For research use only. Not for therapeutic Use.
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[1][2][3].
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].
| Catalog Number | I036636 |
| CAS Number | 380572-02-1 |
| Synonyms | 5-amino-6-[(E)-(3-methoxy-4-oxocyclohexa-2,5-dien-1-ylidene)methyl]-2-(trifluoromethyl)-[1,3,4]thiadiazolo[3,2-a]pyrimidin-7-one |
| Molecular Formula | C14H9F3N4O3S |
| Purity | ≥95% |
| InChI | InChI=1S/C14H9F3N4O3S/c1-24-9-5-6(2-3-8(9)22)4-7-10(18)21-13(19-11(7)23)25-12(20-21)14(15,16)17/h2-5H,18H2,1H3/b6-4+ |
| InChIKey | JCSNCMXWHKOYJB-GQCTYLIASA-N |
| SMILES | COC1=CC(=CC2=C(N3C(=NC2=O)SC(=N3)C(F)(F)F)N)C=CC1=O |
| Reference | [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. |
