation/Immunology
|
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) .
|
-
- HY-155820
-
|
NF-κB
NO Synthase
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
|
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 .
|
-
- HY-155821
-
|
NF-κB
NO Synthase
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
|
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 .
|
-
- HY-122292
-
|
Antibiotic
Bacterial
|
Infection
Inflammation/Immunology
|
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 .
|
-
- HY-N0405R
-
|
TNF Receptor
Interleukin Related
|
Neurological Disease
Cancer
|
Orientin (Standard) is the analytical standard of Orientin. This product is intended for research and analytical applications. 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 .
|
-
- HY-116626
-
|
NF-κB
p38 MAPK
MMP
|
Cancer
|
SM-7368 is a potent NF-kB inhibitor that targets downstream of MAPK p38 activation . SM-7368 inhibits TNF-α-induced MMP-9 upregulation. SM-7368 can be used for the research of chemotherapies targeting TNF-α-mediated tumor invasion and metastasis .
|
-
- HY-101448
-
WAY-171318
|
MMP
Apoptosis
Interleukin Related
TNF Receptor
Caspase
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
TMI-1 (WAY-171318) inhibits TNF converting enzyme (TACE) (IC50 of 8.4 nM), ADAM-TS-4, ADAM-17 and various MMPs with oral activity. TMI-1 significantly suppresses the secretion of TNF-α , alleviating collagen-induced arthritis in mice. TMI-1 inhibits cancer cell proliferation, induces apoptosis through a caspase-dependent pathway. TMI-1 also reverses TRPV1 upregulation and lowers the levels of inflammatory factors (TNF-α、IL-1β、IL-6) in nerve cells, protecting against paclitaxel-induced neurotoxicity. TMI-1 leads to changes in pro-atherogenic lipoprotein profiles, but does not affect the progression of early lesions .
|
-
- HY-162316
-
|
NF-κB
|
Inflammation/Immunology
|
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) .
|
-
- HY-161520
-
|
Glucocorticoid Receptor
NF-κB
|
Inflammation/Immunology
|
Glucocorticoid receptor/NF-κB modulator-1 (Compound 20) is a derivative of ocotillol. Glucocorticoid receptor/NF-κB modulator-1 suppresses the degradation of glucocorticoid receptor (GR) mRNA and GR protein, inhibits the activation of NF-κB signaling pathway. Glucocorticoid receptor/NF-κB modulator-1 downregulates levels of NO, interleukin-6 and tumor necrosis factor-alpha (TNF-α). Glucocorticoid receptor/NF-κB modulator-1 ameliorates sepsis in mouse model .
|
-
- HY-N0619A
-
Mulberroside D
|
TNF Receptor
Interleukin Related
Tyrosinase
|
Inflammation/Immunology
|
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 .
|
-
- HY-115913
-
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
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 .
|
-
- HY-157325
-
|
RIP kinase
|
Inflammation/Immunology
|
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 .
|
-
- HY-162600
-
|
CDK
|
Inflammation/Immunology
|
CDK8-IN-15 (Compound 46) is a potent CDK8 inhibitors with an IC50 value of 57 nM. It can enhance the thermal stability of CDK8 along with inhibition against NF-κB and have favourable selectivity across the CDK family and tyrosine kinase. Additionally, it also demostrates a positive effect in vitro psoriasis model induced by TNF-α and alleviats the inflammatory response enhancing the expression of Foxp3 and IL-10, which is promising for research of psoriasis diseases .
|
-
- HY-162797
-
|
Phosphodiesterase (PDE)
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
|
PDE4-IN-18 (compound 1l) is a PDE4 inhibitor (IC50=1.55 μM) with anti-inflammatory activity. PDE4-IN-18 exerts anti-inflammatory effects by reducing excessive immune cell infiltration and intestinal membrane formation, as well as reducing the mRNA expression of pro-inflammatory cytokines (such as TNF-α and IL-6) in synovial tissue. PDE4-IN-18 can be used in the study of rheumatoid arthritis and psoriasis .
|
-
- HY-144727
-
|
Bacterial
TNF Receptor
|
Infection
Inflammation/Immunology
|
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 .
|
-
- HY-144737
-
|
Bacterial
TNF Receptor
|
Infection
Inflammation/Immunology
|
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 .
|
-
- HY-142958
-
-
- HY-P99782
-
-
- HY-N6969A
-
|
Adrenergic Receptor
|
Cancer
|
Dicentrine hydrochloride is a drug with anti-inflammatory and anti-cancer activity. Dicentrine hydrochloride exerts its effects by enhancing TNF-α-induced apoptosis in A549 lung adenocarcinoma cells. Dicentrine hydrochloride increases caspase-8, -9, -3 and poly(ADP-ribose) polymerase (PARP) activities. Dicentrine hydrochloride inhibits TNF-α-induced invasion and migration of A549 cells. Dicentrine hydrochloride significantly inhibited the TNF-α-activated TAK1, p38, JNK and Akt signaling pathways, and reduced the transcriptional activities of NF-κB and AP-1 .
|
-
- HY-119799
-
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
UK-500001 is an orally active inhibitor for phosphodiesterase 4 (PDE4), which inhibits PDE4D3 (IC50 is 0.28 nM), PDE4B2 (IC50 is 22.8 nM), PDE4A4 (IC50 is 26.1 nM) and PDE4C2 (IC50 is 271 nM). UK-500001 exhibits anti-inflammatory efficacy and inhibits TNF-α and IFN-γ release in human and rodent macrophagic cell lines in nanomolar levels. UK-500001 ameliorates chronic obstructive pulmonary disease (COPD) and asthma .
|
-
- HY-100735
-
-
- HY-N3625
-
Coronalonic acid
|
NF-κB
|
Inflammation/Immunology
|
Coronalolic acid, extract from the apical bud of Gardenia sootepenesis Hutch, inhibits TNF-α-induced NF-κB activity and NO production .
|
-
- HY-147924
-
|
Keap1-Nrf2
NO Synthase
ROS Kinase
|
Inflammation/Immunology
|
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 .
|
-
- HY-N8936
-
|
Others
|
Inflammation/Immunology
|
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)
.
|
-
- HY-130252
-
YQ128
1 Publications Verification
|
NOD-like Receptor (NLR)
Interleukin Related
|
Inflammation/Immunology
|
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.
|
-
- HY-163747
-
|
VEGFR
|
Cancer
|
VEGFR-2-IN-47 (compound 7g) is a potent VEGFR-2 inhibitor with an IC50 value of 0.072 µM. VEGFR-2-IN-47 can induce G2 / M phase cell cycle arrest, promote apoptosis, and boost immunomodulation by downregulating TNF-α expression and upregulating IL-2 levels in MCF-7 cells. VEGFR-2-IN-47 has the potential to be used for the research of cancer such as breast cancer and liver carcinoma .
|
-
- HY-N0619R
-
|
TNF Receptor
Interleukin Related
Tyrosinase
|
Inflammation/Immunology
|
Mulberroside A (Standard) is the analytical standard of Mulberroside A. This product is intended for research and analytical applications. 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 .
