SPHINX31

SPHINX31 is a potent inhibitor of serine/arginine-rich protein kinase 1 (SRPK1, IC50 = 5.9 nM). It is selective for SRPK1 over a panel of 50 kinases at a concentration of 1 µM. SPHINX31 inhibits phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1), an SRPK1 substrate, in PC3 cells (EC50 = 360 nM) and increases expression of the anti-angiogenic VEGF-A165b splice variant in retinal pigment epithelial (RPE) cells. In vivo, SPHINX31 (2 µg per eye) inhibits blood vessel growth and macrophage infiltration in the eyes of a mouse model of choroidal neovascularization.Formal Name: 5-(4-pyridinyl)-N-[2-[4-(2-pyridinylmethyl)-1-piperazinyl]-5-(trifluoromethyl)phenyl]-2-furancarboxamide. CAS Number: 1818389-84-2. Molecular Formula: C27H24F3N5O2. Formula Weight: 507.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 33 mg/ml, DMF:PBS (pH7.2) (1:30): 0.03 mg/ml, DMSO: 10 mg/ml, Ethanol: 10 mg/ml. lambdamax: 269, 317 nm. SMILES: O=C(C1=CC=C(C2=CC=NC=C2)O1)NC(C=C(C(F)(F)F)C=C3)=C3N(CC4)CCN4CC5=CC=CC=N5. InChi Code: 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). InChi Key: VURLRACCOCGFDB-UHFFFAOYSA-N.