2-(5-Chloro-2-fluorophenyl)pteridin-4-yl)pyridin-4-yl amine SD-208 Transforming Growth Factor-b Type I Receptor Kinase Inhibitor V Light yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable pteridine compound that blocks TGF-b signaling and displays anti-tumor properties. Acts as a potent, selective, and reversible inhibitor of TGF-b RI/ALK5 kinase (EC50 = 48 nM). It inhibits p38a, MAPKAP, PKD, and p38a only at much higher concentrations (≥867 nM), while exhibiting little activity aginst TGF-b RII, p38g, JNK, ERK2, MAPKK6, PKA, or PKC even at concentrations as high as 50 µM. Inhibits TGF-b-mediated cellular functions both in vitro and in vivo. Purity: ≥97% by HPLC. CAS 627536-09-8. Ref.: Ge, R., et al. 2006. Clin. Cancer Res. 12, 4315. Kapoun, A. M., et al. 2006. Mol. Pharmacol. 70, 518. Jian, H., et al. 2006. Genes Dev. 20, 666. Hayashi, T., et al. 2004. Clin. Cancer Res. 10, 7540. Uhl, M., et al. 2004. Cancer Res. 64, 7954. |