CDD-1281 (CDD1281) is a potent, selective inhibitor of BMP type 2 receptor BMPR2 with IC50 of 1.2 nM and Kiapp value of 8 nM.
CDD-1281 displays high selectivity (>110-fold–>830-fold) over other type 1 and type 2 TGFβ family kinases.
CDD-1281 inhibited BMP-mediated gene expression in mammalian cell cultures, suppressed BRE-reporter activity in a luciferase reporter (293T-BRE-Luc) assays with IC50 of 6.19 uM.
Pretreatment with CDD-1281 (25 uM) significantly decreased the phosphorylation of SMAD1/5 (pSMAD1/5) in BMP9 stimulation of pSMAD1/5 in HUVECs.
CDD-1281 is not only selective among the TGFβ family but also completely selective against >408 off-target kinases.
