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Merck
CN

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.

别名:

Casein Kinase II Inhibitor VIII, CK2 Inhibitor VIII, DYRK1B Inhibitor, Flt-3 Inhibitor VII, 4-(2-(4-Methoxybenzamido)thiazol-5-yl)benzoic acid

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关于此项目

经验公式(希尔记法):
C18H14N2O4S
化学文摘社编号:
分子量:
354.38
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
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产品名称

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.

InChI

1S/C18H14N2O4S/c1-24-14-8-6-12(7-9-14)16(21)20-18-19-10-15(25-18)11-2-4-13(5-3-11)17(22)23/h2-10H,1H3,(H,22,23)(H,19,20,21)

InChI key

UPIVZLFKYMNZDG-UHFFFAOYSA-N

SMILES string

O=C(C1=CC=C(OC)C=C1)NC2=NC=C(C3=CC=C(C(O)=O)C=C3)S2

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

Quality Level

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

Disclaimer

Toxicity: Standard Handling (A)

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).

Other Notes

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

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Legal Information

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

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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