Background:

2OH-BNPP1 is an inhibitor of BUB1 kinase, a Ser/Thr kinase, used for the treatment of cancer.

2OH-BNPP1 (0.1-50 μM) abrogates TGFβ signaling in a dose dependent manner. 2OH-BNPP1 dose-dependently impairs the TGFβ-induced phosphorylation of proteins that mediate canonical and non-canonical TGFβ signaling in multiple cancer cell lines and normal cell lines[1].

2OH-BNPP1 (50 mg/kg) blocks TGFβ signaling in vivo, and significantly decreases abundance of phosphorylated SMAD2 in tumor-bearing mice[1].

[1]. Nyati S, et al. The kinase activity of the Ser/Thr kinase BUB1 promotes TGF-β signaling. Sci Signal. 2015 Jan 6;8(358):ra1.