GW 788388

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Cat.No. 3264 - GW 788388 | C25H23N5O2 | CAS No. 452342-67-5
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)
Datasheet
Citations (4)
Reviews
Literature
Pathways

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

Compound Libraries

GW 788388 is also offered as part of the Tocriscreen Plus and Tocriscreen Stem Cell Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 42.55 100

Preparing Stock Solutions

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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References

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


If you know of a relevant reference for GW 788388, please let us know.

View Related Products by Product Action

View all TGF-β Receptor Inhibitors

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

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

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

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


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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


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Stem Cells Scientific Review

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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

TGF-β

TGF-β Signaling Pathway

The TGF-β signaling pathway is involved in the regulation of growth and proliferation of cells along with migration, differentiation and apoptosis.