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Description: Potent and selective inhibitor of TGF-βRI
Chemical Name: 4-[4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]-2-pyridinyl]-N-(tetrahydro-2H-pyran-4-yl)-benzamide
Purity: ≥98% (HPLC)
Biological Activity for GW 788388
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.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline
Compound Libraries for GW 788388
GW 788388 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.
Technical Data for GW 788388
| M. Wt | 425.48 |
| Formula | C25H23N5O2 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 452342-67-5 |
| PubChem ID | 10202642 |
| InChI Key | SAGZIBJAQGBRQA-UHFFFAOYSA-N |
| Smiles | O=C(NC5CCOCC5)C(C=C4)=CC=C4C1=CC(C2=CNN=C2C3=CC=CC=N3)=CC=N1 |
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.
Solubility Data for GW 788388
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 42.55 | 100 |
Preparing Stock Solutions for GW 788388
The following data is based on the product molecular weight 425.48. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.35 mL | 11.75 mL | 23.5 mL |
| 5 mM | 0.47 mL | 2.35 mL | 4.7 mL |
| 10 mM | 0.24 mL | 1.18 mL | 2.35 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.47 mL |
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Product Datasheets for GW 788388
References for GW 788388
References are publications that support the biological activity of the product.
Tan et al (2010) Targeted inhibition of AVNreceptor-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
Petersen et al (2008) Oral administration of GW788388, an inhibitor of TGF-beta type I and II receptor kinases, decreases renal fibrosis. Kidney Int. 73 705 PMID: 18075500
If you know of a relevant reference for GW 788388, please let us know.
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Keywords: GW 788388, GW 788388 supplier, GW788388, transforming, growth, factor, type, I, receptors, tgfbeta, tgfb, tgfβ, inhibitors, inhibits, TGF-βRI, TGF-beta, Receptors, 3264, Tocris Bioscience
4 Citations for GW 788388
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
Castillero et al (2015) Cardiac myostatin upregulation occurs immediately after myocardial ischemia and is involved in skeletal muscle activation of atrophy. Biochem Biophys Res Commun 457 106 PMID: 25528587
Roux et al (2016) Transforming Growth Factor Beta 1 Modulates the Functional Expression of the Neurokinin-1 Receptor in Human Keratocytes. Curr Eye Res 41 1035 PMID: 26673553
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? Please let us know.
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Literature in this Area
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Stem Cell Research Product Guide
This product guide provides a background to the use of small molecules in stem cell research and lists over 200 products for use in:
- Self-renewal and Maintenance
- Differentiation
- Reprogramming
- Organoid Generation
- GMP and Ancillary Material Grade Products
Stem Cells Scientific Review
Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.
Stem Cells Poster
Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.
Pathways for GW 788388
