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Merck

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.

別名:

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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この商品について

実験式（ヒル表記法）:
C23H18N4O3
CAS番号:
301836-43-1
分子量:
398.41
MDL number:
MFCD09037526
UNSPSC Code:
12352200
NACRES:
NA.77

主要文書

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製品名

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

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

保管分類

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

試験成績書（COA）

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以前この製品を購入いただいたことがある場合

文書ライブラリで、最近購入した製品の文書を検索できます。

文書ライブラリにアクセスする

Michael Ranes et al.
Molecular cell, 81(16), 3246-3261 (2021-08-06)
The Wnt/β-catenin pathway is a highly conserved, frequently mutated developmental and cancer pathway. Its output is defined mainly by β-catenin's phosphorylation- and ubiquitylation-dependent proteasomal degradation, initiated by the multi-protein β-catenin destruction complex. The precise mechanisms underlying destruction complex function have
Tianzhi Huang et al.
Molecular cell, 81(6), 1276-1291 (2021-02-05)
Aberrant cell proliferation is a hallmark of cancer, including glioblastoma (GBM). Here we report that protein arginine methyltransferase (PRMT) 6 activity is required for the proliferation, stem-like properties, and tumorigenicity of glioblastoma stem cells (GSCs), a subpopulation in GBM critical

グローバルトレードアイテム番号

カタログ番号GTIN
218696-1MGCN04055977202496

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