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ALK5 Inhibitor I

ALX-270-448-M001 1 mg 69.00 USD
ALX-270-448-M005 5 mg 101.00 USD
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Cell permeable, potent, selective and ATP-competitive inhibitor of TGF-β RI kinase (IC50=51nM). Displays ~15-fold greater selectivity over p38α MAPK (IC50=740nM). Inhibits TGF-β-dependent cellular growth (IC50=89nM in NIH 3T3 mouse fibroblasts) and transcription activation (IC50=47nM in mink lung cells). Suppresses invasion of MDA-MB-231 breast cancer cells in a matrigel invasion assay.

Product Specification

Alternative Name:TGF-β RI Kinase Inhibitor I, 3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole
Purity:≥97% (1H-NMR)
Appearance:Yellow to brown solid.
Solubility:Soluble in DMSO or methanol.
Long Term Storage:-20°C
Use/Stability:Stable for 2 years after receipt when stored at -20°C. Stock solutions are stable for up to 3 months when stored at -20°C.
Handling:Protect from light.
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Product Literature References

Closed-channel culture system for efficient and reproducible differentiation of human pluripotent stem cells into islet cells: K. Hirano, et al.; Biochem. Biophys. Res. Commun. 487, 344 (2017), Application(s): hiPSC line 253G1, Abstract;
Emdogain-regulated gene expression in palatal fibroblasts requires TGF-βRI kinase signaling: A. Stähli, et al.; PLoS One 9, e105672 (2014), Abstract; Full Text
Successful shape-based virtual screening: the discovery of a potent inhibitor of the type I TGFbeta receptor kinase (TbetaRI): J. Singh, et al.; Bioorg. Med. Chem. Lett. 13, 4355 (2003), Abstract;
Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain: J.S. Sawyer, et al.; J. Med. Chem. 46, 3953 (2003), Abstract;

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