5.34350

CDC-like Kinase Inhibitor, Cpd-2

• Synonym(s): CDC-like Kinase Inhibitor, Cpd-2, CLK Inhibitor, Cpd-2
• Empirical Formula (Hill Notation): C₂₀H₂₀N₆O
• Molecular Weight: 360.41
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Assay: ≥98% (HPLC)
• Quality Level: 100
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: light pink
• solubility: DMSO: 100 mg/mL
• storage temp.: 2-8°C

Description

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable