SRPKIN-1 is a covalent and irreversible SRPK1/2 inhibitor with IC 50 s of 35.6 and 98 nM, respectively. Anti-angiogenesis effect
In Vitro
SRPKIN-1 treatment at 200 nM (10, 50, 100, 200 nM, 16 hours) significantly reduces SR protein phosphorylation at the steady state with or without washout. ? SRPK-IN-1 potently converts VEGF from pro-angiogenic to anti-angiogenic isoform. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Ba/F3 cells Concentration: 0-10000 nM Incubation Time: 72 h Result: Potently decreased the level of SR phosphorylation in a dose-dependent manner, leading to increased VEGF-A165b RNA as well as protein even at a dose of 200 nM.
In Vivo
SRPKIN-1 (50 nM, 300 nM,1 μL, 5 times) blocks angiogenesis in a CNV mouse model through VEGF alternative splicing . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Mice Dosage: 50 nM, 300 nM, 1 μL Administration: Intravitreal injection, 5 times Result: SRPKIN-1-treated mice is significantly suppressed in a dose-dependent manner based upon measurement of the CNV area .
