SRPIN803 is a potent CK2 and SRPK1 dual inhibitor, with IC50s of 203 nM and 2.4 μM, respectively. SRPIN803 exhibits antiangiogenic activity. SRPIN803 can be used for the research of age-related macular degeneration.
SRPIN803 inhibits the activity of SRPK1 toward LBRNt (62-92), with an IC50 of 7.5 μM, while the c(RGDyK)-conjugated compounds completely abolishes its inhibitory activity[2].SRPIN803 has slightly cytostatic activity against Hcc827, PC3, and U87 (GI50=80-98 μM)[2].
SRPIN803 (topical administration of eye ointment) significantly inhibits choroidal neovascularization in a mouse model of age-related macular degeneration[2].SRPIN803 (100 μM; 72 h) inhibit zebrafish angiogenesis[2].SRPIN803 (4.6 nL of 10 μM; microinjection; 72 h) block angiogenesis in the developing embryo at the one-cell stage of zebrafish[2].
References:
[1]. Leonidis G, et, al. Synthesis and Biological Evaluation of a c(RGDyK) Peptide Conjugate of SRPIN803. ACS Omega. 2021 Oct 14;6(42):28379-28393.
[2]. Vedove AD, et, al. A novel class of selective CK2 inhibitors targeting its open hinge conformation. Eur J Med Chem. 2020 Jun 1;195:112267.
[3]. Morooka S, et, al. Identification of a Dual Inhibitor of SRPK1 and CK2 That Attenuates Pathological Angiogenesis of Macular Degeneration in Mice.