1651890-44-6
1651890-44-6 structure
- Name: Pyridoclax
- Chemical Name: 3'-Methyl-3''-[(E)-2-phenylvinyl]-3,2':5',2'':5'',3'''-quaterpyridine
- CAS Number: 1651890-44-6
- Molecular Formula: C29H22N4
- Molecular Weight: 426.512
- Catalog: Signaling Pathways Apoptosis Bcl-2 Family
- Create Date: 2018-03-08 07:52:24
- Modify Date: 2024-01-30 17:32:46
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Pyridoclax is a potential Mcl-1 inhibitor.
| Name | 3'-Methyl-3''-[(E)-2-phenylvinyl]-3,2':5',2'':5'',3'''-quaterpyridine |
|---|---|
| Synonyms |
3,2':5',2'':5'',3'''-Quaterpyridine, 3'-methyl-3''-[(E)-2-phenylethenyl]-
3'-Methyl-3''-[(E)-2-phenylvinyl]-3,2':5',2'':5'',3'''-quaterpyridine Pyridoclax |
| Description | Pyridoclax is a potential Mcl-1 inhibitor. |
|---|---|
| Related Catalog | |
| Target |
Mcl-1 |
| In Vitro | Pyridoclax directly binds to Mcl-1. Without cytotoxic activity when administered as a single agent, Pyridoclax induces apoptosis in combination with Bcl-xL-targeting siRNA or with ABT-737 in ovarian, lung, and mesothelioma cancer cells[1]. Pyridoclax directly binds to Mcl-1, and hence sensitizes ovarian carcinoma cells to Bcl-xL-targeting strategies. Pyridoclax induces apoptosis in ovarian, and also in lung, and mesothelioma cancer cells when it is administrated in combination with Bcl-xL-targeting siRNA or Bcl-xL targeting molecules such as ABT-737 or its orally available derivative ABT-263[2]. |
| Kinase Assay | For donor saturating assays, Hela cells are seeded on 12-well plates and transfected with 200 ng/well of plasmid pRluc-BimL coding for BRET donor and an increasing quantity of BRET acceptor plasmids peYFP-Mcl-1 (or with pCMV-Mcl-1 as a control). Twenty-four hours after transfection, cells are trypsinized, reseeded into white flat bottom 96-well plates, and incubated for another day before measurements. A single donor/acceptor ratio (200/800) is used to carry out the drug treatment assay. After reseeding, cells are then subject to a 16 h Pyridoclax treatment. Light emission at 485 and 530 nm is measured consecutively using the Mithras fluorescence-luminescence detector LB 940 after adding the luciferase substrate, coelenterazine H, at a final concentration of 5 μM. BRET ratios are calculated[1]. |
| References |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 663.6±55.0 °C at 760 mmHg |
| Molecular Formula | C29H22N4 |
| Molecular Weight | 426.512 |
| Flash Point | 288.5±24.5 °C |
| Exact Mass | 426.184448 |
| LogP | 5.64 |
| Vapour Pressure | 0.0±1.9 mmHg at 25°C |
| Index of Refraction | 1.676 |
| Storage condition | 2-8℃ |