GW 788388

Cat. No. 3264

GW 788388 C25H23N5O2 [452342-67-5]

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Chemical Name: 4-[4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]-2-pyridinyl]-N-(tetrahydro-2H-pyran-4-yl)-benzamide

Biological Activity

Potent inhibitor of transforming growth factor-β type I receptor (ALK5) (IC50 values are 18 and 93 nM for ALK5 binding and for TGF-β cellular assay respectively). Inhibits esophageal squamous cell carcinoma (ESCC)-induced neoangiogenesis. Orally active.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Technical Data

Soluble to 100 mM in DMSO
>98 %
Store at +4°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

Tan et al (2010) Targeted inhibition of activin receptor-like kinase 5 signaling attenuates cardiac dysfunction following myocardial infarction. Am.J.Physiol.Heart Circ.Physiol. 298 H1415. PMID: 20154262.

Noma et al (2008) The essential role of fibroblasts in esophageal squamous carcinoma-induced angiogenesis. Gastroenterology 134 1981. PMID: 18439605.

Gellibert et al (2006) Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-β type I receptor inhibitor. J.Med.Chem. 49 2210. PMID: 16570917.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for GW 788388 include:

Woods et al (2015) Increased Expression of TGF-β Signaling Components in a Mouse Model of Fibrosis Induced by Submandibular Gland Duct Ligation. PLoS One 10 e0123641. PMID: 25955532.

Jajosky et al (2014) RepSox slows decay of CD34+ acute myeloid leukemia cells and decreases T cell immunoglobulin mucin-3 expression. Stem Cells Transl Med 3 836. PMID: 24855276.

Do you know of a great paper that uses GW 788388 from Tocris? If so please let us know.

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Keywords: GW 788388, supplier, GW788388, transforming, growth, factor, type, I, receptors, tgfbeta, tgfb, tgfβ, inhibitors, inhibits, TGF-βRI, Tocris Bioscience, TGF-β Receptor Inhibitor products

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