An inhibitor of ALK5
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SM-16

Item No. 34061

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[4-(1,3-benzodioxol-5-yl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-2-yl]-bicyclo[2.2.2]octane-1-carboxamide
CAS Number
614749-78-9
Molecular Formula
C25H26N4O3
Formula Weight
430.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:5): 0.16 mg/mlEthanol: Slightly soluble
SMILES
NC(C12CCC(CC2)(C3=NC(C4=CC=CC(C)=N4)=C(C5=CC=C(OCO6)C6=C5)N3)CC1)=O
InChi Code
InChI=1S/C25H26N4O3/c1-15-3-2-4-17(27-15)21-20(16-5-6-18-19(13-16)32-14-31-18)28-23(29-21)25-10-7-24(8-11-25,9-12-25)22(26)30/h2-6,13H,7-12,14H2,1H3,(H2,26,30)(H,28,29)
InChi Key
JUHTXZGCTPDXRU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $186

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    10 mg

    $351

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    25 mg

    $728

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    Product Description

    SM-16 is an inhibitor of activin-like kinase 5 (ALK5), also known as the TGF-β type 1 receptor (Ki = 44 nM).1 It is selective for ALK5 over a panel of 60 non-ALK kinases, as well as ALK1 and ALK6, at 10 µM. SM-16 inhibits TGF-β1-induced reporter activity (IC50 = 64 nM) and SMAD2/3 phosphorylation (IC50s = 160-620 nM) in vitro. In vivo, SM-16 (15 and 30 mg/kg) inhibits neointimal formation and luminal narrowing in a rat model of carotid injury. SM-16 (5 mg/kg) inhibits tumor growth in an AB12 murine malignant mesothelioma model.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fu, K., Corbley, M.J., Sun, L., et al. SM16, an orally active TGF-beta type I receptor inhibitor prevents myofibroblast induction and vascular fibrosis in the rat carotid injury model. Arterioscler. Thromb. Vasc. Biol. 28(4), 665-671 (2008).

    2. Suzuki, E., Kim, S., Cheung, H.-K., et al. A novel small-molecule inhibitor of transforming growth factor beta type I receptor kinase (SM16) inhibits murine mesothelioma tumor growth in vivo and prevents tumor recurrence after surgical resection. Cancer Res. 67(5), 2351-2359 (2007).