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Pro-inflammatory transcriptional

" in MedChemExpress (MCE) Product Catalog:

28

Inhibitors & Agonists

5

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B1060
    Methylprednisolone succinate sodium
    2 Publications Verification

    Methylprednisolone hydrogen succinate sodium

    Glucocorticoid Receptor Infection Neurological Disease Inflammation/Immunology Cancer
    Methylprednisolone succinate (Methylprednisolone hydrogen succinate) sodium is a prodrug of Methylprednisolone (HY-B0260) and glucocorticoid with immunosuppressant and anti-inflammatory activity. Methylprednisolone succinate sodium binds cytosolic glucocorticoid receptors, translocates to nuclei, and modulates target gene transcription. Methylprednisolone succinate sodium alters Bax, Bcl-2, occludin, and ZO-1 expression; attenuates TLR4/NF-κB signaling; suppresses proinflammatory cytokine production and immune cell activation. Methylprednisolone succinate sodium can be used for the research of intracranial haemorrhage, rheumatoid arthritis, multiple sclerosis, preterminal cancer, inflammatory conditions, shock, immediate-type hypersensitivity, acute myocardial ischemia, hypoxic heart muscle damage, and traumatic spinal cord injury .
    Methylprednisolone succinate sodium
  • HY-175759

    Molecular Glues IFNAR Inflammation/Immunology
    EN1033 is a covalent immune regulatory transcription factor 5/8 (IRF5/8) molecular glue degrader. EN1033 degrades IRF5 in a proteasome-dependent manner. EN1033 engages and degrades IRF8 more robustly and rapidly. EN1033 covalently targets C28 and C223 to destabilize and degrade IRF5 and IRF8 respectively, thereby inhibiting their pro-inflammatory transcriptional activity. EN1033 serves as a promising tool for the study of autoimmune and inflammatory disorders .
    EN1033
  • HY-112671

    RTA dh404

    Keap1-Nrf2 NF-κB Apoptosis Cardiovascular Disease Inflammation/Immunology
    CDDO-dhTFEA (RTA dh404) is a synthetic oleanane triterpenoid compound which potently activates Nrf2 and inhibits the pro-inflammatory transcription factor NF-κB . CDDO-dhTFEA restores hypertension (MAP), increases Nrf2 and expression of its target genes, attenuates activation of NF-κB and transforming growth factor-β pathways, and reduces glomerulosclerosis, interstitial fibrosis and inflammation in the chronic kidney disease (CKD) rats .
    CDDO-dhTFEA
  • HY-N0807
    Swertiamarin
    1 Publications Verification

    MMP NF-κB JAK Keap1-Nrf2 Metabolic Disease Inflammation/Immunology Cancer
    Swertiamarin is an orally active natural product with hypoglycemic, lipid-lowering, anti-rheumatic, and antioxidant activities. Swertiamarin can regulate the levels of pro-inflammatory cytokines, MMP, and NF-κB, and promote osteoblast proliferation. Swertiamarin has antioxidant and hepatoprotective effects against carbon tetrachloride induced rat liver toxicity through the Nrf2/HO-1 pathway. Swertiamarin can attenuate inflammatory mediators by regulating JAK2/STAT3 transcription factors in adjuvant induced arthritis rats. Swertiamarin can be used in the research of diabetes and arthritis .
    Swertiamarin
  • HY-B1900
    Methylprednisolone succinate
    2 Publications Verification

    Methylprednisolone hydrogen succinate

    Glucocorticoid Receptor Bacterial Toll-like Receptor (TLR) NF-κB Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Methylprednisolone succinate (Methylprednisolone hydrogen succinate) is a prodrug of Methylprednisolone (HY-B0260) and glucocorticoid with immunosuppressant and anti-inflammatory activity. Methylprednisolone succinate binds cytosolic glucocorticoid receptors, translocates to nuclei, and modulates target gene transcription. Methylprednisolone succinate alters Bax, Bcl-2, occludin, and ZO-1 expression; attenuates TLR4/NF-κB signaling; suppresses proinflammatory cytokine production and immune cell activation. Methylprednisolone succinate can be used for the research of intracranial haemorrhage, rheumatoid arthritis, multiple sclerosis, preterminal cancer, inflammatory conditions, shock, immediate-type hypersensitivity, acute myocardial ischemia, hypoxic heart muscle damage, and traumatic spinal cord injury .
    Methylprednisolone succinate
  • HY-N12586

