627536-09-8

Solubility:Soluble to 20 mM in DMSO

Storage:Store at RT

Biologieal

SD-208 is TGF-βR I kinase inhibitor with IC₅₀ =49 nM based on direct enzymatic assay of TGFRI kinase (ALK5) activity with a specificity of >100-fold against TGFRII and at least 17-fold over members of a panel of related protein kinases including p38a, p38b, p38d, JNK1, EGFR, MAPKAPK2, MKK6, ERK2, PKC, PKA, PKD, CDC2, and CaMKII. tent, orally active ATP-competitive transforming growth factor-β receptor 1 (TGF-βRI) inhibitor (IC₅₀ = 49nM). Displays > 100-fold and > 17-fold selectivity over TGF-βRII and other common kinases respectively. Exhibits anti-inflammatory and antitumor activity.

Reference

Uhl et al (2004) SD-208, a novel transforming growth factor β feceptor I kinase inhibitor, inhibits growth and invasiveness and enhances immunogeneicity of murine and human glioma cells in vitro and in vivo. Cancer Res. 64 7954. Kapoun et al (2006) Transforming growth factor-β receptor type I receptor (TGFβRI) kinase activity but not p38 activation is required for TGFβRI-induced myofibroblast differentiation and profibrotic gene expression. Mol.Pharmacol. 70 518. Leung et al (2006) Effect of transforming growth factor-β receptor I kinase inhibitor 2,4-disubstituted pteridine (SD-208) in chronic allergic airway inflammation and remodeling. J.Pharmacol.Exp.Ther. 319 586.