SRPKIN-1 (JH-XI-05-01) is a potent, selective, covalent SRPK1/2 inhibitor with IC50 of 35.6/98 nM, respectively.
SRPKIN-1 significantly attenuates SR protein phosphorylation in HeLa cells at 200 nM, switches VEGF splicing to produce the VEGF-A165b isoform (at 100 nM), converts the pro-angiogenic VEGF-A165a to the anti-angiogenic VEGF-A165b isoform, therefore functioning as an antagonist for VEGF-A165a to block angiogenesis.
SRPKIN-1 blocks laser-induced neovascularization in a murine retinal model.
