2767124-77-4

2767124-77-4 structure

Name: (R)-STU104
Chemical Name: (R)-STU104
CAS Number: 2767124-77-4
Molecular Formula: C₁₈H₁₈O₄
Molecular Weight: 298.33
Catalog: Signaling Pathways MAPK/ERK Pathway p38 MAPK
Create Date: 2022-09-19 07:51:41
Modify Date: 2024-01-17 11:55:14
(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[1].

Name	(R)-STU104

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[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> MAPK/ERK Pathway >> p38 MAPK
Target	IC50: 0.58 μM (TNF-α), 4.0 μM (MKK3 phosphorylation)[1]
In Vitro	(R)-STU104 attenuates phosphorylation levels of Mnk1, MK2, and elF4E, leading to the downregulation of TNF-α expression and production[1].
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[1]. Pharmacokinetic Parameters of (R)-STU104 in male C57 mice[1]. IV (5 mg/kg) PO (30 mg/kg) Tmax (h) 0.083 AUC0-t (μg/L·h) 7249 9895 AUC0-∞ (μg/L·h) 8635 16991 MRT0-∞ (h) 7.32 12.52 Cmax (ng/mL) 2920 2290 t1/2 (ng/mL) 9.29 8.67 VZ (L/kg) 7.76 3.68 CLZ (ng/mL) 0.58 0.29 F (%) 33% Animal Model: C57BL/6 mice (dextran sodium sulfate (DSS)-induced acute ulcerative colitis)[1] 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.
References	[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.

Molecular Formula	C₁₈H₁₈O₄
Molecular Weight	298.33

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