218156-96-8

Serine/arginine-rich protein kinase 1 (SRPK1) targets proteins that contain multiple serine/arginine (SR) dipeptides, including SR-rich splicing factor 1, SRSF1. SRPIN340 is an isonicotinamide compound that inhibits SRPK1 (K_i = 0.89 μM). It is about 10-fold less effective against SRPK2 and does not inhibit the related SRPKs, Clk1 and Clk4. SRPIN340 suppresses the propagation of Sindbis virus in Vero cells and the replication of hepatitis C virus in Huh7/Rep-Feo-2a cells. By blocking SRPK1-mediated phosphorylation of SRSF1, SRPIN340 modulates alternative splicing of VEGF, reducing neovascularization both in cells and in animals.

SRPIN340 is a SRPK1 kinase inhibitor, which shows potential novel targeted therapeutic strategy in prostate cancer.

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1) Fukuhara?et al.?(2006),?Utilization of host SR protein kinases and RNA-splicing machinery during viral replication; Proc. Natl. Acad. Sci. USA,?103?11329 2) Gammons?et al.?(2013),?SRPK1 inhibition modulates VEGF splicing to reduce pathological neovascularization in a rat model of retinopathy of prematurity; Invest. Ophthalmol. Vis. Sci.,?54?5797 3) Gammons?et al.?(2014),?Targeting SRPK1 to control VEGF-mediated tumour angiogenesis in metastatic melanoma; Br. J. Cancer,?111?477