|
-
- HY-169004
-
|
TGF-beta/Smad
Interleukin Related
|
Neurological Disease
Inflammation/Immunology
|
CBT-295 is an orally active autotaxin (ATX) inhibitor. CBT-295 exhibits a significant reduction in inflammatory cytokines like TGF-β, TNF-α and IL-6 levels, also reduced bile duct proliferation marker CK-19 and lowered liver fibrosis. The reversal of liver fibrosis with CBT-295 led to a reduction in blood and brain ammonia levels. CBT-295 also reduced neuroinflammation induced by ammonia. CBT-295 is promising for research of liver cirrhosis and associated encephalopathy .
|
-
- HY-156454
-
-
- HY-155243
-
|
DNA/RNA Synthesis
|
Inflammation/Immunology
|
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 .
|
-
- HY-N8816
-
|
NF-κB
|
Inflammation/Immunology
|
Stipuleanoside R2 inhibits NF-κB activation stimulated by TNFα in a dose-dependent manner with IC50 value of 4.1 μM .
|
-
- HY-P10241
-
|
Apoptosis
Caspase
|
Cancer
|
Ac-LEHD-CHO is an inhibitor for caspase 8/9. Ac-LEHD-CHO prevents GalN/TNF-α-induced hepatotoxicity and hepatocyte apoptosis .
|
-
- HY-19744
-
|
MyD88
|
Inflammation/Immunology
|
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 .
|
-
- HY-155199
-
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
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 .
|
-
- HY-N4288
-
|
Glutathione Peroxidase
Cathepsin
Phosphatase
|
Inflammation/Immunology
Cancer
|
4-Methylesculetin is an orally active coumarin derivative, with potent anti-oxidant and anti-inflammatory activities. 4-Methylesculetin inhibits myeloperoxidase activity. 4-Methylesculetin protects bone resorption by reducing the elevated levels of bone-joint exoglycosidases, cathepsin-D and tartrate resistant acid phosphatases. 4-Methylesculetin ameliorats the upregulated non-enzymatic inflammatory markers like TNF-α, IL-1β, IL-6, COX-2 and PGE2, which is promising for research of inflammatory diseases .
|
-
- HY-P99499
-
JNJ 63723283; JNJ 3283
|
PD-1/PD-L1
Interleukin Related
TNF Receptor
|
Cancer
|
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 .
|
-
- HY-155027
-
|
Dipeptidyl Peptidase
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
Cancer
|
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) .
|
-
- HY-139066
-
Trichosanic acid
|
TNF Receptor
GLUT
Proteasome
Tau Protein
PKC
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
Punicic acid is a bioactive compound of pomegranate seed oil. Punicic acid is an isomer of conjugated α-linolenic acid and ω-5 polyunsaturated fatty acids. Punicic acid has anti-inflammatory and antioxidant activities and can inhibit the expression of inflammatory mediators such as tumor necrosis factor α (TNF-α). Punicic acid can also reduce the formation of β-amyloid deposits and hyperphosphorylation of tau by increasing the expression of GLUT4 protein and inhibiting the overactivation of calpain, and is used to prevent and treat neurodegenerative diseases. In addition, punicic acid also has breast cancer inhibitor properties that depend on lipid peroxidation and PKC pathways .
|
-
- HY-155998
-
|
NF-κB
|
Inflammation/Immunology
|
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 .
|
-
- HY-122786
-
|
Antibiotic
HIV
|
Infection
|
3-O-Methylviridicatin is an indole alkaloid. 3-O-Methylviridicatin inhibits TNF-alpha induced HIV replication with an IC50 of 2.5 μM .
|
-
- HY-163748
-
|
GSK-3
|
Inflammation/Immunology
|
GSK-3β inhibitor 17 (compound 5 n) is a potent GSK-3β inhibitor. GSK-3β inhibitor 17 decreases cisplatin (HY-17394) induced p-p65, KIM-1 protein and mRNA expression. GSK-3β inhibitor 17 decreases cisplatin induced TNF-α, IL-1β, IL-6 and MCP-1 mRNA expression. GSK-3β inhibitor 17 shows anti-inflammation effect and has the potential for the research of acute kidney injury .
|
-
- HY-13743
-
Linomide; FCF89; ABR212616
|
TNF Receptor
|
Inflammation/Immunology
|
Roquinimex (Linomide; PNU212616; ABR212616) is a quinoline derivative immunostimulant which increases NK cell activity and macrophage cytotoxicity; inhibits angiogenesis and reduces the secretion of TNF alpha.
|
-
- HY-12348
-
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
LEO 29102 is a potent phosphodiesterase 4 (PDE4) inhibitor with an IC50 value of 5 nM. LEO 29102 inhibits TNFα release. LEO 29102 has the potential for the research of atopic dermatitis .
|
-
- HY-15648F
-
|
Histone Demethylase
|
Cancer
|
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 .
|
-
- HY-146483
-
|
Amyloid-β
|
Neurological Disease
Inflammation/Immunology
|
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) .
|
-
- HY-162641
-
|
IRAK
NF-κB
p38 MAPK
TNF Receptor
|
Inflammation/Immunology
|
AF-45 inhibits IRAK4 and IRAK1, with IC50s of 128 nM and 1765 nM. AF-45 inhibits the release of IL-6 and TNF-α in macrophages, with IC50s of 0.53-1.54 μM and 0.6-2.75 μM. AF-45 is also an inhibitor for NF-κB/MAPK signaling pathway. AF-45 exhibits anti-inflammatory activities against DSS-induced ulcerative colitis and Lipopolysaccharide (HY-D1056)-induced acute lung injury in mouse model. AF-45 exhibits good pharmacokinetic characteristics in rat models .
|
-
- HY-147045
-
-
- HY-160412
-
-
- HY-163102
-
|
Others
|
Inflammation/Immunology
|
IA-14069 is a TNF-alpha inhibitor that exhibits anti-inflammatory properties while also influencing the production of pro-inflammatory cytokines, making it a valuable tool in colon cancer research.
|
-
- HY-132248
-
Lenalidomide 5'-amine
|
TNF Receptor
|
Inflammation/Immunology
|
C5 Lenalidomide (Lenalidomide 5'-amine) is a thalidomide analog and is a potent inhibitor of TNF-alpha production (IC50=100 μM in LPS stimulated human PBMC) .
|
-
- HY-112456
-
|
IKK
|
Inflammation/Immunology
|
IKK2-IN-4 (compound 4) is a potent IKK-2 inhibitor, with an IC50 of 25 nM. IKK2-IN-4 can inhibit the LPS-induced production of TNFα in PBMCs .
|
-
- HY-126026
-
|
NF-κB
|
Inflammation/Immunology
|
NF-κB-IN-17 (Zinc5) is a NF-κB inhibitor. NF-κB-IN-17 inhibits TNF-α-induced NF-κB DNA binding activity in C2C12 cells .
|
-
- HY-N0907
-
-
- HY-108623
-
CP-80,633
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
Atizoram (CP-80,633), a cyclic nucleotide phosphodiesterase (PDE4) inhibitor, elevates plasma cyclic AMP levels and decreases tumor necrosis factor-α (TNFα) production in mice .
