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Merck
CN

218696

Casein Kinase I Inhibitor, D4476

The Casein Kinase I Inhibitor, D4476, also referenced under CAS 301836-43-1, controls the biological activity of Casein Kinase I. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

别名:

Casein Kinase I Inhibitor, D4476, CK1 Inhibitor, 4-(4-(2,3-Dihydrobenzo[1,4]dioxin-6-yl)-5-pyridin-2-yl-1H-imidazol-2-yl)benzamide

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关于此项目

经验公式（希尔记法）:
C23H18N4O3
化学文摘社编号:
301836-43-1
分子量:
398.41
MDL number:
MFCD09037526
UNSPSC Code:
12352200
NACRES:
NA.77

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产品名称

Casein Kinase I Inhibitor, D4476, The Casein Kinase I Inhibitor, D4476, also referenced under CAS 301836-43-1, controls the biological activity of Casein Kinase I. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

SMILES string

[nH]1c(nc(c1c5ncccc5)c3cc4c(cc3)OCCO4)c2ccc(cc2)C(=O)N

InChI

1S/C23H18N4O3/c24-22(28)14-4-6-15(7-5-14)23-26-20(21(27-23)17-3-1-2-10-25-17)16-8-9-18-19(13-16)30-12-11-29-18/h1-10,13H,11-12H2,(H2,24,28)(H,26,27)

InChI key

DPDZHVCKYBCJHW-UHFFFAOYSA-N

assay

≥95% (HPLC)

form

crystalline solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

solubility

DMSO: 40 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

100

相关类别

Biochem/physiol Actions

Cell permeable: yes
Product competes with ATP.
Reversible: yes
Target IC50: 0.2 µM against CK1 from S. pombe; 0.3 µM for CK1δ 0.5 µM against ALK5

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell-permeable triaryl substituted imidazolo compound that acts as a potent, reversible and relatively specific ATP-competitive inhibitor of CK1 (IC50 = 0.2 µM from S. pombe; 0.3 µM for CK1δ) and ALK5 (IC50 = 0.5 µM). A weak inhibitor of p38α MAP kinase (IC50 = 12 µM) and only weakly affects the activities of a panel of kinases tested, including PKB, SGK and GSK-3β. Suppresses the site-specific phosphorylation (Ser322 and Ser325) and nuclear exclusion of FOXO1a in H4IIE hepatoma cells. Shown to be ~10-fold more potent than IC261 (Cat. No. 400090; IC50 = 2.5 µM for CK1).
A cell-permeable, reversible, potent, and relatively specific ATP-competitive inhibitor of CK1 (IC50 = 200 nM from S. pombe; 0.3 µM for CK1δ) and ALK5 (IC50 = 500 nM). A weak inhibitor of p38α MAP kinase (IC50 = 12 µM) and several other kinases tested, including PKB, SGK, and GSK-3β. Suppresses the site-specific phosphorylation (Ser322 and Ser325) and nuclear exclusion of FOXO1A in H4IIE hepatoma cells. Shown to be ~ 10-fold more potent than IC261 (Cat. No. 400090; IC50 = 2.5 µM for CK1).

Packaging

Packaged under inert gas

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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