    ERK Reactive Oxygen Species (ROS) COX PGE synthase STAT HCV HCV Protease Infection Neurological Disease Cancer
    Pheophytin a is a multi-target inhibitor, anticancer agent, antioxidant and antiviral agent. Pheophytin a directly binds to and inhibits HCV-NS3/4A protease (IC50=0.89 μM) to block viral replication. Pheophytin a also scavenges free radicals, reduces ferric ions, and exhibits cytotoxic activity against breast cancer cells. Pheophytin a effectively inhibits LPS-induced production of nitric oxide, prostaglandin E2, NOS2 and COX-2, as well as various pro-inflammatory cytokines, by downregulating the transcription levels of inflammatory mediators and blocking the ERK1/2 and STAT-1 pathways. In a low nerve growth factor environment, Pheophytin a also enhances ERK1/2 phosphorylation and synergistically promotes neurite outgrowth through MAPK pathway. Pheophytin a can be used to investigate the pathogenic mechanisms of diseases including chronic hepatitis C, sepsis, breast cancer and Alzheimer's disease .
    Pheophytin a
  • HY-B0327
    Irsogladine
    3 Publications Verification

    Dicloguamine

    Phosphodiesterase (PDE) NF-κB AP-1 TRP Channel Interleukin Related Inflammation/Immunology Cancer
    Irsogladine (Dicloguamine) is an orally active gastric mucosal protective agent. Irsogladine inhibits breast cancer recurrence and lung metastasis in nude mice . Irsogladine inhibits the transcriptional activities of NF-κB and AP-1, suppresses the activities of PDE and PDE4 to elevate intracellular cAMP levels, and activates TRPV1 and KATP channels. Irsogladine enhances iNOS expression, NO production, and the activation of cAMP-responsive elements. Irsogladine inhibits the development and progression of intestinal polyps in Apc-mutant mice. Irsogladine alleviates oxidative stress, increases gastric mucosal blood flow, and stimulates the production of endogenous prostaglandins. Irsogladine promotes insulin secretion in MIN6 cells. Irsogladine inhibits tumor angiogenesis, cancer cell proliferation, and the production of proinflammatory cytokines. Irsogladine exerts protective effects on astrocytes in ethanol/hydrochloric acid-induced gastric ulcers in mice. Irsogladine prevents colitis in IL-10 gene-deficient mice by reducing the production of IL-12 and IL-23. Irsogladine upregulates gap junction intercellular communication in pancreatic cancer cells via the PKA pathway. Irsogladine is applicable to research related to breast cancer, intestinal polyposis, gastric ulcer, spontaneous colitis, glioma, liver cancer, and pancreatic cancer [5][6] .
    Irsogladine
  • HY-160222

    HSV STING IFNAR NF-κB Infection
    HSV-60mer sodium is a 60 bp double-stranded DNA oligonucleotide derived from the HSV-1 genome, and also an IFNβ inducer. HSV-60mer sodium colocalizes with endogenous cytoplasmic IFI16 in immune cells. HSV-60mer sodium activates the transcription factors IRF3 and NF-κB, induces the production of proinflammatory cytokines, and inhibits HSV-1 replication in immune cells. HSV-60mer sodium can be used in studies related to herpes simplex virus type 1 infection .
    HSV-60mer sodium
  • HY-159647B

