SRPK inhibitor Property

Boiling point:

395.9±42.0 °C(Predicted)

Density 

1.306±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO: soluble20mg/mL, clear

form 

powder

pka

11.09±0.70(Predicted)

color 

white to beige

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.

Safety

Hazard Codes 

Xn

Risk Statements 

22

WGK Germany 

3

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P330Rinse mouth.

P501Dispose of contents/container to..…

SRPK inhibitor Chemical Properties,Usage,Production

Description

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.

Uses

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

References

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