Transforming growth factor (TGF) -β is a multifunctional cytokine that can inhibit endothelial and epithelial cellular proliferation, stimulate matrix accumulation, and suppress inflammation. Signaling by the TGF-β superfamily is mediated by two types of transmembrane receptor serine/threonine kinases, types I and II, ligand interaction with a homodimer of type II receptors recruits and activates homodimers of type I receptors or activin receptor-like kinases (ALKs)[3]. SB505124 is an inhibitor of TGFβ receptor ALK4 and ALK5 with IC50 of 47 nM and 129 nM, respectively[3]. FaO cells or NRP 154 cells were protected from TGF-β–induced apoptosis by SB-505124 (0.01-1µM) in a concentration-dependent manner[3]. Specific inhibition of the TGF-β type I receptor/ALK5 serine-threonine kinase with SB-505124 (500 nM) abolished the effects of TGF-β1 on F-actin assembly in HUVEC cells[4]. Treatment with 0.25 μM-SB505124 in Sh3bp2KI/KI bone marrow stromal cultures reduced RANKL (a critical regulator of osteoclast formation) expression almost back down to wild type levels[5].
SB-505124 细胞研究
细胞系
浓度
检测类型
检测时间
活性说明
数据源
human HaCaT cells
Function assay
Inhibition of ALK5 in human HaCaT cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay, IC50=43.8 nM
24786585
mouse 4T1 cells
Function assay
Inhibition of ALK5 in mouse 4T1 cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay, IC50=76.6 nM
24786585
mouse NMuMG cells
0.1-0.5 μM
Function assay
1 h
Inhibition of ALK5 activity in mouse NMuMG cells assessed as TGFbeta-induced phosphorylation of Smad2 at 0.1 to 0.5 uM after 1 hr by Western blot analysis
23047226
Sf9 insect cells
Function assay
Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 insect cells using casein as substrate by proprietary radioisotopic protein kinase assay, IC50=34.9 nM
Inhibition of ALK5 in human HaCaT cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay, IC50=43.8 nM
24786585
mouse 4T1 cells
Function assay
Inhibition of ALK5 in mouse 4T1 cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay, IC50=76.6 nM
24786585
mouse NMuMG cells
0.1-0.5 μM
Function assay
1 h
Inhibition of ALK5 activity in mouse NMuMG cells assessed as TGFbeta-induced phosphorylation of Smad2 at 0.1 to 0.5 uM after 1 hr by Western blot analysis
23047226
Sf9 insect cells
Function assay
Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 insect cells using casein as substrate by proprietary radioisotopic protein kinase assay, IC50=34.9 nM
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