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Results for "

Pro-inflammatory transcriptional

" in MedChemExpress (MCE) Product Catalog:

12

Inhibitors & Agonists

2

Natural
Products

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-159647
    PLX-4545

    		Molecular Glues IKZF Family Cancer
    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 .
    PLX-4545
  • HY-112671
    CDDO-dhTFEA

    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

    		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-146564
    R-HP210

    		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-175759
    EN1033

    		Interleukin Related CCR Inflammation/Immunology
    EN1033 is a covalent Immune regulatory transcription factor 5/8 (IRF5/8) degrader. EN1033 destabilizes and degrades IRF5 and IRF8 by covalently targeting cysteine residues C28 and C223, respectively, inhibiting their pro-inflammatory transcriptional activity, such as the reduced mRNA level of IL1A, IL1B and CCL2. EN1033 can be used for autoimmune and inflammatory diseases research .
    EN1033
  • HY-14353
    GSK-9772

    		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
    Talaromyketide B

    		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-159647B
    (1S,2S,3R)-PLX-4545

    		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-171591
    SIK2-IN-4

    		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-175782
    SMU-R39

    		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-162152
    biKEAP1

    		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-146561
    S-HP210

    		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

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