Description
SB-525334 can inhibit TGF-beta1 with IC50 of 14.3 nM.
Storage
2 years at -20centigrade Powder
Molecular Formula
C21H21N5
Chemical Name
6-(2-tert-butyl-4-(6-methylpyridin-2-yl)-1H-imidazol-5-yl)quinoxaline
Solubility
DMSO 69 mg/mL Water
In vitro
SB-525334 inhibited ALK5 phosphorylation of Smad3 with an IC 50 value of 14.3 nM. ALK4 phosphorylation of Smad3 was inhibited by SB-525334 with an IC 50 value of 58.5 nM, and ALK2 phosphorylation of Smad1 exhibited an IC 50 value greater than 10 uM. As a consequence of inhibiting the ALK5 receptor, SB-525334 suppressed Smad2/3 nuclear localization in RPTE cells.
In vivo
SB-525334 showed acceptable bioavailability and plasma half-life in the SD rat for dosing up to 10 mg/kg/day. SB-525334 showed acceptable bioavailability and plasma half-life in the SD rat for dosing up to 10 mg/kg/day.
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