| Identification | Back Directory | [Name]
(E)-6-(4-hydroxy-3-methoxybenzylidene)-5-imino-2-(trifluoromethyl)-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-7(6H)-one | [CAS]
380572-02-1 | [Synonyms]
(E)-6-(4-hydroxy-3-methoxybenzylidene)-5-imino-2-(trifluoromethyl)-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-7(6H)-one | [Molecular Formula]
C14H9F3N4O3S | [MOL File]
380572-02-1.mol | [Molecular Weight]
370.31 |
| Chemical Properties | Back Directory | [Boiling point ]
428.5±55.0 °C(Predicted) | [density ]
1.69±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
9.28±0.35(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Description]
SRPIN-803 is a selective dual inhibitor of SRPK1 and CK2. | [Uses]
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]. | [in vivo]
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]. | [IC 50]
CK2: 203 nM (IC50); SRPK1: 2.4 μM (IC50) | [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. DOI:10.1021/acsomega.1c04576
[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. DOI:10.1016/j.ejmech.2020.112267
[3] Morooka S, et, al. Identification of a Dual Inhibitor of SRPK1 and CK2 That Attenuates Pathological Angiogenesis of Macular Degeneration in Mice. DOI:10.1124/mol.114.097345 |
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PHARMEKS Ltd.
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+7 (495) 702-9648 |
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www.pharmeks.com |
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