A selective inhibitor of TGF-β type 1 receptor (TGFBR1 or ALK5; IC50 = 18 nM); 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; reduces typical features of fibrosis

GW 788388 – 25 mg

Brand:
Cayman
CAS:
452342-67-5
Storage:
-20
UN-No:
Non-Hazardous - 2811 / 6.1

GW 788388 is a selective inhibitor of transforming growth factor-β (TGF-β) type 1 receptor (TGFBR1 or ALK5; IC50 = 18 nM).{27870} 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.{27870} 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.{27872,27874,27875} GW 788388 also blocks TGF-β-mediated production of VEGF by fibroblasts, as well as subsequent angiogenesis in vitro.{27873} Inhibition of ALK5 signaling by GW 788388 also induces hypertrophy in femoral growth plates in rats.{27871}  

 

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Description

A selective inhibitor of TGF-β type 1 receptor (TGFBR1 or ALK5; IC50 = 18 nM); 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; reduces typical features of fibrosis

Formal name: 4-​[4-​[3-​(2-​pyridinyl)​-​1H-​pyrazol-​4-​yl]​-​2-​pyridinyl]​-​N-​(tetrahydro-​2H-​pyran-​4-​yl)​-benzamide

Synonyms: 

Molecular weight: 425.5

CAS: 452342-67-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Activin-like Kinases (ALKs)||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Signaling|Growth Factor Receptors||Research Area|Cell Biology|Cytoskeleton & Motor Proteins||Research Area|Cell Biology|ECM & Adhesion Molecules

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