GW788388 | TGF-ß receptor kinase inhibitor
CAS:
452342-67-5
Catalog Number:
10-5521
Activity:
TGF-ß receptor kinase inhibitor
Chemical Names:
4-(4-(3-(Pyridin-2-yl)-1H-pyrazol-4-yl)pyridin-2-yl)-N-(tetrahydro-2H-pyran-4-yl)benzamide
Molecular Weight:
425.49
Molecular Formula:
C25H23N5O2
Solubility:
Soluble in DMSO (18 mg/ml with warming)
Physical Properties:
Off-white solid
Purity:
>98% HPLC
NMR (Conforms)
NMR (Conforms)
Storage Temperature:
-20°C
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.
Shipping Code:
RT
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $80.00 | ||
| 25 mg | $260.00 |
GW788388 (452342-67-5) is a potent inhibitor of TGF-β receptor kinases ALK4, ALK5 (IC50=18 nM), ALK7, and TGFβRII, but not BMP type II receptor kinase.1,2 Blocks TGF-β-mediated signaling, including collagen type I and VEGF, in turn reducing fibrosis and angiogenesis in various mouse models.3,4 GW788388 attenuates TGF-β-induced epithelial to mesenchymal transition (EMT) in human peritoneal mesothelial cells.5
References/Citations:
- 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-ß Receptor Inhibitor GW788388 on the Epithelial to Mesenchymal Transition of Peritoneal Mesothelial Cells; Int. J. Mol. Sci. 22 4739
CAS:
452342-67-5
Catalog Number:
10-5521
Activity:
TGF-ß receptor kinase inhibitor
Chemical Names:
4-(4-(3-(Pyridin-2-yl)-1H-pyrazol-4-yl)pyridin-2-yl)-N-(tetrahydro-2H-pyran-4-yl)benzamide
Molecular Weight:
425.49
Molecular Formula:
C25H23N5O2
Solubility:
Soluble in DMSO (18 mg/ml with warming)
Physical Properties:
Off-white solid
Purity:
>98% HPLC
NMR (Conforms)
NMR (Conforms)
Storage Temperature:
-20°C
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.
Shipping Code:
RT
Safety Data Sheet:
N/A
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
GW788388 (452342-67-5) is a potent inhibitor of TGF-β receptor kinases ALK4, ALK5 (IC50=18 nM), ALK7, and TGFβRII, but not BMP type II receptor kinase.1,2 Blocks TGF-β-mediated signaling, including collagen type I and VEGF, in turn reducing fibrosis and angiogenesis in various mouse models.3,4 GW788388 attenuates TGF-β-induced epithelial to mesenchymal transition (EMT) in human peritoneal mesothelial cells.5
References/Citations:
- 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-ß Receptor Inhibitor GW788388 on the Epithelial to Mesenchymal Transition of Peritoneal Mesothelial Cells; Int. J. Mol. Sci. 22 4739
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