(R)-STU104

Research use only, not for human use.

(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.

(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.

(R)-STU104 attenuates phosphorylation levels of Mnk1, MK2, and elF4E, leading to the downregulation of TNF-α expression and production.

(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.

——

Apoptosis

TNF

TNF | MAPK

——

——

2767124-77-4

298.33

C18H18O4

>98% (HPLC)

——

O(C)C1=C2[C@H](CC(=O)C2=CC(OC)=C1)C3=CC=C(OC)C=C3

——

(-20℃)

With Ice Pack

≥ 2 years