|
-
- HY-15648B
-
|
Histone Demethylase
Apoptosis
|
Cancer
|
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 .
|
-
- HY-N0281
-
7,8-Dihydroxycoumarin
|
EGFR
PKA
PKC
Autophagy
Apoptosis
AMPK
Akt
mTOR
Reactive Oxygen Species
Caspase
Bcl-2 Family
PARP
Parasite
|
Inflammation/Immunology
Cancer
|
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 .
|
-
- HY-169103
-
|
NO Synthase
COX
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
Inflammation/Immunology
|
Neuroprotective agent 5 (compound 28) is a brain permeabilizing agent with anti-neuritis, anti-oxidative damage and neuroprotective effects. Neuroprotective agent 5 exhibits a potent NO inhibitory effect (EC50=0.49 μM), inhibits the release of proinflammatory factors PGE2 and TNF-α, downregulates the expression of iNOS and COX-2 proteins, and promotes the polarization of BV-2 cells from the proinflammatory M1 phenotype to the anti-inflammatory M2 phenotype. In addition, Neuroprotective agent 5 can also inhibit acetylcholinesterase (AChE) activity and Aβ42 aggregation in a dose-dependent manner. Neuroprotective agent 5 can be used for the study of Alzheimer's disease .
|
-
- HY-32015
-
|
MAP3K
|
Inflammation/Immunology
|
Cot inhibitor-1 (compound 28) is a selective tumor progression loci-2 (Tpl2) kinase inhibitor with an IC50 of 28 nM. Cot inhibitor-1 shows an inhibition of TNF-alpha production in human whole blood with an IC50 of 5.7 nM .
|
-
- HY-156798
-
ADS032
1 Publications Verification
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
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 .
|
-
- HY-150612
-
|
p38 MAPK
|
Cancer
|
(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 .
|
-
- HY-P0224
-
fMLP; N-Formyl-MLF
|
TNF Receptor
|
Inflammation/Immunology
|
N-Formyl-Met-Leu-Phe (fMLP; N-Formyl-MLF) is a chemotactic peptide and a specific ligand of N-formyl peptide receptor (FPR). N-Formyl-Met-Leu-Ph is reported to inhibit TNF-alpha secretion.
|
-
- HY-N2110
-
|
Akt
|
Inflammation/Immunology
|
Phellopterin is a natural product isolated from Angelica dahurica. Phellopterin reduces TNF-alpha-induced VCAM-1 expression through regulation of the Akt and PKC pathway, which contributes to inhibit the adhesion of monocytes to endothelium .
|
-
- HY-N0906
-
-
- HY-122521
-
|
NF-κB
|
Inflammation/Immunology
|
Sootepin D (compound 6), a triterpene from the apical bud of Gardenia sootepensis, inhibits TNF-α-induced NF-κB activity with an IC50 of 8.3μM. Sootepin D has anti-inflammatory activity .
|
-
- HY-N13184
-
|
TNF Receptor
|
Inflammation/Immunology
|
Giraldoid B is an active ingredient that can be isolated from Girald Daphne Bark. Giraldoid B can inhibit LPS induced NO and b>TNF-α production in RAW264.7 and has anti-inflammatory activity .
|
-
- HY-138063
-
|
TNF Receptor
NF-κB
|
Inflammation/Immunology
|
Siegeskaurolic acid is an orally active anti-inflammatory agent. Siegeskaurolic acid inhibits the productions of nitric oxide (NO), prostaglandin E(2) (PGE(2)), tumor necrosis factor-alpha (TNF-alpha) and the activationon of nuclear factor-kappaB .
|
-
- HY-W010201
-
(±)-Citronellol; (±)-β-Citronellol
|
Reactive Oxygen Species
ERK
PI3K
TNF Receptor
Atg8/LC3
p62
Apoptosis
Necroptosis
Autophagy
Fungal
|
Cardiovascular Disease
Neurological Disease
Cancer
|
Citronellol ((±)-Citronellol) is an orally active inducer of apoptosis. Citronellol can prevent oxidative stress, mitochondrial dysfunction, and apoptosis in the SH-SY5Y cell Parkinson's disease model induced by 6-OHDA by regulating the ROS-NO, MAPK/ERK, and PI3K/Akt signaling pathways. Citronellol can induce necroptosis in human lung cancer cells through the TNF-α pathway and accumulation of ROS. Citronellol can reduce the levels of LC-3 and p62 to regulate the autophagy pathway, inhibit oxidative stress and neuroinflammation, and thus have neuroprotective effects on Parkinson's rats. Citronellol exhibits anti-fungal activity against Trichophyton rubrum by inhibiting ergosterol synthesis .
|
-
- HY-113953
-
|
Caspase
Apoptosis
|
Inflammation/Immunology
|
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 .
|
-
- HY-W082785A
-
-
- HY-N0281R
-
|
EGFR
PKA
PKC
Autophagy
Apoptosis
AMPK
Akt
mTOR
Reactive Oxygen Species
Caspase
Bcl-2 Family
PARP
Parasite
|
Inflammation/Immunology
Cancer
|
Daphnetin (Standard) is the analytical standard of Daphnetin. This product is intended for research and analytical applications. 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-1 , ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research .
|
-
- HY-118157
-
|
Others
|
Inflammation/Immunology
|
3,5,7-Trimethoxyflavone, a flavonoid compound, can inhibit the TNF-α-induced high expression and secretion of MMP-1 by cells. 3,5,7-Trimethoxyflavone can be used to ameliorate skin damage .
|
-
- HY-114221
-
UR13870
|
p38 MAPK
|
Inflammation/Immunology
|
Org 48762-0 is a potent, orally active and selective p38 inhibitor with EC50 of 0.1 μM. Org 48762-0 reduces LPS-induced TNFα release and prevents bone damage in collagen-induced arthritis in mice .
|
-
- HY-B0392
-
-
- HY-155759
-
|
Others
|
Inflammation/Immunology
Cancer
|
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 .
|
-
- HY-N9699
-
|
NF-κB
|
Inflammation/Immunology
|
8α-Hydroxyhirsutinolide is a sesquiterpene lactone. 8α-Hydroxyhirsutinolide inhibits TNF-α-induced NF-κB activity (IC50: 1.9 μM) and NO production. 8α-Hydroxyhirsutinolide can be isolated from Vernonia cinerea .
|
-
- HY-N2055
-
|
Toll-like Receptor (TLR)
NF-κB
TNF Receptor
AMPK
|
Neurological Disease
Inflammation/Immunology
|
Kaempferol 3-O-sophoroside is an orally active derivative of Kaempferol. It exhibits anti-inflammatory, analgesic, and antidepressant effects. Kaempferol 3-O-sophoroside is an inhibitor of the cell surface receptor toll-like receptor (TLR) 2/4 for High mobility group box 1 (HMGB1), and it also exerts anti-inflammatory effects by blocking the activation of NF-κB expression and the production of TNF-α. Kaempferol 3-O-sophoroside promotes the production of brain-derived neurotrophic factor (BDNF) and enhances autophagy by binding to AMP-activated protein kinase (AMPK), thereby exerting antidepressant effects. Kaempferol 3-O-sophoroside holds promise for research in the fields of inflammation and neurodegenerative diseases .
