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D4476

🥰Excellent
Catalog No. T2449Cas No. 301836-43-1
Alias D 4476, Casein Kinase I Inhibitor

D4476 (Casein Kinase I Inhibitor) is an effective, selective, and cell-permeant CK1 (casein kinase 1) inhibitor( IC50=300 nM in a cell-free assay).

D4476

D4476

🥰Excellent
Purity: 99.96%
Catalog No. T2449Alias D 4476, Casein Kinase I InhibitorCas No. 301836-43-1
D4476 (Casein Kinase I Inhibitor) is an effective, selective, and cell-permeant CK1 (casein kinase 1) inhibitor( IC50=300 nM in a cell-free assay).
Pack SizePriceAvailabilityQuantity
1 mg34 €In Stock
2 mg47 €In Stock
5 mg67 €In Stock
10 mg82 €In Stock
25 mg153 €In Stock
50 mg226 €In Stock
100 mg407 €In Stock
200 mg597 €In Stock
500 mg937 €In Stock
1 mL x 10 mM (in DMSO)74 €In Stock
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Purity:99.96%
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Product Introduction

Bioactivity
Description
D4476 (Casein Kinase I Inhibitor) is an effective, selective, and cell-permeant CK1 (casein kinase 1) inhibitor( IC50=300 nM in a cell-free assay).
Targets&IC50
CK1:300 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.[1] 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.[2] Treatment of leukemia stem cells (LSCs) with D4476 shows highly selective killing of LSCs over normal HSPCs.[3]
Kinase Assay
CK1 kinase assay: All protein kinase assays (25 μL) are carried out at room temperature (21℃). Assays are performed for 40 min using a Biomek 2000 Laboratory Automation Workstation in a 96-well format. The concentrations of magnesium acetate and [γ-33P]ATP (800 cpm/pmol) in the assays are 10 mM and 0.1 mM, respectively. Assays are initiated with MgATP and stopped by the addition of 5 μL of 0.5 M orthophosphoric acid. Aliquots are then spotted on to P30 ?ltermats, washed four times in 75 mM phosphoric acid to remove ATP, once in methanol, then dried and counted for radioactivity. CK1 δ (5-20 m-units), diluted in 20 mM Hepes, pH 7.5, 0.15 M NaCl, 0.1 mM EGTA, 0.1% (v/v) Triton X-100, 5 mM dithiothreitol, 50% (v/v) glycerol, is assayed against the peptide RRKDLHDDEEDEAMSITA in an incubation containing 20 mM Hepes, pH 7.5, 0.15 M NaCl, 0.1 mM EDTA, 5 mM DTT, 0.1% (v/v) Triton X-100 and 0.5 mM substrate peptide.
Cell Research
MM cells are seeded in triplicate into 96-well plates in 100 μL culture media. D4476 is added to each well at concentrations of 0, 5, 10, 20, 30, 40, and 50 μM in another 100 μL culture media. Cell viability is measured with MTT at the 72 h drug exposure. Absorbance is measured at 570 nm with spectrophotometer.(Only for Reference)
AliasD 4476, Casein Kinase I Inhibitor
Chemical Properties
Molecular Weight398.41
FormulaC23H18N4O3
Cas No.301836-43-1
SmilesNC(=O)c1ccc(cc1)-c1nc(c([nH]1)-c1ccccn1)-c1ccc2OCCOc2c1
Relative Density.1.338 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 40 mg/mL (100.4 mM), Sonication is recommended.
Ethanol: 19.9 mg/mL (50 mM)
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.5100 mL12.5499 mL25.0998 mL125.4989 mL
5 mM0.5020 mL2.5100 mL5.0200 mL25.0998 mL
10 mM0.2510 mL1.2550 mL2.5100 mL12.5499 mL
20 mM0.1255 mL0.6275 mL1.2550 mL6.2749 mL
50 mM0.0502 mL0.2510 mL0.5020 mL2.5100 mL
DMSO
1mg5mg10mg50mg
100 mM0.0251 mL0.1255 mL0.2510 mL1.2550 mL

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