    Molecular Glues IKZF Family Cancer
    (1S,2S,3R)-PLX-4545 is the (1S,2S,3R) enantiomer of PLX-4545 (HY-159647). PLX-4545 is an orally active and selective cereblon-based molecular glue degrader of IKZF2 (zinc finger transcription factor Helios). PLX-4545 can reprogram immunosuppressive regulatory T cells into pro-inflammatory effector T cells, thereby enhancing anti-tumor immune responses .
    (1S,2S,3R)-PLX-4545
  • HY-N0902

    13,14-Dihydrosanguinarine

    Fungal Bacterial Interleukin Related Infection Inflammation/Immunology
    Dihydrosanguinarine (13,14-Dihydrosanguinarine) is an alkaloid with antibacterial and anti-inflammatory activities, and also an important precursor of Sanguinarine (HY-N0052). Dihydrosanguinarine targets and regulates the TNF/IL-17/PI3K signaling pathway, downregulates the levels of pro-inflammatory factors such as IL-17A, TNF-α and IL-6, upregulates the expression of TGF-β, inhibits myeloperoxidase activity, and regulates the transcription of multiple inflammation-related genes. Dihydrosanguinarine exhibits antibacterial activity against a variety of oral microorganisms. Dihydrosanguinarine can be used in research related to liver inflammation and oral flora dysbiosis .
    Dihydrosanguinarine
  • HY-101318
    β-Funaltrexamine hydrochloride
    2 Publications Verification

    β-FNA hydrochloride

    Opioid Receptor p38 MAPK STAT NF-κB NO Synthase Toll-like Receptor (TLR) Cardiovascular Disease Neurological Disease
    β-Funaltrexamine (β-FNA) hydrochloride is a blood-brain barrier-permeable, selective and irreversible μ-opioid receptor antagonist with immunomodulatory, anti-inflammatory and neuroprotective activities. β-Funaltrexamine hydrochloride inhibits p38 MAPK and TLR4 signaling by blocking μ-opioid receptors, and reduces the transcriptional activities of NF-κB, AP-1, CREB and Stat. Furthermore, β-Funaltrexamine hydrochloride inhibits iNOS activation and pro-inflammatory microglial polarization, converting microglia to an anti-inflammatory phenotype, thereby downregulating neuroinflammation and ameliorating neuronal degeneration. β-Funaltrexamine hydrochloride is widely applicable to research related to stroke, cerebral ischemia/reperfusion injury and neurodegenerative diseases .
    β-Funaltrexamine hydrochloride
  • HY-B1900R
    Methylprednisolone succinate (Standard)
    1 Publications Verification

    Methylprednisolone hydrogen succinate (Standard)

    Reference Standards Glucocorticoid Receptor Bacterial Toll-like Receptor (TLR) NF-κB Metabolic Disease Inflammation/Immunology Cancer
    Methylprednisolone succinate (Standard) is the analytical standard of Methylprednisolone succinate (HY-B1900). This product is intended for research and analytical applications. Methylprednisolone succinate (Methylprednisolone hydrogen succinate) is a prodrug of Methylprednisolone (HY-B0260) and glucocorticoid with immunosuppressant and anti-inflammatory activity. Methylprednisolone succinate binds cytosolic glucocorticoid receptors, translocates to nuclei, and modulates target gene transcription. Methylprednisolone succinate alters Bax, Bcl-2, occludin, and ZO-1 expression; attenuates TLR4/NF-κB signaling; suppresses proinflammatory cytokine production and immune cell activation. Methylprednisolone succinate can be used for the research of intracranial haemorrhage, rheumatoid arthritis, multiple sclerosis, preterminal cancer, inflammatory conditions, shock, immediate-type hypersensitivity, acute myocardial ischemia, hypoxic heart muscle damage, and traumatic spinal cord injury .
    Methylprednisolone succinate (Standard)
  • HY-162152

    Keap1-Nrf2 Inflammation/Immunology
    biKEAP1 (compound 3) is an inhibitor targeting the dimerKEAP1. biKEAP1 binds to cellular KEAP1 dimers and releases the NRF2 protein sequestered by KEAP1, resulting in immediate activation of NRF2. biKEAP1 also promotes nuclear translocation of NRF2 and directly inhibits proinflammatory cytokine transcription. biKEAP1 can reduce acute inflammation and reduce inflammatory damage in acute inflammation models .
    biKEAP1
  • HY-124404

