1596348-32-1
1596348-32-1 structure
- Name: KDM5-C70
- Chemical Name: 4288BE400F
- CAS Number: 1596348-32-1
- Molecular Formula: C17H28N4O3
- Molecular Weight: 336.429
- Catalog: Signaling Pathways Epigenetics Histone Demethylase
- Create Date: 2018-06-21 17:53:30
- Modify Date: 2024-01-10 16:40:42
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KDM5-C70 is an ethyl ester derivative of KDM5-C49 and a potent, cell-permeable and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels[1][2].
| Name | 4288BE400F |
|---|---|
| Synonyms |
4288BE400F
4-Pyridinecarboxylic acid, 2-[[[2-[[2-(dimethylamino)ethyl]ethylamino]-2-oxoethyl]amino]methyl]-, ethyl ester Ethyl 2-{[(2-{[2-(dimethylamino)ethyl](ethyl)amino}-2-oxoethyl)amino]methyl}isonicotinate |
| Description | KDM5-C70 is an ethyl ester derivative of KDM5-C49 and a potent, cell-permeable and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels[1][2]. |
|---|---|
| Related Catalog | |
| Target |
KDM5 histone demethylase[1][2] |
| In Vitro | KDM5-C70 (10-9-10-5 M; 7 days; MM.1S myeloma cells) treatment shows antiproliferative effects after 7 days of treatment at elevated concentrations (estimated 50% reduction of viability/proliferation for KDM5-C70 at ~20 μM)[1]. KDM5-C70 (50 μM; 7 days; MM.1S myeloma cells) treatment decreases the level of phosphorylation of retinoblastoma protein (Rb), while leaving the total level of phosphorylated Rb (pRb) unchanged, indicating impairment of cell cycle progression[1]. Chromatin immunoprecipitation followed by next-generation sequencing shows an increase in H3K4me3 levels around transcription start sites with KDM5-C70 but little change with GSK467A at 50 μM inhibitor concentrations[1]. Cell Viability Assay[1] Cell Line: MM.1S myeloma cells Concentration: 10-9-10-5 M Incubation Time: 7 days Result: Showed antiproliferative effects after 7 days of treatment at elevated concentrations. Western Blot Analysis[1] Cell Line: MM.1S myeloma cells Concentration: 50 μM Incubation Time: 7 days Result: Decreased the level of phosphorylation of retinoblastoma protein (Rb). |
| References |
| Density | 1.1±0.1 g/cm3 |
|---|---|
| Boiling Point | 466.6±45.0 °C at 760 mmHg |
| Molecular Formula | C17H28N4O3 |
| Molecular Weight | 336.429 |
| Flash Point | 236.0±28.7 °C |
| Exact Mass | 336.216156 |
| LogP | 0.75 |
| Vapour Pressure | 0.0±1.2 mmHg at 25°C |
| Index of Refraction | 1.525 |