Biological Activity
Selective serine arginine protein kinase (SRPK) 1 inhibitor (Ki = 0.89 μM). Inhibits SRPK2 at higher concentrations. Does not significantly inhibit other SRPKs such as CLK1 and CLK4, or other classes of SR kinases. Down-regulates expression of VEGF165 but does not affect VEGF165b expression.
Compound Libraries
SRPIN340 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 349.35 |
| Formula | C18H18F3N3O |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 218156-96-8 |
| PubChem ID | 2797577 |
| InChI Key | DWFGGOFPIISJIT-UHFFFAOYSA-N |
| Smiles | O=C(C3=CC=NC=C3)NC1=C(N2CCCCC2)C=CC(C(F)(F)F)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. HCl | 17.47 | 50 | |
| DMSO | 34.94 | 100 | |
| ethanol | 34.94 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 349.35. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.86 mL | 14.31 mL | 28.62 mL |
| 5 mM | 0.57 mL | 2.86 mL | 5.72 mL |
| 10 mM | 0.29 mL | 1.43 mL | 2.86 mL |
| 50 mM | 0.06 mL | 0.29 mL | 0.57 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
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 PMID: 23761094
Fukuhara et al (2006) Utilization of host SR protein kinases and RNA-splicing machinery during viral replication. Proc.Natl.Acad.Sci.USA 103 11329 PMID: 16840555
Oltean et al (2012) SRPK1 inhibition in vivo: modulation of VEGF splicing and potential treatment for multiple diseases. Biochem.Soc.Trans. 40 831 PMID: 22817743
Keywords: SRPIN340, supplier, SR, Protein, Kinase, inhibitors, Phosphorylation, Inhibitor, 340(SRPIN)340, Serine-Arginine-Rich, Protein, inhibits, SRPK1, SRPK2, Other, Kinases, Other, Kinases, Tocris Bioscience
