[CAS NO. 301836-43-1] D 4476

Name: D 4476
Brand: Arctom Scientific
SKU: SLK-S7642

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PRODUCTS SPECIFICATIONS [301836-43-1]

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Catalog

SLK-S7642

Brand

Selleck

CAS

301836-43-1

DESCRIPTION [301836-43-1]

Overview

MDL	MFCD09037526
Molecular Weight	398.41
Molecular Formula	C23H18N4O3
SMILES	C(N)(=O)C1=CC=C(C=2NC(=C(N2)C3=CC=CC=N3)C=4C=C5C(=CC4)OCCO5)C=C1

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.5100 mL	12.5499 mL	25.0998 mL
5 mM	0.5020 mL	2.5100 mL	5.0200 mL
10 mM	0.2510 mL	1.2550 mL	2.5100 mL
50 mM	0.0502 mL	0.2510 mL	0.5020 mL

Description

D 4476 is a potent, selective, and cell-permeant inhibitor with of 200 nM and 300 nM in a cell-free assay for CK1 from Schizosaccharomyces pombe and CK1δ, respectively. Also acts as an inhibitor with of 500 nM.

Targets

CK1 from Schizosaccharomyces pombe ^[1]	CK1δ ^[1]	ALK5 ^[1]
200 nM	300 nM	500 nM

In vitro

D4476 (10 μM) effectively inhibits CK1 and ALK5 with the activities of about 7% and 22% versus control group, respectively. In H4IIE hepatoma cells, D4476 specifically inhibits the phosphorylation of endogenous forkhead box transcription factor O1a (FOXO1a) on Ser322 and Ser325, without affecting the phosphorylation of other sites. D4476 induces cytotoxicity in ANBL6, INA6 and RPMI8226 lines; MM1S and U266 lines are less sensitive; and OPM1 line is totally resistant. High concentrations (50 μM) D4476 induced toxicity in all multiple myeloma (MM) lines. In MM cells, D4476 increases the protein levels of TP53, P27, and FADD, as well as the cell cycle progression and induction of apoptosis. Treatment of leukemia stem cells (LSCs) with D4476 shows highly selective killing of LSCs over normal HSPCs.

References

[1] Rena G, et al. EMBO Rep. 2004, 5(1), 60-65.
[2] Hu Y, et al. Leukemia. 2015, 29(2), 474-482.
[3] J?r?s M, et al. J Exp Med. 2014,211(4), 605-612.
[4] Bain J, et al. Biochem J. 2003, 371(Pt 1), 199-204.

Synonyms

Benzamide, 4-[4-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]-

4-[4-(2,3-Dihydro-1,4-benzodioxin-6-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]benzamide

D 4476

Casein kinase I inhibitor