Merck, 5343500001, CDC-like Kinase Inhibitor, Cpd-2

General description
A cell-permeable imidazo[1,2-b]pyrazol derived compound that acts as a highly potent and specific inhibitor of CDC-like kinases (CLK; IC₅₀ = 1.1 and 2.4 nM for CLK1 and CLK2, respectively). Exhibits only trivial activity against serine-arginine protein kinases (SRPK) 1, 2, and 3 (IC₅₀ = 200, 310, and 230 nM, respectively). Induces pre-mRNA splicing alteration of multiple genes involved in growth and survival pathways resulting in the depletion of respective proteins. Causes a significance decrease in endogenous phosphorylated serine-arginine proteins and enlarges nuclear speckles in MDA-MB-468 cells. Induces apoptosis and Inhibits the growth of multiple cancer cell lines (GI₅₀ = 3.0, 1.9, 1.7, 2.2, 1.4, 2.0, and 0.6 µM for MDA-MB-468, A549, COLO205, HCT116, NCIH23, SW620, and COLO320 DM cells, respectively).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
CLK1
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Araki, S., et al. 2015. Plos One.10, e0116929.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)