    Aryl Hydrocarbon Receptor Na+/K+ ATPase Prostaglandin Receptor Inflammation/Immunology
    12(R)-HETE is a CYP-dependent arachidonic acid metabolite that acts as a proinflammatory lipid mediator. 12 (R)-HETE widely exists in various tissues including the eye, skin and liver. In the cornea, 12(R)-HETE is metabolized via pathways such as β-oxidation into the precursor of 12(R)-HETrE. Without direct receptor binding, 12(R)-HETE indirectly activates AHR-mediated target gene transcription, while inhibiting the enzymatic activity of Na+,K+-ATPase and the intracellular calcium elevation induced by TP agonists. 12(R)-HETE also possesses multiple physiological effects such as chemotaxis, proangiogenesis, vasodilation, natriuresis, diuresis and intraocular pressure reduction, and can be widely used in studies related to psoriasis, inflammatory skin diseases and ocular inflammation .
    12(R)-HETE
  • HY-171591

    Salt-inducible Kinase (SIK) Interleukin Related TNF Receptor Infection
    SIK2-IN-4 (Compound 4) is a highly selective SIK1/2 inhibitor (IC50s 0.143 and 0.076 μM, respectively). SIK2-IN-4 reduces the phosphorylation of transcription coactivator 3 (CRTC3) by targeting SIK1/2, thereby regulating cAMP response element binding protein (CREB)-dependent transcriptional activity. SIK2-IN-4 inhibits the production of pro-inflammatory cytokines such as TNF (IC50: 0.11 µM), IL-12/23 p40 (IC50: 0.25 µM), and IL-23 (IC50: 0.47 µM), while inducing the expression of the anti-inflammatory cytokine IL-10. SIK2-IN-4 can be used to study intestinal inflammation and other chronic inflammatory diseases .
    SIK2-IN-4
  • HY-14353

    LXR Neurological Disease Inflammation/Immunology
    GSK-9772 is a Liver X Receptor (LXR) modulator of the N-phenyl tertiary amine class (NPTAs) with high affinity for LXR β ligand (IC50=30 nM). GSK-9772 has anti-inflammatory activity by binding to LXR, specifically by interacting with the region associated with the transcriptional repression function of the receptor, thereby inhibiting the expression of pro-inflammatory genes. GSK-9772 can be used in the study of inflammatory and neurodegenerative diseases .
    GSK-9772
  • HY-N15347

    NF-κB p38 MAPK Interleukin Related TNF Receptor NO Synthase COX Inflammation/Immunology
    Talaromyketide B is a polyketide compound with anti-inflammatory activity, discovered in the soil bacterium Talaromyces sp. KYS-41. Talaromyketide B inhibits the activation of the NF-κB and MAPK signaling pathways and dose-dependently suppresses pro-inflammatory cytokines, such as IL-1β, IL-6, IL-10, and TNF-α, as well as the transcriptional activity of inflammatory mediators, including iNOS and COX-2. Talaromyketide B holds potential for research in the fields of immunity and inflammatory diseases .
    Talaromyketide B
  • HY-175782

    Toll-like Receptor (TLR) NF-κB p38 MAPK Inflammation/Immunology
    SMU-R39 is a TLR7 and TLR8 antagonist with IC50 values of 3.22 μM and 0.24 μM, respectively. SMU-R39 binds to recombinant mTLR7 protein (KD = 2.36 μM) and to recombinant hTLR8 protein (KD = 105 nM). SMU-R39 suppresses downstream NF-κB and MAPK signaling, and reduces secretion/transcription of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) in PBMCs and THP-1 cells. SMU-R39 demonstrates anti-inflammatory efficacy in Imiquimod (IMQ) (HY-B0180)-induced psoriasis mouse model. SMU-R39 can be used for the study of autoimmune diseases such as psoriasis .
    SMU-R39
  • HY-146564

