SRPKIN-1 is a covalent and irreversible SRPK1/2 inhibitor with IC50s of 35.6 and 98 nM, respectively. Anti-angiogenesis effect.
IC50&Target
IC50: 35.6 nM (SRPK1), 98 nM (SRPK2)
体外研究
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.
Cell Viability Assay
Cell 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.
体内研究
SRPKIN-1 (50 nM, 300 nM,1 μL, 5 times) blocks angiogenesis in a CNV mouse model through VEGF alternative splicing.
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.
分子量
472.53
CAS号
2089226-94-6
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, stored under nitrogen, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
溶解性数据
In Vitro:
DMSO : ≥ 110 mg/mL (232.79 mM)
*"≥" means soluble, but saturation unknown.
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
2.1163 mL
10.5813 mL
21.1627 mL
5 mM
0.4233 mL
2.1163 mL
4.2325 mL
10 mM
0.2116 mL
1.0581 mL
2.1163 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: