SRPKIN-1是共价，不可逆的SRPK1/2抑制剂，IC50分别为35.6和98nM。有抗血管生成作用。
SRPKIN-1 is a covalent and irreversible SRPK1/2 inhibitor with IC50s of 35.6 and 98 nM, respectively. Anti-angiogenesis effect[1].
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[1]. SRPK-IN-1 potently converts VEGF from pro-angiogenic to anti-angiogenic isoform[1].|| Cell Viability Assay[1]||Cell Line:|Ba/F3 cells|Concentration:|0-10000 nM|Incubation Time:| 72 h|Result:|
SRPKIN-1 (50 nM, 300 nM,1 μL, 5 times) blocks angiogenesis in a CNV mouse model through VEGF alternative splicing[1].|| Animal Model:|Mice[1]|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[1].
[1]. Hatcher JM, et al. SRPKIN-1: A Covalent SRPK1/2 Inhibitor that Potently Converts VEGF from Pro-angiogenic to Anti-angiogenic Isoform. Cell Chem Biol. 2018 Apr 19;25(4):460-470.e6.
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