SRPKIN-1 - SRPK 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESRPKIN-1Cat. No.: HY-116856CAS No.: 2089226-94-6分式: CHFNOS分量: 472.53作靶点: SRPK作通路: Cell Cycle/DNA Damage储存式: Please store the product under the recommended conditions inthe COA.溶解性数据体外实验 DMSO : 115 mg/mL (243.37 mM; Need ultrason

2、ic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 5.75 mg/mL (12.17 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 5.75 mg/mL (12.17 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE物活性 SRPKIN-1共价，不可逆的 SRPK1/2 抑制剂，IC50 分别为35.6 和 98 nM。有抗管成

3、作 1。IC50 & Target IC50: 35.6 nM (SRPK1), 98 nM (SRPK2) 1体外研究 SRPKIN-1 treatment at 200 nM (10, 50, 100, 200 nM, 16 hours) significantly reduces SR proteinphosphorylation at the steady state with or without washout 1.SRPK-IN-1 potently converts VEGF from pro-angiogenic to anti-angiogenic isoform 1.Ce

4、ll Viability Assay 1Cell Line: Ba/F3 cellsConcentration: 0-10000 nMIncubation Time: 72 hResult: Potently decreased the level of SR phosphorylation in a dose-dependent manner, leadingto increased VEGF-A165b RNA as well as protein even at a dose of 200 nM 1.体内研究 SRPKIN-1 (50 nM, 300 nM,1 L, 5 times) b

5、locks angiogenesis in a CNV mouse model through VEGFalternative splicing 1.Animal Model: Mice 1Dosage: 50 nM, 300 nM, 1 LAdministration: Intravitreal injection, 5 timesResult: SRPKIN-1-treated mice is significantly suppressed in a dose-dependent manner basedupon measurement of the CNV area 1.REFEREN

6、CES1. Hatcher JM, et al. SRPKIN-1: A Covalent SRPK1/2 Inhibitor that Potently Converts VEGF from Pro-angiogenic to Anti-angiogenicIsoform. Cell Chem Biol. 2018 Apr 19;25(4):460-470.e6.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-