218860

Casein Kinase II Inhibitor VIII

The Casein Kinase II Inhibitor VIII controls the biological activity of Casein Kinase II. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): Casein Kinase II Inhibitor VIII, CK2 Inhibitor VIII, DYRK1B Inhibitor, Flt-3 Inhibitor VII, 4-(2-(4-Methoxybenzamido)thiazol-5-yl)benzoic acid
• Empirical Formula (Hill Notation): C₁₈H₁₄N₂O₄S
• CAS Number: 1361229-76-6
• Molecular Weight: 354.38
• MDL number: MFCD28127268
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥99% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white
• solubility: DMSO: 50 mg/mL
• shipped in: wet ice
• storage temp.: 2-8°C
• SMILES string: O=C(C1=CC=C(OC)C=C1)NC2=NC=C(C3=CC=C(C(O)=O)C=C3)S2

Description

General description

A cell-permeable thiazolamide compound that acts as a potent, reversible, and ATP-competitive inhibitor against casein kinase-2/CK2 (IC₅₀ = 32 and 46 nM against CK2α and CK2α′, respectively), as well as DYRK1B and FLt-3 (82% and 76% inhibition, respectively, at 30 nM), while diplaying reduced or little potency toward other targets in a 70-kinase panel selectivity profile study. Shown to effectively block the proliferation of a variety of cancer cells (IC₅₀ = 2.6, 1.6, and 2.4 µM, in A549, HCT116, and MCF-7 cultures, respectively).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
CK2

Reversible: yes

Secondary Target
DYRK1B, Flt-3

Target IC₅₀: 32 and 46 nM for CK2&alpha

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 6 months at -20°C.

Other Notes

Hou, Z., et al. 2012. J. Med. Chem.55, 2899.

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