GW 788388

Pricing Availability Delivery Time Qty
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 (2)
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.

All Tocris products are intended for laboratory research use only.

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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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

Safety Datasheet

References

References are publications that support the products' biological activity.

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 GW 788388, please let us know.

View Related Products by Product Action

View all TGF-β Receptor Inhibitors

Keywords: GW 788388, supplier, GW788388, transforming, growth, factor, type, I, receptors, tgfbeta, tgfb, tgfβ, inhibitors, inhibits, TGF-βRI, TGF-beta, Receptors, TGF-beta, Receptors, Tocris Bioscience

2 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


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

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Reviews

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Literature in this Area

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  • Epigenetics in Cancer
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Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

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Stem Cells

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.

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.

Protocols

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