有力的平滑刺猬信号拮抗剂;Potent smoothened and hedgehog signaling antagonist;SANT-1 directly binds to Smoothened (Smo) receptor with Kd of 1.2 nM and inhibits Smo agonist effects with IC50 of 20 nM.;SANT-1 directly binds to Smoothened (Smo) receptor with Kd of 1.2 nM and inhibits Smo agonist effects with IC50 of 20 nM.Treatment of Anaplastic lymphoma kinase (ALK)-positive anaplastic large cell lymphoma cells2 and chronic lymphocytic leukemia cells3 with SANT-1 induced cell death.
靶点:
IC50: 20 nM (Shh signaling), 30 nM (SmoA1)
参考文献:
1. Chen JK, et al. Small molecule modulation of Smoothened activity. Proc Natl Acad Sci U S A. 2002 Oct 29;99(22):14071-6.