- D4476
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- $36.00 / 1mg
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2024-11-19
- CAS:301836-43-1
- Min. Order:
- Purity: 99.96%
- Supply Ability: 10g
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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 |
| 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 | D4476 has been used as a casein kinase I inhibitor (CKI) in various experiments. | 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 | +4°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. |
| 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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