Catalog Number: 3264
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.
Technical Data
  • M.Wt:
    425.48
  • Formula:
    C25H23N5O2
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    452342-67-5
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.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline
Background References
  1. Targeted inhibition of activin receptor-like kinase 5 signaling attenuates cardiac dysfunction following myocardial infarction.
    Tan et al.
    Am.J.Physiol.Heart Circ.Physiol., 2010;298:H1415
  2. The essential role of fibroblasts in esophageal squamous carcinoma-induced angiogenesis.
    Noma et al.
    Gastroenterology, 2008;134:1981
  3. 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.
    Gellibert et al.
    J.Med.Chem., 2006;49:2210
Citations:

The citations listed below are publications that use Tocris products. Selected citations for GW 788388 include:

2 Citations: Showing 1 - 2
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  1. Increased Expression of TGF-β Signaling Components in a Mouse Model of Fibrosis Induced by Submandibular Gland Duct Ligation.
    Authors: Woods Et al.
    PLoS One 2015;10:e0123641
  2. RepSox slows decay of CD34+ acute myeloid leukemia cells and decreases T cell immunoglobulin mucin-3 expression.
    Authors: Jajosky Et al.
    Stem Cells Transl Med 2014;3:836

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