An inhibitor of TGF-β signaling
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SMAD3 Inhibitor, SIS3

Item No. 15945

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-2-propen-1-one
CAS Number
1009104-85-1
Molecular Formula
C28H27N3O3
Formula Weight
453.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2) (1:3): 0.2 mg/ml
λmax
234, 292, 319 nm
SMILES
COC1=CC(CCN(C(/C=C/C2=C(C3=CC=CC=C3)N(C)C4=C2C=CC=N4)=O)C5)=C5C=C1OC
InChi Code
InChI=1S/C28H27N3O3/c1-30-27(19-8-5-4-6-9-19)22(23-10-7-14-29-28(23)30)11-12-26(32)31-15-13-20-16-24(33-2)25(34-3)17-21(20)18-31/h4-12,14,16-17H,13,15,18H2,1-3H3/b12-11+
InChi Key
IJYPHMXWKKKHGT-VAWYXSNFSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $72

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    1 mg

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    5 mg

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    Product Description

    SMAD3 Inhibitor, SIS3 selectively inhibits TGF-β and activin signaling by suppressing Smad3 phosphorylation (IC50 = 3 µM) without affecting the MAPK/p38, ERK, or PI3-kinase signaling pathways.1 It has been shown to reduce TGF-β1-induced type 1 procollagen expression and myofibroblast differentiation in normal dermal fibroblasts as well as scleroderma fibroblasts.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jinnin, M., Ihn, H., and Tamaki, K. Characterization of SIS3, a novel specific inhibitor of Smad3, and its effect on transforming growth factor-β1-induced extracellular matrix expression. Mol. Pharmacol. 69(2), 597-607 (2006).

    Product Citations

    Beach, J.A., Aspuria, P.J., Cheon, D.J., et al. Sphingosine kinase 1 is required for TGF-β mediated fibroblast-to-myofibroblast differentiation in ovarian cancer. Oncotarget 7(4), 4167-4182 (2016).