GW788388 Property

Density 

1.34

storage temp. 

2-8°C

solubility 

Soluble in DMSO (18 mg/ml with warming)

form 

solid

color 

Off-white

Stability:

Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H320Causes eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

GW788388 Chemical Properties,Usage,Production

Description

GW 788388 is a selective inhibitor of transforming growth factor-β (TGF-β) type 1 receptor (TGFBR1 or ALK5; IC₅₀ = 18 nM). It inhibits the expression of collagen type I in cells (IC₅₀ = 93 nM) and in mice when given orally at 10 mg/kg once a day. As TGF-β stimulates fibrosis in a range of tissues, GW 788388 reduces typical features of fibrosis, including tissue remodeling, increased expression of α-smooth muscle actin and production of collagen I. GW 788388 also blocks TGF-β-mediated production of VEGF by fibroblasts, as well as subsequent angiogenesis in vitro. Inhibition of ALK5 signaling by GW 788388 also induces hypertrophy in femoral growth plates in rats.

Uses

GW788388 is a new TGF-beta type I receptor inhibitor with a much improved pharmacokinetic profile compared with SB431542.

storage

Store at +4°C

References

Gellibert et al. (2006), Discovery of 4-{4-[3-(pyridine-2-yl)-1H-pyrazol-4-yl}pyridine-2-yl}-N-(tetrahydro-2H-pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor; J. Med. Chem. 49 2210 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 De Oliveira et al. (2012), Oral administration of GW788388, an inhibitor of transforming growth factor beta signaling, prevents heart fibrosis in Chagas disease; PLoS Negl. Trop. Dis. 6 e1696 Noma et al. (2008), The essential role of fibroblasts in esophageal squamous cell carcinoma-induced angiogenesis; Gastroenterology. 134 1981 Lho et al. (2021), Effects of TGF-? Receptor Inhibitor GW788388 on the Epithelial to Mesenchymal Transition of Peritoneal Mesothelial Cells; Int. J. Mol. Sci. 22 4739