| 货号 | 16284-1mg |
| 描述 | Serine/arginine-rich protein kinase 1 (SRPK1) targets proteins that contain multiple serine/arginine (SR) dipeptides, including SR-rich splicing factor 1, SRSF1.1 SRPIN340 is an isonicotinamide compound that inhibits SRPK1 (Ki = 0.89 µM).2 It is about 10-fold less effective against SRPK2 and does not inhibit the related SRPKs, Clk1 and Clk4.2 SRPIN340 suppresses the propagation of Sindbis virus in Vero cells and the replication of hepatitis C virus in Huh7/Rep-Feo-2a cells.2,3 By blocking SRPK1-mediated phosphorylation of SRSF1, SRPIN340 modulates alternative splicing of VEGF, reducing neovascularization both in cells and in animals.4,5,6 |
| 别名 | SRPK Inhibitor; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Ghosh, G. and Adams, J.A. Phosphorylation mechanism and structure of serine-arginine protein kinases. FEBS Journal 278(4), 587-597 (2011). 2.Fukuhara, T.,Hosoya, T.,Shimizu, S., et al. Utilization of host SR protein kinases and RNA-splicing machinery during viral replication. Proceedings of the National Academy of Sciences of the United States of America 103(30), 11329-11333 (2006). 3.Karakama, Y.,Sakamoto, N.,Itsui, Y., et al. Inhibition of hepatitis C virus replication by a specific inhibitor of serine-arginine-rich protein kinase. Antimicrobial Agents and Chemotherapy 54(8), 3179-3186 (2010). 4.Ghadimi, M.P.,Lopez, G.,Torres, K.E., et al. Targeting the PI3K/mTOR axis, alone and in combination with autophagy blockade, for the treatment of malignant peripheral nerve sheath tumors. Molecular Cancer Therapeutics 11(8), 1758-1769 (2012). 5.Gammons, M.V.R.,Dick, A.D.,Harper, S.J., et al. SRPK1 inhibition modulates VEGF splicing to reduce pathological neovascularization in a rat model of retinopathy of prematurity. Invest.Ophthalmol.Vis.Sci. 54(8), 5797-5806 (2013). 6.Dong, Z.,Noda, K.,Kanda, A., et al. Specific inhibition of serine/arginine-rich protein kinase attenuates choroidal neovascularization. Molecular Vision 19, 536-543 (2013). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 349.4 |
| 分子式 | C18H18F3N3O |
| CAS号 | 218156-96-8 |
| 稳定性 | ≥ 2 years |
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