5-Methyl-N-(2-morpholino-5-(trifluoromethyl)phenyl)furan-2-carboxamide

SPHINX is a selective SRPK1 inhibitor with an IC50 value of 0.58 μM. SPHINX effectively reduces Choroidal Neovascularization (CNV) in vivo. SPHINX can be used for the research of (age-related macular degenaration) AMD[1].

Research Areas >> Others

Signaling Pathways >> Cell Cycle/DNA Damage >> SRPK

IC50: 0.58 μM (SRPK1)[1]

SPHINX (10 μM; 2 h) affects EGF-induced phosphorylation of SRSF1 and SRSF2[1]. SPHINX (5 μM; 24 h) reduces the expression of VEGF165 relative to GAPDH control either in primary RPE and ARPE-19 cell lines[1]. Western Blot Analysis[1] Cell Line: ARPE-19 cell line Concentration: 10 μM Incubation Time: 2 hours Result: Blocked EGF-induced phosphorylation of SRSF1 and SRSF2.

SPHINX (10 ng; i.o. on laser photocoagulation day 0 and day 7) affects neovascular growth in vivo[1]. SPHINX (25 ng; i.o. on laser photocoagulation day 0 and day 7) affects the CNV area in CNV rats[1]. Animal Model: C57/B6 mice with laser-induced CNV[1] Dosage: 10 ng Administration: Intraocular injection; 10 ng on laser photocoagulation day 0 and day 7 Result: Significantly reduced neovascular growth compared with saline-injected controls. Animal Model: Norway Brown rats with laser-induced choroidal neovascularization[1] Dosage: 25 ng (10 ng/uL) Administration: Intraocular injection; 25 ng (10 ng/uL) on laser photocoagulation day 0 and day 7 Result: Significantly reduced the CNV area compared with saline injected controls.

[1]. Gammons MV, et al. Topical antiangiogenic SRPK1 inhibitors reduce choroidal neovascularization in rodent models of exudative AMD. Invest Ophthalmol Vis Sci. 2013 Sep 5;54(9):6052-62.