GW 788388
Chemical Name: 4-[4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]-2-pyridinyl]-N-(tetrahydro-2H-pyran-4-yl)-benzamide
Purity: ≥98%
Biological Activity
GW 788388 is a 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. Reduces renal fibrosis in vivo. Orally active.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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Induction of Colonic Regulatory T Cells by Mesalamine by Activating the Aryl Hydrocarbon Receptor
K Oh-Oka, Y Kojima, K Uchida, K Yoda, K Ishimaru, S Nakajima, J Hemmi, H Kano, Y Fujii-Kuri, R Katoh, H Ito, A Nakao
Cell Mol Gastroenterol Hepatol, 2017;4(1):135-151. -
RepSox slows decay of CD34+ acute myeloid leukemia cells and decreases T cell immunoglobulin mucin-3 expression.
Jajosky A, Coad J, Vos J, Martin K, Senft J, Wenger S, Gibson L
Stem Cells Transl Med, 2014;3(7):836-48. -
Targeted inhibition of AVNreceptor-like kinase 5 signaling attenuates cardiac dysfunction following myocardial infarction.
Tan et al.
Am.J.Physiol.Heart Circ.Physiol., 2010;298:H1415 -
The essential role of fibroblasts in esophageal squamous carcinoma-induced angiogenesis.
Noma et al.
Gastroenterology, 2008;134:1981 -
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 -
Oral administration of GW788388, an inhibitor of TGF-beta type I and II receptor kinases, decreases renal fibrosis.
Petersen et al.
Kidney Int., 2008;73:705
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Citations for GW 788388
The citations listed below are publications that use Tocris products. Selected citations for GW 788388 include:
4 Citations: Showing 1 - 4
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Transforming Growth Factor Beta 1 Modulates the Functional Expression of the Neurokinin-1 Receptor in Human Keratocytes.
Authors: Roux Et al.
Curr Eye Res 2016;41:1035
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Cardiac myostatin upregulation occurs immediately after myocardial ischemia and is involved in skeletal muscle activation of atrophy.
Authors: Castillero Et al.
Biochem Biophys Res Commun 2015;457:106
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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
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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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