|
-
- HY-N0029
-
|
TNF Receptor
NF-κB
|
Inflammation/Immunology
|
Forsythoside B is a phenylethanoid glycoside isolated from Forsythia suspensa (Thunb.) Vahl, a Chinese folk medicinal plant for treating inflammatory diseases and promoting blood circulation. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB.
|
-
- HY-114592
-
-
- HY-W010201R
-
(±)-Citronellol (Standard); (±)-β-Citronellol (Standard)
|
Reactive Oxygen Species
ERK
PI3K
TNF Receptor
Atg8/LC3
p62
Apoptosis
Necroptosis
Autophagy
Fungal
|
Cardiovascular Disease
Neurological Disease
Cancer
|
Citronellol (Standard) is the analytical standard of Citronellol. Citronellol (Standard) is an orally active inducer of apoptosis. Citronellol (Standard) can prevent oxidative stress, mitochondrial dysfunction, and apoptosis in the SH-SY5Y cell Parkinson's disease model induced by 6-OHDA by regulating the ROS-NO, MAPK/ERK, and PI3K/Akt signaling pathways. Citronellol (Standard) can induce necroptosis in human lung cancer cells through the TNF-α pathway and accumulation of ROS. Citronellol (Standard) can reduce the levels of LC-3 and p62 to regulate the autophagy pathway, inhibit oxidative stress and neuroinflammation, and thus have neuroprotective effects on Parkinson's rats. Citronellol (Standard) exhibits anti-fungal activity against Trichophyton rubrum by inhibiting ergosterol synthesis .
|
-
- HY-14305
-
|
p38 MAPK
|
Inflammation/Immunology
|
BMS-582949 (compound 7k) is an orally active and highly selective p38α MAP kinase inhibitor, with IC50 values of 13 nM for p38α, and 50 nM for cellular TNFα. BMS-582949 can be used for research on rheumatoid arthritis .
|
-
- HY-N6857
-
|
NF-κB
|
Inflammation/Immunology
|
Armepavine, an active compound from Nelumbo nucifera, exerts not only anti-inflammatory effects on human peripheral blood mononuclear cells, but also immunosuppressive effects on T lymphocytes and on lupus nephritic mice. Armepavine inhibits TNF-α-induced MAPK and NF-κB signaling cascades .
|
-
- HY-N0803
-
β-Myrcene
|
NF-κB
|
Others
|
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 .
|
-
- HY-W014049
-
|
NO Synthase
|
Others
|
N'-Nitro-D-arginine, a nitric oxide synthesis inhibitor, also is a vasodilator that relaxes the smooth muscles and increases blood flow to the penis, improving erections. N'-Nitro-D-arginine also inhibits neutrophil migration by blocking receptors for tumour necrosis factor alpha (TNFα) and interleukin 8 (IL8) .
|
-
- HY-18759
-
|
p38 MAPK
TNF Receptor
|
Inflammation/Immunology
|
BMS-751324 is a p38α MAPK inhibitor. BMS-751324 equips a precursor of carbamyl-methyl linkage, containing esters and phosphate functional groups derived from hydroxyphenylacetic acid (HPA). BMS-751324 effectively inhibits foot swelling and LPS-induced TNFα production in an arthritic rat model .
|
-
- HY-W013557
-
3-Hydroxy-xanthen-9-one
|
Integrin
|
Inflammation/Immunology
|
3-Hydroxyxanthone (3-Hydroxy-xanthen-9-one) is a xanthone compound, with . 3-Hydroxyxanthone inhibits NADPH-catalysed lipid peroxidation in human umbilical vein endothelial cells (HUVECs). 3-Hydroxyxanthone also inhibits TNF-alpha induced ICAM-1 expression .
|
-
- HY-161381
-
-
- HY-114766
-
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
Pumafentrine is an orally active, potent dual PDE3/PDE4 inhibitor. Pumafentrine dose-dependently ameliorates the clinical score and colonic TNFα production in murine Dextran sulphate sodium (DSS; HY-116282C)-induced colitis in a preventive setting .
|
-
- HY-N2110R
-
|
Akt
|
Inflammation/Immunology
|
Phellopterin (Standard) is the analytical standard of Phellopterin. This product is intended for research and analytical applications. Phellopterin is a natural product isolated from Angelica dahurica. Phellopterin reduces TNF-alpha-induced VCAM-1 expression through regulation of the Akt and PKC pathway, which contributes to inhibit the adhesion of monocytes to endothelium .
|
-
- HY-153952
-
-
- HY-118101
-
|
Apoptosis
NF-κB
|
Inflammation/Immunology
|
15-Deoxy-Δ12,14-prostaglandin A1 is a deoxyanalog of prostaglandins that inhibits NF-κB signaling and induces apoptosis. 15-Deoxy-Δ12,14-prostaglandin A1 inhibits TNF-α-induced upregulation of inflammatory endothelial cell adhesion molecule (CAM) and avoids monocyte arrest .
|
-
- HY-107427
-
|
MAPKAPK2 (MK2)
p38 MAPK
|
Inflammation/Immunology
|
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 .
|
-
- HY-N10047
-
|
NF-κB
PPAR
|
Cardiovascular Disease
|
7,8-Didehydrocimigenol is an active triterpenoid that can be isolated from Cimicifugae rhizoma. 7,8-Didehydrocimigenol inhibits TNF-α-induced VCAM-1 expression, inhibits NF-kB activity and phosphorylation of ERK1/2 and Akt, increases PPAR-γ expression. 7,8-Didehydrocimigenol can be used for the research of cardiovascular disorders such as atherosclerosis .
|
-
- HY-N0803S
-
β-Myrcene-d6
|
NF-κB
|
Neurological Disease
Cancer
|
Myrcene-d6 is the deuterium labeled Myrcene. 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 .
|
-
- HY-N6857R
-
|
NF-κB
|
Inflammation/Immunology
|
Armepavine (Standard) is the analytical standard of Armepavine. This product is intended for research and analytical applications. Armepavine, an active compound from Nelumbo nucifera, exerts not only anti-inflammatory effects on human peripheral blood mononuclear cells, but also immunosuppressive effects on T lymphocytes and on lupus nephritic mice. Armepavine inhibits TNF-α-induced MAPK and NF-κB signaling cascades .
|
-
- HY-N0803R
-
|
NF-κB
|
Others
|
Myrcene (Standard) is the analytical standard of Myrcene. This product is intended for research and analytical applications. 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 .
|
-
- HY-155179
-
|
PAK
HDAC
|
Cancer
|
ZMF-23 is a PAK1/HDAC6 dual inhibitor. ZMF-23 inhibits PAK1 and HDAC6 regulated aerobic glycolysis and migration. ZMF-23 induces TNF-α-regulated necroptosis, and further enhances apoptosis. ZMF-23 inhibits the Warburg effect and cell migration. ZMF-23 can be used for research of triple-negative breast cancer (TNBC) .
|
-
- HY-109804
-
|
Reactive Oxygen Species
|
Inflammation/Immunology
|
CORM-401 is an oxidant-sensitive CO-releasing molecule. CORM-401 induces NO increase in the regulation of endothelial calcium signalling. CORM-401 reduces TNF-α/CHX and H2O2-induced ROS production. CORM-401 uncouples mitochondrial respiration and inhibits glycolysis .
