D4476
Modify Date: 2024-01-10 09:32:13
D4476 structure
|
Common Name | D4476 | ||
|---|---|---|---|---|
| CAS Number | 301836-43-1 | Molecular Weight | 398.414 | |
| Density | 1.3±0.1 g/cm3 | Boiling Point | 675.0±55.0 °C at 760 mmHg | |
| Molecular Formula | C23H18N4O3 | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | 362.0±31.5 °C | |
Use of D4476D4476 is a potent, selective and cell-permeable inhibitor of casein kinase 1(CK1) with an IC50 value of 0.3 μM in vitro. |
| Name | 4-[4-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-pyridin-2-yl-1H-imidazol-2-yl]benzamide |
|---|---|
| Synonym | More Synonyms |
| Description | D4476 is a potent, selective and cell-permeable inhibitor of casein kinase 1(CK1) with an IC50 value of 0.3 μM in vitro. |
|---|---|
| Related Catalog | |
| Target |
CK1:0.3 μM (IC50) |
| In Vitro | D4476 is a potent and rather selective inhibitor of CK1 in vitro and in cells. In H4IIE hepatoma cells, D4476 specifically inhibits the phosphorylation of endogenous forkhead box transcription factor O1a (FOXO1a) on Ser322 and Ser325 within its MPD, without affecting the phosphorylation of other sites. CK1δ assayed at 0.1 mM ATP using a phosphorylated peptide TFRPRTSpSNASTIS corresponding to residues 312–325 of FOXO1a is inhibited with an IC50 value of 0.3 μM. The IC50 value for CK1δ decreases progressively as the concentration of ATP is lowered, indicating that D4476 is an ATP-competitive inhibitor of CK1. CK1[1]. |
| Cell Assay | D4476 is used for inhibition of Csnk1a1. D4476 is added to leukemia cells cultured in 96-well plates (5,000 cells per well) in medium supplemented with 10 ng/mL mIL-3. A D4476 dose titration is performed by adding 2.5 µM, 5 µM, 10 µM, 20 µM, and 40 µM D4476 to cell cultures in a final DMSO percentage of 0.4%. Similarly, D4476 is added to LSK cells cultured in SFEM medium supplemented with mTpo and mScf. The number of cells after 96 h of treatment is assessed with CountBright absolute counting beads using flow cytometry[2]. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 675.0±55.0 °C at 760 mmHg |
| Molecular Formula | C23H18N4O3 |
| Molecular Weight | 398.414 |
| Flash Point | 362.0±31.5 °C |
| Exact Mass | 398.137878 |
| PSA | 103.12000 |
| LogP | 3.84 |
| Vapour Pressure | 0.0±2.1 mmHg at 25°C |
| Index of Refraction | 1.663 |
| Storage condition | 2-8°C |
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
|---|---|
| RIDADR | NONH for all modes of transport |
|
Acetylation of Beclin 1 inhibits autophagosome maturation and promotes tumour growth.
Nat. Commun. 6 , 7215, (2015) Beclin 1, a protein essential for autophagy, regulates autophagy by interacting with Vps34 and other cofactors to form the Beclin 1 complex. Modifications of Beclin 1 may lead to the induction, inhibi... |
|
|
Small molecule-directed immunotherapy against recurrent infection by Mycobacterium tuberculosis.
J. Biol. Chem. 289(23) , 16508-16515, (2014) Tuberculosis remains the biggest infectious threat to humanity with one-third of the population infected and 1.4 million deaths and 8.7 million new cases annually. Current tuberculosis therapy is leng... |
|
|
The selectivity of protein kinase inhibitors: a further update.
Biochem. J. 408 , 297-315, (2007) The specificities of 65 compounds reported to be relatively specific inhibitors of protein kinases have been profiled against a panel of 70-80 protein kinases. On the basis of this information, the ef... |
| 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-(pyridin-2-yl)-1H-imidazol-2-yl]benzamide |
| Benzamide, 4-[4-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]- |
| CK1 Inhibitor |
| 4-[4-(2,3-Dihydro-1,4-benzodioxin-6-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]benzamide |
| Casein Kinase I Inhibitor |
| D4476 |