C-5635020 is a potent and selective inhibitor of TGFβ type II receptor (TGFβ RII), binds to TGFβ RII with a docking score of -13.9 kcal/mol.
C-5635020 has preference for TGFβ RII than TGFβ RI (docking score of −7.9 kcal/mol).
C-5635020 targets the kinase domain of TGFβ RII with superior binding affinities compared to the standard drug, staurosporine.
C-5635020 inhibited TGFβ RII and TGFβ induced phosphorylation on Smad 2/3 in MDA-MB 231 and MCF-7 cells, inhibited the proliferation of both cell lines with GI50 of 204.2 nM for MDA-MB 231 and 154.9 nM for MCF-7, respectively.
C-5635020 induced apoptosis in breast cancer cells.