|
-
- HY-12557
-
|
CaSR
Wnt
TNF Receptor
|
Inflammation/Immunology
|
γ-Glutamylvaline is an activator of CaSR with anti-inflammatory activity. γ-Glutamylvaline inhibits TNF-α-induced proinflammatory cytokine production and increases Wnt5a expression. γ-Glutamylvaline activates calcium-sensing receptor pathways in adipocytes of 3T3-L1 mice and prevents low-grade chronic inflammation .
|
-
- HY-N0029R
-
|
TNF Receptor
NF-κB
|
Inflammation/Immunology
|
Forsythoside B (Standard) is the analytical standard of Forsythoside B. This product is intended for research and analytical applications. Forsythoside B is a phenylethanoid glycoside isolated from Forsythia suspensa (Thunb.) Vahl, a Chinese folk medicinal plant for treating inflammatory diseases and promoting blood circulation. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB.
|
-
- HY-110177
-
|
NF-κB
|
Inflammation/Immunology
|
SP-100030 is a potent NF-κB and activator protein-1 (AP-1) double inhibitor (IC50s=50 and 50 nM, respectively). SP-100030 inhibits IL-2, IL-8, and TNF-alpha production in Jurkat and other T cell lines. SP-100030 decreases murine collagen-induced arthritis (CIA) .
|
-
- HY-N8015S1
-
|
Bacterial
Endogenous Metabolite
Isotope-Labeled Compounds
|
Cancer
|
Octanal-d2 is deuterated labeled Myrcene (HY-N0803). 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 .
|
-
- HY-151966
-
|
PROTACs
IAP
Caspase
|
Cancer
|
TD1092 is a pan-IAP degrader, degrades cIAP1, cIAP2, and XIAP. TD1092 activates Caspase 3/7, and promotes cancer cells apoptosis via IAP degradation. TD1092 inhibits TNFα mediated NF-κB pathway and reduces the phosphorylation of IKK, IkBα, p65, and p38. TD1092 can act as PROTAC, and is used for cancer research .
|
-
- HY-161901
-
|
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
BC-1293 is an inhibitor for E3 ligase subunit FBXO24. BC-1293 disrupts the interaction between FBXO24 and aspartyl-tRNA synthetase (DARS2) and increases the level of DARS2. BC-1293 increases levels of IL-1β, IL-9, MIP-2, and TNF α, and exhibits immunostimulatory activity in mice .
|
-
- HY-18862
-
|
p38 MAPK
|
Inflammation/Immunology
|
PF-03715455 is a potent inhaled p38 MAPK inhibitor. PF-03715455 shows some selectivity for p38α over p38β with respective IC50 values of 0.88 and 23 nM. PF-03715455 potently inhibits LPS-induced TNFα production in human whole blood (IC50=1.7 nM). PF-03715455 has potential for the treatment of COPD (chronic obstructive pulmonary disease) .
|
-
- HY-N3807
-
|
Acyltransferase
ERK
NF-κB
|
Infection
Cardiovascular Disease
Cancer
|
Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 73 μM in an enzyme assay using rat liver microsomes . Enniatin B1 crosss the blood-brain barrier . Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation .
|
-
- HY-P1847
-
|
NF-κB
|
Cancer
|
IKKγ NBD Inhibitory Peptide is a highly specific inhibitor NF-κB inhibitor. IKKγ NBD Inhibitory Peptide acts by disrupting the interaction between IKKγ/NEMO-binding domain (NBD) with IKKα and IKKβ, thus blocking TNF-α-induced NF-kB activation. IKKγ NBD Inhibitory Peptide could significantly suppresses inflammation and ameliorate the cerebral ischemia-induced neurological deficits .
|
-
- HY-N11996
-
|
NO Synthase
NF-κB
|
Others
|
Aloenin aglycone (compound 13) is an NF-κB inhibitor that can be isolated from aloe exudate. Aloenin aglycone inhibits TNFα-induced NF-κB transcriptional activity (IC50: 18.7 μM). Aloenin aglycone (10 μM) also reduced inducible nitric oxide synthase (iNOS) and intercellular adhesion molecule 1 (ICAM-1) gene expression after treatment of HepG2 cells with 10 ng/mL TNFα .
|
-
- HY-151369
-
|
RIP kinase
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
AV123 (compound 12) is a non-cytotoxic RIPK1 inhibitor (IC50=12.12 µM). AV123 blocks the TNF-α-induced necroptotic (EC50=1.7 μM) but not the apoptotic cell death. AV123 can be used in the study of necrotic chronic conditions such as ischemia-reperfusion injury of the brain, heart and kidney, inflammatory diseases, neurodegenerative diseases and infectious diseases .
|
-
- HY-N9541
-
|
Others
|
Inflammation/Immunology
|
Chaetoglobosin Vb is a novel cytotoxic alkaloid with anti-inflammatory and antioxidant activities. Chaetoglobosin Vb can inhibit oxidative stress induced by LPS stimulation, reduce the production of reactive oxygen species and increase the expression of the antioxidant enzyme superoxide dismutase (SOD). Chaetoglobosin Vb significantly reduced the gene and protein expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) induced by LPS, and alleviated the production of proinflammatory cytokines such as TNF-α, IL-6 and IL-1β. Chaetoglobosin Vb exerts its biological activity through the TLR4-mediated MyD88-dependent signaling pathway and the TRIF-dependent signaling pathway, which is specifically manifested by inhibiting the phosphorylation of p38, ERK, and JNK MAPK and the translocation of NF-κB p65 subunit to the nucleus. Chaetoglobosin Vb showed no cytotoxic effect in the concentration range of 25-100 μM and promoted SOD enzyme activity and phosphorylation of p38, ERK1/2 and JNK in a dose-dependent manner .
|
-
- HY-P99252
-
Anti-Human CD6 Recombinant Antibody
|
CD6
|
Infection
Inflammation/Immunology
|
Itolizumab (Anti-Human CD6 Recombinant Antibody) is a humanized recombinant anti-CD6 monoclonal antibody (MAb) targeting the extracellular SRCR distal domain 1 of CD6. Itolizumab reduces T-cell proliferation and inhibits the production of pro-inflammatory cytokines, such as INF-γ, TNFα and IL-6. Itolizumab can be used in the research of psoriasis, rheumatoid arthritis (RA), COVID-19 .
|
-
- HY-P1847A
-
|
NF-κB
|
Inflammation/Immunology
|
IKKγ NBD Inhibitory Peptide TFA is a highly specific inhibitor NF-κB inhibitor. IKKγ NBD Inhibitory Peptide TFA acts by disrupting the interaction between IKKγ/NEMO-binding domain (NBD) with IKKα and IKKβ, thus blocking TNF-α-induced NF-kB activation. IKKγ NBD Inhibitory Peptide TFA could significantly suppresses inflammation and ameliorate the cerebral ischemia-induced neurological deficits .