    NF-κB Inflammation/Immunology
    R-HP210 acts on the NF-κB mediated tethered transrepression function (IC50=3.80 μM). R-HP210 represses the LPS-induced transcription of a variety of proinflammatory genes such as IL-1β, IL-6 and COX-2. R-HP210 does not induce the transactivation functions of Glucocorticoids (GCs) .
    R-HP210
  • HY-146561

    Glucocorticoid Receptor NF-κB Inflammation/Immunology
    S-HP210 is a potent and selective glucocorticoid receptor (GR) with an IC50 value of 1.92 μM for NF-κB transrepression (TR). S-HP210 represses the LPS-induced transcription of a variety of proinflammatory genes such as IL-1β, IL-6 and COX-2. S-HP210 is nontoxic at effective doses against mouse fibroblasts 3T3 cells .
    S-HP210
  • HY-105854A

    Ras MEK ERK PI3K Akt MMP Keap1-Nrf2 Heme Oxygenase (HO) Reactive Oxygen Species (ROS) Apoptosis Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
    Pipoxolan is an orally active smooth muscle relaxant, anti-inflammatory agent and anticancer agent. Pipoxolan modulates PI3K/AKT signaling pathways, and reduces the levels of Ras/MEK/p-ERK, MMP-2 and MMP-9. Pipoxolan inhibits pro-inflammatory transcription factor pathways, activates Nrf2/HO-1, and suppresses the production of pro-inflammatory mediators. Pipoxolan induces ROS generation, endogenous mitochondrial Apoptosis, and G0/G1 cell cycle arrest. Pipoxolan reduces cerebral infarction size and inhibits intimal hyperplasia. Pipoxolan can be used in research related to cerebral ischemia, intimal hyperplasia, oral squamous cell carcinoma, leukemia and lung cancer .
    Pipoxolan
  • HY-16362

    PG 490-88Na

    Apoptosis TGF-β Receptor NF-κB Interleukin Related IFNAR TNF Receptor Inflammation/Immunology
    Omtriptolide sodium (PG490-88Na) is a derivative of Triptolide (HY-32735). Omtriptolide sodium exhibits significant immunosuppressive, anti-fibrotic and anti-inflammatory properties. The mechanism of action of Omtriptolide sodium is diverse, including inhibiting T cell activation and proliferation, inducing T cell apoptosis (apoptosis), blocking fibroblast maturation/proliferation, inhibiting TGF-β mRNA expression, and suppressing pro-inflammatory cytokines (such as IL-2, IFN-γ, TNF-α) by blocking transcription factors such as NF-κB. Omtriptolide sodium can be used for research on obstructive airway diseases, pulmonary fibrosis and graft-versus-host disease .
    Omtriptolide sodium
  • HY-160938

    β-FNA

    Opioid Receptor STAT NF-κB Toll-like Receptor (TLR) NO Synthase p38 MAPK Cardiovascular Disease Neurological Disease
    β-Funaltrexamine (β-FNA) is a blood-brain barrier-permeable, selective and irreversible μ-opioid receptor antagonist with immunomodulatory, anti-inflammatory and neuroprotective activities. β-Funaltrexamine inhibits p38 MAPK and TLR4 signaling by blocking μ-opioid receptors, and reduces the transcriptional activities of NF-κB, AP-1, CREB and Stat. Furthermore, β-Funaltrexamine inhibits iNOS activation and pro-inflammatory microglial polarization, converting microglia to an anti-inflammatory phenotype, thereby downregulating neuroinflammation and ameliorating neuronal degeneration. β-Funaltrexamine is widely applicable to research related to stroke, cerebral ischemia/reperfusion injury and neurodegenerative diseases .
    β-Funaltrexamine
  • HY-10540

