| Identification | Back Directory | [Name]
4-(4-(2,3-DIHYDROBENZO[1,4]DIOXIN-6-YL)-5-PYRIDIN-2-YL-1H-IMIDAZOL-2-YL)BENZAMIDE | [CAS]
301836-43-1 | [Synonyms]
D4476
D4467
CS-1031
D4476 (D-4476)
D4476;D 4476;D-4476
Casein Kinase I Inhibitor
Casein Kinase I Inhibitor, D4476
CASEIN KINASE I INHIBITOR; D 4476; D-4476
Casein Kinase I Inhibitor, D4476 - CAS 301836-43-1 - Calbiochem
Casein Kinase,inhibit,Autophagy,D-4476,D4476,Inhibitor,Apoptosis
4-(4-(2,3-DIHYDROBENZO[1,4]DIOXIN-6-YL)-5-PYRIDIN-2-YL-1H-IMIDAZOL-2-YL)BENZAMIDE
4-[4-(2,3-Dihydro-1,4-benzodioxin-6-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]benzamide
Benzamide,4-[4-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]-
4-(4-(2,3-DIHYDROBENZO[B][1,4]DIOXIN-6-YL)-5-(PYRIDIN-2-YL)-1H-IMIDAZOL-2-YL)BENZAMIDE
4-[4-(2,3-Dihydro-1,4-benzodioxin-6-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]benzamide D4476 | [Molecular Formula]
C23H18N4O3 | [MDL Number]
MFCD09037526 | [MOL File]
301836-43-1.mol | [Molecular Weight]
398.41 |
| Chemical Properties | Back Directory | [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 | [form ]
solid | [pka]
10.16±0.10(Predicted) | [color ]
light yellow |
| Hazard Information | Back Directory | [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. | [Definition]
ChEBI: 4-[4-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]benzamide is a member of imidazoles. | [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. | [storage]
Store at -20°C | [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. |
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