|
-
- HY-163712
-
|
Estrogen Receptor/ERR
|
Endocrinology
|
17-Epiestriol is an estrogen metabolite and a selective estrogen receptor (ER) β agonist. 17-epiestriol inhibits the mRNA and protein expression of the vascular cell adhesion molecule VCAM-1 induced by tumor necrosis factor α (TNFα). 17-epiestriol also inhibits TNFα-induced VCAM-1 expression and prevents NF-κB migration to the nucleus. 17-Epiestriol also induces the mRNA and protein expression of endothelial nitric oxide synthase .
|
-
- HY-15616
-
|
Melanocortin Receptor
|
Cancer
|
BMS-470539 is a synthetic MC-1R agonist with potent anti-inflammatory properties. BMS-470539 selectively activates human and murine MC-1R with EC50 values ??of 16.8 nM and 11.6 nM, respectively. In vitro studies have shown that BMS-470539 is able to dose-dependently inhibit TNF-alpha-induced NF-kB activation in human melanoma cells expressing MC-1R. In vivo, subcutaneous injection of BMS-470539 into BALB/c mice effectively inhibited LPS-induced TNF-alpha production with an ED50 of approximately 10 μmol/kg and a pharmacodynamic half-life of approximately 8 hours. It also significantly reduced leukocyte infiltration in a lung inflammation model and attenuated paw swelling in a delayed-type hypersensitivity model, highlighting its efficacy as an anti-inflammatory agent through MC-1R modulation .
|
-
- HY-N6796
-
|
Farnesyl Transferase
Ras
Apoptosis
Phospholipase
TNF Receptor
Atg8/LC3
|
Infection
Inflammation/Immunology
Cancer
|
Manumycin A is a polyketide antibiotic and an inhibitor of thioredoxin reductase 1 (TrxR-1). Manumycin A can inhibit the growth of breast cancer cells and exert its anti-tumor activity through LC3. Manumycin A can downregulate the release of pro-inflammatory cytokines in human monocytes stimulated by TNF α, and has potential anti-inflammatory activity. Manumycin A can inhibit the Ras/Raf/ERK1/2 signaling and hnRNP H1 in castration resistant prostate cancer cells to suppress exosome biogenesis and secretion .
|
-
- HY-108642
-
|
p38 MAPK
Casein Kinase
|
Inflammation/Immunology
|
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 .
|
-
- HY-108642B
-
|
p38 MAPK
Casein Kinase
|
Inflammation/Immunology
|
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 .
|
-
- HY-108642A
-
|
p38 MAPK
Casein Kinase
|
Inflammation/Immunology
|
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 .
|
-
- HY-122882
-
|
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
HOIPIN-8 is a potent inhibitor of linear ubiquitin chain assembly complex (LUBAC) with an IC50 of 11 nM. HOIPIN-8 is a HOIPIN-1 derivative with enhanced the potency by 255-fold in the petit-LUBAC inhibition, and 10-fold and 4-fold in the LUBAC- and TNF-α-mediated NF-κB activation, respectively than HOIPIN-1. HOIPIN-1 is a promising tool to explore the cellular functions of LUBAC .
|
-
- HY-P99111
-
CNTO-148
|
TNF Receptor
Apoptosis
Interleukin Related
Caspase
|
Inflammation/Immunology
Cancer
|
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 .
|
-
- HY-161240
-
|
Monoamine Oxidase
|
Neurological Disease
Inflammation/Immunology
|
MAO-B-IN-30 (compound IS7) is a potent, selective and cross the blood-brain barrier MAO-B inhibitor with IC50 values of 19.176, 0.082 µM for MAO-A and MAO-B, respectively. MAO-B-IN-30 shows antiproliferative activity and non-cytotoxic. MAO-B-IN-30 reduces TNF-alpha, IL-6, NF-kB levels. MAO-B-IN-30 has the potential for the research of Parkinson's disease .
|
-
- HY-N0617
-
|
Phosphatase
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
Sanggenon C, a flavonoid, exerts protective effects against cardiac hypertrophy and fibrosis via suppression of the calcineurin/NFAT2 pathway. Sanggenon C inhibits mitochondrial fission to induce apoptosis by blocking the ERK signaling pathway. Sanggenon C inhibits inducible nitric oxide synthase expression in RAW264.7 cells, and TNF-α-stimulated cell adhesion and VCAM-1 expression, by suppressing NF-κB activity. Sanggenon C possesses antioxidant, anti-inflammatory and antitumor activities .
|
-
- HY-124388
-
|
Others
|
Inflammation/Immunology
|
PDE4-IN-20 is a selective submicromolar phosphodiesterase-4 (PDE4) inhibitor with anti-TNF-α properties. PDE4-IN-20 exhibits significant biological activity in vitro and in vivo. The mechanism of action of PDE4-IN-20 is supported by molecular modeling studies, which reveal its binding mode with PDE4. PDE4-IN-20 was optimized in further conformational analysis and showed pharmacological characteristics similar to those of known PDE4 inhibitors .
|
-
- HY-N0194
-
|
Apoptosis
Parasite
|
Inflammation/Immunology
Cancer
|
Asiatic acid, a pentacyclic triterpene found in Centella asiatica (Centella asiatica), has anticancer activity. Asiatic acid induces apoptosis in melanoma cells and has barrier protective effects on human aortic endothelial cells (HAEC). Asiatic acid also has anti-inflammatory activity and inhibits tumor necrosis factor (TNF)-α-induced endothelial barrier dysfunction. Asiatic acid also inhibits NLRP3 inflammasome activation and NF-κB pathway, effectively inhibits inflammation in rats, and has neuroprotective effects in rat spinal cord injury (SCI) model .
|
-
- HY-13453
-
BAY 11-7821
|
IKK
Deubiquitinase
Autophagy
Apoptosis
NF-κB
|
Inflammation/Immunology
Cancer
|
BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells .
|
-
- HY-103490
-
EDHS-206
|
MAP3K
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM) .
|
-
- HY-N10009
-
|
NF-κB
TNF Receptor
COX
ERK
p38 MAPK
Sirtuin
|
Inflammation/Immunology
|
Cudraflavone B is a prenylated flavonoid with anti-inflammatory and anti-tumor properties. Cudraflavone B is also a dual inhibitor of COX-1 and COX-2. Cudraflavone B blocks the translocation of nuclear factor κB (NF-κB) from the cytoplasm to the nucleus in macrophages. Thus, Cudraflavone B inhibits tumor necrosis factor α (TNFα) gene expression and secretion. Cudraflavone B also triggers the mitochondrial apoptotic pathway, activates NF-κB, the MAPK p38, and ERK, and induced the expression of SIRT1. Thus Cudraflavone B inhibits the growth of human oral squamous cell carcinoma cells .
|
-
- HY-N0194R
-
|
Apoptosis
Parasite
|
Inflammation/Immunology
Cancer
|
Asiatic acid (Standard) is the analytical standard of Asiatic acid. This product is intended for research and analytical applications. Asiatic acid, a pentacyclic triterpene found in Centella asiatica (Centella asiatica), has anticancer activity. Asiatic acid induces apoptosis in melanoma cells and has barrier protective effects on human aortic endothelial cells (HAEC). Asiatic acid also has anti-inflammatory activity and inhibits tumor necrosis factor (TNF)-α-induced endothelial barrier dysfunction. Asiatic acid also inhibits NLRP3 inflammasome activation and NF-κB pathway, effectively inhibits inflammation in rats, and has neuroprotective effects in rat spinal cord injury (SCI) model .
