GW 788388

Name: GW 788388
Brand: Tocris Bioscience
SKU: 3264

Tocris Bioscience, part of Bio-Techne | Catalog # 3264

Citations (17)

COA / SDS

Potent and selective inhibitor of TGF-βRI

Key Product Details

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)
Molecular Weight:	425.48

View Full Technical Details for GW 788388

Technical Data
Citations

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 for GW 788388

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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	23.50 mL
5 mM	0.47 mL	2.35 mL	4.70 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 for GW 788388

References are publications that support the biological activity of the product.

Petersen Oral administration of GW788388, an inhibitor of TGF-beta type I and II receptor kinases, decreases renal fibrosis. Kidney Int. 2008 PMID: 18075500
Noma The essential role of fibroblasts in esophageal squamous carcinoma-induced angiogenesis. Gastroenterology 2008 PMID: 18439605
Gellibert 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. 2006 PMID: 16570917
Tan Targeted inhibition of AVNreceptor-like kinase 5 signaling attenuates cardiac dysfunction following myocardial infarction. Am.J.Physiol.Heart Circ.Physiol. 2010 PMID: 20154262