    AEB071 acetate

    PKC NF-κB Inflammation/Immunology
    Sotrastaurin (AEB071) acetate is a selective, orally active PKC inhibitor. Sotrastaurin acetate inactivates NF-κB by inhibiting PKC α, β, θ, γ subtypes, thereby reducing the transcription levels of immune response-related genes. Sotrastaurin acetate effectively inhibits alloreactive T cell proliferation, conventional T cell activation, as well as the production of pro-inflammatory cytokines and B lymphocytes. Sotrastaurin acetate also maintains the functional and phenotypic stability of regulatory T cells, enhances Foxp3 expression and restores the balance of helper T lymphocytes. Sotrastaurin acetate can prolong the survival time of allografts, and alleviate inflammatory responses and myasthenic symptoms by reducing anti-AChR antibody levels. Sotrastaurin acetate is widely used in studies related to kidney transplantation, psoriasis and myasthenia gravis .
    Sotrastaurin acetate
  • HY-183370

    JAK STAT Interleukin Related Inflammation/Immunology
    JAK2/STAT3-IN-2 is an orally active JAK2/STAT3 inhibitor. JAK2/STAT3-IN-2 inhibits the phosphorylation of tyrosine residues in JAK2 and STAT3, blocks downstream signal transduction, disrupts the dimerization and nuclear translocation of STAT3, and suppresses pro-inflammatory transcriptional activity. JAK2/STAT3-IN-2 inhibits the expression of IL-17A and IL-17F, reduces immune cell infiltration, and inhibits the production of NO simultaneously. JAK2/STAT3-IN-2 exerts a protective effect in a mouse model of ulcerative colitis induced by DSS (HY-116282C). JAK2/STAT3-IN-2 can be used for the research of ulcerative colitis .
    JAK2/STAT3-IN-2
  • HY-N18952

    Interleukin Related Inflammation/Immunology
    Heparin disaccharide II-S trisodium (Compound HSH-9) is a heparin-derived disaccharide. Heparin disaccharide II-S trisodium inhibits the spontaneous secretion of proinflammatory mediators IL-8 and IL-1β in intestinal epithelial cells at the post-transcriptional stage .
    Heparin disaccharide II-S trisodium
  • HY-183326

    IDMF

    Keap1-Nrf2 Inflammation/Immunology
    Isosorbide di-(methyl fumarate) (IDMF), topical DMF (HY-17363) derivative, is an NRF2/ARE pathway activator. Isosorbide di-(methyl fumarate) downregulates ANCR targets, modulates epithelial differentiation, represses proinflammatory cytokine genes, IL-17A- and TNF-induced keratinocyte genes, psoriatic skin lesion-specific genes, and immune response genes. Isosorbide di-(methyl fumarate) stimulates oxidative stress response gene transcription, reduces erythema and scaling in Imiquimod (HY-B0180)-induced psoriasiform lesions. Isosorbide di-(methyl fumarate) exhibits no genotoxicity or radiation sensitivity in skin fibroblasts, is nonirritating and nonsensitizing in rodent models. Isosorbide di-(methyl fumarate) can be used for the research of psoriasis vulgaris .
    Isosorbide di-(methyl fumarate)
  • HY-183905

    11β-HSD Glucocorticoid Receptor Reactive Oxygen Species (ROS) Keap1-Nrf2 Neurological Disease
    KR-67607 is a selective 11β-HSD1 inhibitor, with an IC50 value of 4.8 nM against h11β-HSD1 and 7.1 nM against mouse 11β-HSD1. KR-67607 inhibits stress-induced Glucocorticoid receptor nuclear translocation, reduces cortisol levels, suppresses the expression of ROS and proinflammatory cytokines, and enhances Nrf-2-mediated antioxidant gene transcription. KR-67607 maintains trabecular meshwork structure and reverses elevated intraocular pressure. KR-67607 improves ocular antioxidant activity and mucus secretion, reverses ocular surface damage, and prevents ischemia-reperfusion induced ocular injury. KR-67607 can be used in research related to glaucoma and dry eye disease .
    KR-67607

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