|
-
- HY-N0316
-
|
JAK
NF-κB
Reactive Oxygen Species
Apoptosis
VEGFR
c-Myc
|
Cancer
|
Mollugin is an orally active and potent NF-κB inhibitor. Mollugin induces S-phase arrest of HepG2 cells, and increased intracellular reactive oxygen species (ROS) levels. Mollugin induces DNA damage in HepG2 cells, as well as an increase in the expression of p-H2AX. Mollugin shows anti-cancer effect by inhibiting TNF-α-induced NF-κB activation. Mollugin enhances the osteogenic action of BMP-2 (bone morphogenetic protein 2) via the p38-Smad signaling pathway .
|
-
- HY-N0316R
-
|
JAK
NF-κB
Reactive Oxygen Species
Apoptosis
VEGFR
c-Myc
|
Cancer
|
Mollugin (Standard) is the analytical standard of Mollugin. This product is intended for research and analytical applications. Mollugin is an orally active and potent NF-κB inhibitor. Mollugin induces S-phase arrest of HepG2 cells, and increased intracellular reactive oxygen species (ROS) levels. Mollugin induces DNA damage in HepG2 cells, as well as an increase in the expression of p-H2AX. Mollugin shows anti-cancer effect by inhibiting TNF-α-induced NF-κB activation. Mollugin enhances the osteogenic action of BMP-2 (bone morphogenetic protein 2) via the p38-Smad signaling pathway .
|
-
- HY-123882
-
|
Others
|
Others
|
IRAK4-IN-29 is an IRAK4 inhibitor with good selectivity and low nanomolar activity. IRAK4-IN-29 can effectively block the TLR-mediated signal transduction pathway. IRAK4-IN-29 showed significant inhibitory effects in LPS- and R848-induced cytokine experiments. IRAK4-IN-29 can inhibit LPS-induced TNFα in an in vivo model, showing a similar phenotype to IRAK4 gene-deficient mice. IRAK4-IN-29 has good medicinal chemical properties, such as microsomal stability and solubility, showing potential clinical application value .
|
-
- HY-155692
-
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
PDE4-IN-13 is a PDE4 inhibitor with an IC50 of 1.56 μM. PDE4-IN-13 shows anti-inflammatory and antioxidant properties, and can be used for chronic obstructive pulmonary disease (COPD) research .
|
-
- HY-131249
-
|
MAPKAPK2 (MK2)
|
Inflammation/Immunology
|
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 .
|
-
-
-
HY-L177
-
|
896 compounds
|
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 896 antibody inhibitors that can be used for drug development in cancer, immunity, infection and other hot research areas.
|
Cat. No. |
Product Name |
Type |
-
- HY-159669
-
|
Cell Assay Reagents
|
Stercobilin hydrochloride (amixture of isomers) is a bile pigment metabolized by gut bacteria, and it's also an HIV protease inhibitor, with a Ki of 4 μM. Stercobilin hydrochloride (a mixture of isomers) can induce pro-inflammatory activity in mouse macrophage RAW264 cells, including the production of TNF-α and IL-1β. Stercobilin hydrochloride (a mixture of isomers) can be used in studies of inflammation and viral infections .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-118694
-
-
- HY-106359A
-
RDP-58 acetate
|
TNF Receptor
IFNAR
Reactive Oxygen Species
|
Cancer
|
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 .
|
-
- HY-P0224
-
fMLP; N-Formyl-MLF
|
TNF Receptor
|
Inflammation/Immunology
|
N-Formyl-Met-Leu-Phe (fMLP; N-Formyl-MLF) is a chemotactic peptide and a specific ligand of N-formyl peptide receptor (FPR). N-Formyl-Met-Leu-Ph is reported to inhibit TNF-alpha secretion.
|
-
- HY-12557
-
|
CaSR
Wnt
TNF Receptor
|
Inflammation/Immunology
|
γ-Glutamylvaline is an activator of CaSR with anti-inflammatory activity. γ-Glutamylvaline inhibits TNF-α-induced proinflammatory cytokine production and increases Wnt5a expression. γ-Glutamylvaline activates calcium-sensing receptor pathways in adipocytes of 3T3-L1 mice and prevents low-grade chronic inflammation .
|
-
- HY-P1847A
-
|
NF-κB
|
Inflammation/Immunology
|
IKKγ NBD Inhibitory Peptide TFA is a highly specific inhibitor NF-κB inhibitor. IKKγ NBD Inhibitory Peptide TFA acts by disrupting the interaction between IKKγ/NEMO-binding domain (NBD) with IKKα and IKKβ, thus blocking TNF-α-induced NF-kB activation. IKKγ NBD Inhibitory Peptide TFA could significantly suppresses inflammation and ameliorate the cerebral ischemia-induced neurological deficits .
|
-
- HY-P10354
-
-
- HY-106359
-
-
- HY-P10241
-
|
Apoptosis
Caspase
|
Cancer
|
Ac-LEHD-CHO is an inhibitor for caspase 8/9. Ac-LEHD-CHO prevents GalN/TNF-α-induced hepatotoxicity and hepatocyte apoptosis .
|
-
- HY-W014049
-
|
NO Synthase
|
Others
|
N'-Nitro-D-arginine, a nitric oxide synthesis inhibitor, also is a vasodilator that relaxes the smooth muscles and increases blood flow to the penis, improving erections. N'-Nitro-D-arginine also inhibits neutrophil migration by blocking receptors for tumour necrosis factor alpha (TNFα) and interleukin 8 (IL8) .
|
-
- HY-P1847
-
|
NF-κB
|
Cancer
|
IKKγ NBD Inhibitory Peptide is a highly specific inhibitor NF-κB inhibitor. IKKγ NBD Inhibitory Peptide acts by disrupting the interaction between IKKγ/NEMO-binding domain (NBD) with IKKα and IKKβ, thus blocking TNF-α-induced NF-kB activation. IKKγ NBD Inhibitory Peptide could significantly suppresses inflammation and ameliorate the cerebral ischemia-induced neurological deficits .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-108847
-
|
TNF Receptor
Bacterial
|
Inflammation/Immunology
Cancer
|
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 .
|
-
- HY-P99148
-
-
- HY-P99499
-
JNJ 63723283; JNJ 3283
|
PD-1/PD-L1
Interleukin Related
TNF Receptor
|
Cancer
|
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 .
|
-
- HY-P99252
-
Anti-Human CD6 Recombinant Antibody
|
CD6
|
Infection
Inflammation/Immunology
|
Itolizumab (Anti-Human CD6 Recombinant Antibody) is a humanized recombinant anti-CD6 monoclonal antibody (MAb) targeting the extracellular SRCR distal domain 1 of CD6. Itolizumab reduces T-cell proliferation and inhibits the production of pro-inflammatory cytokines, such as INF-γ, TNFα and IL-6. Itolizumab can be used in the research of psoriasis, rheumatoid arthritis (RA), COVID-19 .
