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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).
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
28-July-2017 JSW
Synonyms
CLK Inhibitor, Cpd-2
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).
Form
Light pink solid
Intert gas (Yes/No)
Packaged under inert gas
Chemical formula
C₂₀H₂₀N₆O
Purity
≥98% by HPLC
Solubility
DMSO (100 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
