Biochem/physiol Actions

Target IC₅₀: 0.2 & 2.4 µ

Reversible: yes

Primary TargetCK2, SRPK1

Cell permeable: yes

General description

A cell-permeable, bioavailable, non-toxic thiadiazolopyrimidinone based compound that acts a potent, reversible and ATP-competitive dual inhibitor of CK2 & SRPK1 (IC₅₀ = 0.2 & 2.4 µM, respectively). Displays excellent selectivity in a 306-kinase panel (% inhibition at 10 µM = 82.5, 70.9, 59.9 & 13.7 for CK2α1/β, CK2α2/β, SRPK1 & SRPK2, respectively). Synergistically suppresses VEGF production in a time and dose-dependent manner and down-regulates several angiogenesis genes expression (10 µM in ARPE-19 cells). Shown to be highly efficacious than SRPIN340 (Cat. No. 504293) and significantly inhibit choroidal neovascularization in a mouse model of age-related macular degeneration (intravitreous injection or topical administration). Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

A cell-permeable, bioavailable, non-toxic thiadiazolopyrimidinone based compound that acts a potent, reversible and ATP-competitive dual inhibitor of CK2 & SRPK1 (IC₅₀ = 0.2 & 2.4 µM, respectively). Displays excellent selectivity in a 306-kinase panel (% inhibition at 10 µM = 82.5, 70.9, 59.9 & 13.7 for CK2α1/β, CK2α2/β, SRPK1 & SRPK2, respectively). Synergistically suppresses VEGF production in a time and dose-dependent manner and down-regulates several angiogenesis genes expression (10 µM in ARPE-19 cells). Shown to be highly efficacious than SRPIN340 (Cat. No. 504293) and significantly inhibit choroidal neovascularization in a mouse model of age-related macular degeneration (intravitreous injection or topical administration).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Morooka, S., et al. 2015. Mol. Pharmacol.88, 316.

Packaging

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)