| Stereochemistry | ACHIRAL |
| Molecular Formula | C25H23N5O2 |
| Molecular Weight | 425.4824 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
O=C(NC1CCOCC1)C2=CC=C(C=C2)C3=NC=CC(=C3)C4=CNN=C4C5=NC=CC=C5
InChI
InChIKey=SAGZIBJAQGBRQA-UHFFFAOYSA-N
InChI=1S/C25H23N5O2/c31-25(29-20-9-13-32-14-10-20)18-6-4-17(5-7-18)23-15-19(8-12-27-23)21-16-28-30-24(21)22-3-1-2-11-26-22/h1-8,11-12,15-16,20H,9-10,13-14H2,(H,28,30)(H,29,31)
| Molecular Formula | C25H23N5O2 |
| Molecular Weight | 425.4824 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
GW-788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM in a cell-free assay, also inhibits TGF-β type II receptor and activin type II receptor activities, but does not inhibit BMP type II receptor. GW-788388 exhibits anti-fibrotic and cardioprotective activities. GW-788388 increases survival in studies of Trypanosoma infection and prevents Chagas disease-induced development of cardiac fibrosis. This compound also attenuates systolic dysfunction and left ventricular remodeling in animal models of myocardial infarction. In animal models of diabetes, GW-788388 decreases the occurrence of renal fibrosis. GW-788388 can inhibit TGF-b and activin signalling in vitro and attenuate renal fibrosis in vivo. By blocking the action of the ALK5 and TbRII kinase receptors, TGF-b-induced growth arrest, EMT, and ECM deposition were inhibited in vitro. TGF-b receptor kinase inhibition should attenuate fibrogenesis and improve the fibrotic outcome for patients suffering from diabetic nephropathy.
