SM16
SM16 Basic information
- Product Name:
- SM16
- Synonyms:
-
- 4-[4-(1,3-Benzodioxol-5-yl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-2-yl]bicyclo[2.2.2]octane-1-carboxamide
- CS-2835
- Bicyclo[2.2.2]octane-1-carboxamide, 4-[4-(1,3-benzodioxol-5-yl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-2-yl]-
- SM16
- SM-16,TGF-β Receptor,Inhibitor,inhibit,SM 16,Transforming growth factor beta receptors,SM16
- 4-[5-(2H-1,3-benzodioxol-5-yl)-4-(6-methylpyridin-2-yl)-1H-imidazol-2-yl]bicyclo[2.2.2]octane-1-carboxamide
- SM 16, 10 mM in DMSO
- CAS:
- 614749-78-9
- MF:
- C25H26N4O3
- MW:
- 430.5
- Mol File:
- 614749-78-9.mol
SM16 Chemical Properties
- Boiling point:
- 691.3±55.0 °C(Predicted)
- Density
- 1.354±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:65.0(Max Conc. mg/mL);150.99(Max Conc. mM)
- form
- A solid
- pka
- 11.23±0.10(Predicted)
- color
- White to off-white
SM16 Usage And Synthesis
Uses
SM 16 is a ALK5/ALK4 kinase inhibitor with Kis of 10 and 1.5 nM, respectively.
Biological Activity
SM 16 is an ALK5/ALK4 kinase inhibitor with Ki values of 10 and 1.5 nM, respectively.
in vivo
SM 16 penetrates tumor cells in vivo , suppressing tumor phosphorylated Smad2/3 levels for at least 3 h following treatment of tumor-bearing mice with a single ip bolus of 20 mg/kg SM 16. The growth of established AB12 tumors is significantly inhibited by 5 mg/kg/d SM 16 (P<0.001) delivered via sc miniosmotic pumps over 28 days.
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target
Ki: ALK5 (10 nM), ALK4 (1.5 nM)
storage
Store at -20°C
References
[1] Suzuki E, 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. 2007 Mar 1;67(5):2351-9. DOI:10.1158/0008-5472.CAN-06-2389
[2] Fu K, 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. 2008 Apr;28(4):665-71. DOI:10.1161/ATVBAHA.107.158030
[3] Engebretsen KV, et al. Attenuated development of cardiac fibrosis in left ventricular pressure overload by SM16, an orally active inhibitor of ALK5. J Mol Cell Cardiol. 2014 Nov;76:148-57. DOI:10.1016/j.yjmcc.2014.08.008
SM16Supplier
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