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KDM5-C70 is an ethyl ester derivative of KDM5-C49 and functions as an effective, cell-permeable, pan-KDM5 histone demethylase inhibitor. It exhibits an antiproliferative effect in myeloma cells and induces a genome-wide elevation of H3K4me3 levels.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $37 | In Stock | |
5 mg | $56 | In Stock | |
10 mg | $81 | In Stock | |
25 mg | $143 | In Stock | |
50 mg | $258 | In Stock | |
100 mg | $515 | In Stock | |
200 mg | $737 | In Stock | |
500 mg | $1,130 | In Stock | |
1 mL x 10 mM (in DMSO) | $67 | In Stock |
Description | KDM5-C70 is an ethyl ester derivative of KDM5-C49 and functions as an effective, cell-permeable, pan-KDM5 histone demethylase inhibitor. It exhibits an antiproliferative effect in myeloma cells and induces a genome-wide elevation of H3K4me3 levels. |
In vitro | KDM5-C70 (50 μM; 7 days; MM.1S myeloma cells) treatment reduces the level of phosphorylation of retinoblastoma protein (Rb) while leaving the total level of phosphorylated Rb (pRb) unchanged, indicating impairment of cell cycle progression. KDM5-C70 (1 nM-10 μM; 7 days; MM.1S myeloma cells) treatment displays antiproliferative effects after 7 days of treatment at elevated concentrations (estimated 50% reduction of viability/proliferation for KDM5-C70 at ~20 μM). Chromatin immunoprecipitation followed by next-generation sequencing displays an enhanced H3K4me3 level around transcription start sites with KDM5-C70 but little change with GSK467A at 50 μM inhibitor concentrations [1]. |
Molecular Weight | 336.43 |
Formula | C17H28N4O3 |
Cas No. | 1596348-32-1 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 250 mg/mL (743.10 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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