(R)-STU104

SKU: orb1689372

Description

(R)-STU104 is a novel small molecule PPI inhibitor that targets the TAK1-MKK3 interaction, thereby suppressing the downstream p38 MAPK signaling pathway and TNF-α production. It has demonstrated efficacy in preclinical in vivo models, making it a candidate for research in inflammatory diseases such as ulcerative colitis.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 2767124-77-4
• MW: 298.33
• Purity: 99.42% (May vary between batches)
• Formula: C₁₈H₁₈O₄
• SMILES: O(C)C1=C2[C@H](CC(=O)C2=CC(OC)=C1)C3=CC=C(OC)C=C3
• Target: TNF,p38 MAPK,MAPK

Bioactivity

• Target IC50:
  TNF-α:0.58 μM|MKK3 phosphorylation:4.0 μM
• In Vivo:
  (R)-STU104 demonstrated remarkable dose-effect relationships on both acute and chronic mouse UC models. In addition to its good pharmacokinetic (PK) and safety profile, (R)-STU104 showed better anti-UC efficacy in vivo at 10 mg/kg/d than mesalazine at the dose of 50 mg/kg/d.
• In Vitro:
  (R)-STU104 exhibited the most potent inhibitory activity on TNF-α production, which suppressed the TAK1/MKK3/p38/MnK1/MK2/elF4E signal pathways through binding with MKK3 and disrupting the TAK1 phosphorylating MKK3.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TNF-α, TAK1

Compound Identifiers

PubChem CID

156579934