|
-
- HY-P99111
-
CNTO-148
|
TNF Receptor
Apoptosis
Interleukin Related
Caspase
|
Inflammation/Immunology
Cancer
|
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 .
|
-
- HY-P99782
-
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
- HY-N0619
-
-
- HY-N6607R
-
-
- HY-N3364
-
-
- HY-122292
-
|
Structural Classification
Animals
Antibiotics
Source classification
|
Antibiotic
Bacterial
|
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 .
|
-
- HY-N0405R
-
-
- HY-N0619A
-
-
- HY-N6969A
-
|
Structural Classification
Alkaloids
Other Alkaloids
Source classification
Stephania epigaea Lo
Plants
Menispermaceae
|
Adrenergic Receptor
|
Dicentrine hydrochloride is a drug with anti-inflammatory and anti-cancer activity. Dicentrine hydrochloride exerts its effects by enhancing TNF-α-induced apoptosis in A549 lung adenocarcinoma cells. Dicentrine hydrochloride increases caspase-8, -9, -3 and poly(ADP-ribose) polymerase (PARP) activities. Dicentrine hydrochloride inhibits TNF-α-induced invasion and migration of A549 cells. Dicentrine hydrochloride significantly inhibited the TNF-α-activated TAK1, p38, JNK and Akt signaling pathways, and reduced the transcriptional activities of NF-κB and AP-1 .
|
-
- HY-N3625
-
-
- HY-N8936
-
-
- HY-N0619R
-
-
- HY-N8816
-
-
- HY-N4288
-
-
- HY-P99499
-
-
- HY-139066
-
-
- HY-N0907
-
-
- HY-N0281
-
7,8-Dihydroxycoumarin
|
Structural Classification
Daphne
Classification of Application Fields
Thymelaeaceae
Source classification
Coumarins
Phenols
Polyphenols
Phenylpropanoids
Plants
Disease Research Fields
Cancer
|
EGFR
PKA
PKC
Autophagy
Apoptosis
AMPK
Akt
mTOR
Reactive Oxygen Species
Caspase
Bcl-2 Family
PARP
Parasite
|
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 .
|
-
- HY-N2110
-
-
- HY-N0906
-
-
- HY-122521
-
-
- HY-N13184
-
-
- HY-138063
-
-
- HY-W010201
-
-
- HY-N0281R
-
|
Structural Classification
Daphne
Thymelaeaceae
Source classification
Coumarins
Phenols
Polyphenols
Phenylpropanoids
Plants
|
EGFR
PKA
PKC
Autophagy
Apoptosis
AMPK
Akt
mTOR
Reactive Oxygen Species
Caspase
Bcl-2 Family
PARP
Parasite
|
Daphnetin (Standard) is the analytical standard of Daphnetin. This product is intended for research and analytical applications. 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-1 , ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research .
|
-
- HY-118157
-
-
- HY-N9699
-
-
- HY-N2055
-
-
- HY-N0029
-
-
- HY-W010201R
-
-
- HY-N6857
-
-
- HY-N0803
-
-
- HY-N2110R
-
-
- HY-N10047
-
-
- HY-N6857R
-
-
- HY-N0803R
-
-
- HY-N0029R
-
-
- HY-N3807
-
-
- HY-N11996
-
-
- HY-N9541
-
|
Structural Classification
Alkaloids
Microorganisms
Pyrrole Alkaloids
Source classification
|
Others
|
Chaetoglobosin Vb is a novel cytotoxic alkaloid with anti-inflammatory and antioxidant activities. Chaetoglobosin Vb can inhibit oxidative stress induced by LPS stimulation, reduce the production of reactive oxygen species and increase the expression of the antioxidant enzyme superoxide dismutase (SOD). Chaetoglobosin Vb significantly reduced the gene and protein expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) induced by LPS, and alleviated the production of proinflammatory cytokines such as TNF-α, IL-6 and IL-1β. Chaetoglobosin Vb exerts its biological activity through the TLR4-mediated MyD88-dependent signaling pathway and the TRIF-dependent signaling pathway, which is specifically manifested by inhibiting the phosphorylation of p38, ERK, and JNK MAPK and the translocation of NF-κB p65 subunit to the nucleus. Chaetoglobosin Vb showed no cytotoxic effect in the concentration range of 25-100 μM and promoted SOD enzyme activity and phosphorylation of p38, ERK1/2 and JNK in a dose-dependent manner .
|
-
- HY-N6796
-
-
- HY-N0617
-
-
- HY-N0194
-
-
- HY-N10009
-
|
Structural Classification
Brosimopsis oblongifolia
Source classification
Phenols
Polyphenols
Plants
Moraceae
|
NF-κB
TNF Receptor
COX
ERK
p38 MAPK
Sirtuin
|
Cudraflavone B is a prenylated flavonoid with anti-inflammatory and anti-tumor properties. Cudraflavone B is also a dual inhibitor of COX-1 and COX-2. Cudraflavone B blocks the translocation of nuclear factor κB (NF-κB) from the cytoplasm to the nucleus in macrophages. Thus, Cudraflavone B inhibits tumor necrosis factor α (TNFα) gene expression and secretion. Cudraflavone B also triggers the mitochondrial apoptotic pathway, activates NF-κB, the MAPK p38, and ERK, and induced the expression of SIRT1. Thus Cudraflavone B inhibits the growth of human oral squamous cell carcinoma cells .
|
-
- HY-N0194R
-
|
Triterpenes
Structural Classification
Terpenoids
Source classification
Tagetes lucida Cav.
Umbelliferae
Plants
|
Apoptosis
Parasite
|
Asiatic acid (Standard) is the analytical standard of Asiatic acid. This product is intended for research and analytical applications. Asiatic acid, a pentacyclic triterpene found in Centella asiatica (Centella asiatica), has anticancer activity. Asiatic acid induces apoptosis in melanoma cells and has barrier protective effects on human aortic endothelial cells (HAEC). Asiatic acid also has anti-inflammatory activity and inhibits tumor necrosis factor (TNF)-α-induced endothelial barrier dysfunction. Asiatic acid also inhibits NLRP3 inflammasome activation and NF-κB pathway, effectively inhibits inflammation in rats, and has neuroprotective effects in rat spinal cord injury (SCI) model .
|
-
- HY-N0316
-
-
- HY-N0316R
-
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-12085S
-
|
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].
|
-
-
- HY-N8593S
-
|
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].
|
-
-
- HY-19717S
-
|
DCVC- 13C3, 15N is 15N and 13C labeled DCVC. 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 .
|
-
-
- HY-N0803S
-
|
Myrcene-d6 is the deuterium labeled Myrcene. 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 .
|
-
-
- HY-N8015S1
-
|
Octanal-d2 is deuterated labeled Myrcene (HY-N0803). 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 .
|
-
Cat. No. |
Product Name |
|
Classification |
-
- HY-130252
-
YQ128
1 Publications Verification
|
|
Alkynes
|
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.
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- HY-148908
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Azide
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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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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Cat. No. |
Product Name |
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Classification |
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- HY-154698
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Nucleosides and their Analogs
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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 .
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