For research use only. Not for therapeutic Use.
SPHINX31 is a potent and selective SRPK1 inhibitor, with an IC50 of 5.9 nM. SPHINX31 inhibits phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1). SPHINX31 also decreases the mRNA expression of pro-angiogenic VEGF-A165a isoform. SPHINX31 can be used to research neovascular eye disease[1][2][3].
SPHINX31 (0.3-10 μM; 24 h) significantly down-regulates the expression of VEGF-A165a mRNA[2].
SPHINX31 (0.3 μM; 24 h) suppresses SRSF1 phosphorylation and nuclear localization[2].
SPHINX31 (0.3-10 μM; 24 h) decreases pre-tube formation and the rate of migration for human umbilical vein endothelial cells (HUVECs)[2].
SPHINX31 (200 μg/mL; twice daily topical eye drops) protects the retinal endothelial permeability barrier from diabetes-associated loss of integrity[3].
Catalog Number | I019194 |
CAS Number | 1818389-84-2 |
Synonyms | 5-pyridin-4-yl-N-[2-[4-(pyridin-2-ylmethyl)piperazin-1-yl]-5-(trifluoromethyl)phenyl]furan-2-carboxamide |
Molecular Formula | C27H24F3N5O2 |
Purity | ≥95% |
InChI | InChI=1S/C27H24F3N5O2/c28-27(29,30)20-4-5-23(35-15-13-34(14-16-35)18-21-3-1-2-10-32-21)22(17-20)33-26(36)25-7-6-24(37-25)19-8-11-31-12-9-19/h1-12,17H,13-16,18H2,(H,33,36) |
InChIKey | VURLRACCOCGFDB-UHFFFAOYSA-N |
SMILES | C1CN(CCN1CC2=CC=CC=N2)C3=C(C=C(C=C3)C(F)(F)F)NC(=O)C4=CC=C(O4)C5=CC=NC=C5 |
Reference | [1]. Batson J, et al. Development of Potent, Selective SRPK1 Inhibitors as Potential Topical Therapeutics for Neovascular Eye Disease. ACS Chem Biol. 2017 Mar 17;12(3):825-832. [2]. Supradit K, et al. Inhibition of serine/arginine-rich protein kinase-1 (SRPK1) prevents cholangiocarcinoma cells induced angiogenesis. Toxicol In Vitro. 2022 Aug;82:105385. [3]. C. Allen, et al. The SRPK1 inhibitor SPHINX31 prevents increased retinal permeability in a rodent model of diabetes. Acta Ophthalmologica. Volume 95, Issue S259. |