(R)-STU104

CAS No. 2767124-77-4

(R)-STU104( —— )

Catalog No. M35452 CAS No. 2767124-77-4

(R)-STU104 is a novel TAK1-MKK3 protein-protein interaction (PPI) inhibitor that inhibits TNF-α and suppresses the TAK1/MKK3/p38/MnK1/MK2/elF4E signalling pathway by binding to MKK3 and disrupting TAK1 phosphorylation of MKK3.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    (R)-STU104
  • Note
    Research use only, not for human use.
  • Brief Description
    (R)-STU104 is a novel TAK1-MKK3 protein-protein interaction (PPI) inhibitor that inhibits TNF-α and suppresses the TAK1/MKK3/p38/MnK1/MK2/elF4E signalling pathway by binding to MKK3 and disrupting TAK1 phosphorylation of MKK3.
  • Description
    (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.
  • In Vitro
    (R)-STU104 attenuates phosphorylation levels of Mnk1, MK2, and elF4E, leading to the downregulation of TNF-α expression and production.
  • In Vivo
    (R)-STU104 (1, 3 and 10 mg/kg; IG for 7 days) ameliorates the symptoms of DSS-induced experimental colitis in mice, and significantly inhibits inflammatory cytokine protein.Pharmacokinetic Parameters of (R)-STU104 in male C57 mice.Animal Model:C57BL/6 mice (dextran sodium sulfate (DSS)-induced acute ulcerative colitis) Dosage:1, 3 and 10 mg/kg Administration:IG, for 7 days Result:Ameliorated the symptoms of DSS-induced experimental colitis, and significantly inhibited inflammatory cytokine protein TNF-α, IL-1β, IL-6, and IL-23.
  • Synonyms
    ——
  • Pathway
    Apoptosis
  • Target
    TNF
  • Recptor
    TNF | MAPK
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2767124-77-4
  • Formula Weight
    298.33
  • Molecular Formula
    C18H18O4
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    O(C)C1=C2[C@H](CC(=O)C2=CC(OC)=C1)C3=CC=C(OC)C=C3
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Tang ML, et al. Discovery of First-in-Class TAK1-MKK3 Protein-Protein Interaction (PPI) Inhibitor (R)-STU104 for the Treatment of Ulcerative Colitis through Modulating TNF-α Production. J Med Chem. 2022 May 12;65(9):6690-6709.?
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