An inhibitor of the TAK1-MKK3 protein-protein interaction
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(R)-STU104

Item No. 45375

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3R)-2,3-dihydro-4,6-dimethoxy-3-(4-methoxyphenyl)-1H-inden-1-one
CAS Number
2767124-77-4
Molecular Formula
C18H18O4
Formula Weight
298.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/ml
SMILES
COC1=C2[C@@H](C3=CC=C(C=C3)OC)CC(C2=CC(OC)=C1)=O
InChi Code
InChI=1S/C18H18O4/c1-20-12-6-4-11(5-7-12)14-10-16(19)15-8-13(21-2)9-17(22-3)18(14)15/h4-9,14H,10H2,1-3H3/t14-/m1/s1
InChi Key
OYJBHGSSAJNKJF-CQSZACIVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $172

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    10 mg

    $319

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    25 mg

    $490

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    Product Description

    (R)-STU104 is an inhibitor of the protein-protein interaction between TGF-β-activated kinase 1 (TAK1) and MAP kinase kinase 3 (MKK3).1 It binds MKK3 (KD = 71 nM), inhibits the phosphorylation of MKK3 in RAW 264.7 macrophages (IC50 = 4 µM), and disrupts the interaction between MKK3 and TAK1 in the same cells. (R)-STU104 reduces TNF-α levels (IC50 = 0.58 µM) and p38 and eukaryotic initiation factor 4E (eIF4E) phosphorylation in LPS-stimulated RAW 264.7 macrophages. It increases body weight and colon length and reduces serum levels of TNF-α, IL-1β, IL-6, and IL-23 in mouse model of ulcerative colitis induced by dextran sulfate (DSS; Item No. 23250). It also increases the survival rate in an IL-10-/- knockout mouse model of chronic ulcerative colitis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tang, M.-L., Li, H., Nig, J.-F., 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. 65(9), 6690-6709 (2022).