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 Details
Alternative Name: | TGF-β RI Kinase Inhibitor I, 3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole |
|
Formula: | C17H12N4 |
|
MW: | 272.3 |
|
CAS: | 396129-53-6 |
|
Purity: | ≥97% (TLC) |
|
Appearance: | Yellow to brown solid. |
|
Solubility: | Soluble in DMSO or methanol. |
|
Shipping: | Ambient |
|
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. |
|
Regulatory Status: | RUO - Research Use Only |
|
Please mouse over
Product Literature References
Chemically defined conditions for long-term maintenance of pancreatic progenitors derived from human induced pluripotent stem cells: S. Konagaya, et al.; Sci. Rep.
9, 640 (2019),
Abstract;
Full Text
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;