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4-(4-(2,3-DIHYDROBENZO[1,4]DIOXIN-6-YL)-5-PYRIDIN-2-YL-1H-IMIDAZOL-2-YL)BENZAMIDE

CAS No.：301836-43-1

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4-(4-(2,3-DIHYDROBENZO[1,4]DIOXIN-6-YL)-5-PYRIDIN-2-YL-1H-IMIDAZOL-2-YL)BENZAMIDE Basic information

Product Name:	4-(4-(2,3-DIHYDROBENZO[1,4]DIOXIN-6-YL)-5-PYRIDIN-2-YL-1H-IMIDAZOL-2-YL)BENZAMIDE
Synonyms:	4-(4-(2,3-DIHYDROBENZO[1,4]DIOXIN-6-YL)-5-PYRIDIN-2-YL-1H-IMIDAZOL-2-YL)BENZAMIDE;D4476;4-[4-(2,3-Dihydro-1,4-benzodioxin-6-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]benzamide;Casein Kinase I Inhibitor;4-[4-(2,3-Dihydro-1,4-benzodioxin-6-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]benzamide D4476;Casein Kinase I Inhibitor, D4476;D4476;D 4476;D-4476;Benzamide,4-[4-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]-
CAS:	301836-43-1
MF:	C23H18N4O3
MW:	398.41
EINECS:
Product Categories:	Inhibitors;Signalling
Mol File:	301836-43-1.mol

4-(4-(2,3-DIHYDROBENZO[1,4]DIOXIN-6-YL)-5-PYRIDIN-2-YL-1H-IMIDAZOL-2-YL)BENZAMIDE Chemical Properties

Boiling point	675.0±55.0 °C(Predicted)
density	1.338±0.06 g/cm3(Predicted)
storage temp.	2-8°C
solubility	DMSO: ~20mg/mL
pka	10.16±0.10(Predicted)
form	solid
color	light yellow

Safety Information

WGK Germany

MSDS Information

4-(4-(2,3-DIHYDROBENZO[1,4]DIOXIN-6-YL)-5-PYRIDIN-2-YL-1H-IMIDAZOL-2-YL)BENZAMIDE Usage And Synthesis

Description	D 4476 is a cell-permeant inhibitor of casein kinase 1 (CK1; IC₅₀ = 200 nM from S. pombe, 300 nM for CK1δ). It is a less effective inhibitor of PKD1 (IC₅₀ = 9.1 μM) and p38α MAPK (IC₅₀ = 5.8 μM), and only weakly affects the activities of a panel of kinases tested. D 4476 blocks CK1-mediated phosphorylation of FOXO1a, RhoB, and p53. As an inhibitor of ALK5, D 4476 prevents Smad3 activation and suppresses TGF-β1-induced gene expression without cytotoxicity in A498 cells.
Uses	4-[4-(2,3-Dihydro-1,4-benzodioxin-6-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]-benzamide is a novel CK1 inhibitor that potently inhibits CK1 with an IC50 value of 78 nM.
Uses	D4476 has been used as a casein kinase I inhibitor (CKI) in various experiments.
Biological Activity	Selective inhibitor of casein kinase 1 (CK1) and TGF- β type-I receptor (ALK5) that displays > 20-fold selectivity over SAPK2/p38 and a much greater selectivity over all other protein kinases tested. Suppresses site-specific phosphorylation and nuclear exclusion of FOXO1a.
Biochem/physiol Actions	D4476 may prevent or enhance apoptosis. It triggers tumor suppressor p53 and impairs transcription factor E2F-1.
references	1. g. rena, j. bain, m. elliott and p. cohen, embo rep 2004, 5, 60-65. 2. v. tillement, i. lajoie-mazenc, a. casanova, c. froment, m. penary, d. tovar, r. marquez, b. monsarrat, g. favre and a. pradines, exp cell res 2008, 314, 2811-2821. 3. a. s. huart, n. j. maclaine, d. w. meek and t. r. hupp, j biol chem 2009, 284, 32384-32394.

4-(4-(2,3-DIHYDROBENZO[1,4]DIOXIN-6-YL)-5-PYRIDIN-2-YL-1H-IMIDAZOL-2-YL)BENZAMIDE Preparation Products And Raw materials

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