SB-505124 is a selective inhibitor of transforming growth factor-β type I receptor (ALK5), ALK4 and ALK7 (IC50 values are 47 and 129 nM for ALK5 and ALK4 respectively). SB-505124 also blocks more complex endpoints of TGF-beta action, as evidenced by its ability to abrogate cell death caused by TGF-beta1 treatment. SB-505124 is three to five times more potent than a related ALK5 inhibitor described previously, SB-431542.
|Source||Arthritis Res Ther (2017). Figure 1. SB-505124|
|Cell Lines||Primary bovine chondrocytes|
|Incubation Time||1 h|
|Results||Subsequently, we analyzed the effects of the ALK4/5/7-kinase inhibitor SB-505124, the ALK1/2/3-kinase inhibitor LDN-193189 and the TAK1-kinase inhibitor (5Z)-7-Oxozeaenol on TGFβ1-induced R-Smad phosphorylation|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 60 mg/mL
Ethanol 60 mg/mL
SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptors ALK4, ALK5, and ALK7.
DaCosta Byfield S, et al. Mol Pharmacol. 2004 Mar;65(3):744-52. PMID: 14978253.
|Related TGF-beta/Smad Products|
ITD-1 is a selective inhibitor of TGF-β signaling (IC50 ~ 0.4-0.8 μM).
R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5nM, an approximately 5000-fold more selectivity for ALK5 than p38 mitogen-activated protein kinase (MAPK).
LY3200882 is a novel, highly selective TGFβRI small molecule inhibitor.
SRI-011381 hydrochloride is an agonist of the TGF-beta signaling pathway for treatment of Alzheimer's disease.
Disitertide is a TGF-β1 inhibitor.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.