1628208-23-0
1628208-23-0 structure
- Name: CPI-455
- Chemical Name: 6-Isopropyl-7-oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carbonitrile
- CAS Number: 1628208-23-0
- Molecular Formula: C16H14N4O
- Molecular Weight: 278.309
- Catalog: Signaling Pathways Epigenetics Histone Demethylase
- Create Date: 2018-04-30 13:49:05
- Modify Date: 2024-01-02 23:33:12
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CPI-455 is a specific KDM5 inhibitor.
| Name | 6-Isopropyl-7-oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carbonitrile |
|---|---|
| Synonyms |
6-Isopropyl-7-oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carbonitrile
Pyrazolo[1,5-a]pyrimidine-3-carbonitrile, 4,7-dihydro-6-(1-methylethyl)-7-oxo-5-phenyl- CPI-455 |
| Description | CPI-455 is a specific KDM5 inhibitor. |
|---|---|
| Related Catalog | |
| Target |
KDM5[1] |
| In Vitro | CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4 trimethylation (H3K4me3) and decreases the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents[1]. CPI-455, with high measured affinity for the target KDM5 proteins. Within 24 hours, increases in H3K4me3, but not H3K4me2, are observed after exposure to either of the two active compounds, CPI-455 and CPI-766, in a dosedependent manner. IC50 calculation for KDM5 Inhibitor CPI0455 in 3 luminal breast cancer cell lines MCF-7, T-47 and EFM-19 are 35.4, 26.19 and 16.13 μM, respectively[2]. |
| Cell Assay | MCF-7 is a luminal breast cancer cell line. MCF-7 is grown in MEM supplemented with 10% fetal bovine serum (FBS) and is incubated at 37°C with a 5% CO2 atmosphere. For each treatment condition, 2.5×105 MCF-7 cells are plated in T25 flask and allowed to rest overnight. The following day, the media is aspirated and replaced with media containing DAC at a final concentration of 62.5 nM. DAC media is aspirated and replaced every 24 hours for a total treatment time of 72 hours. Following DAC treatment, media is aspirated and replaced with media supplemented with 2% FBS containing KDM5 inhibitors (e.g., CPI-455) at a final concentration of 9.375 μM. Cells are harvested following 72 hours of KDM5 inhibitor treatment[1]. |
| References |
[2]. Benjamin R. Leadem. NOVEL HISTONE DEMETHYLASE INHIBITORS SYNERGISTICALLY |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 488.7±55.0 °C at 760 mmHg |
| Molecular Formula | C16H14N4O |
| Molecular Weight | 278.309 |
| Flash Point | 249.3±31.5 °C |
| Exact Mass | 278.116760 |
| LogP | 2.46 |
| Appearance | white solid |
| Vapour Pressure | 0.0±1.2 mmHg at 25°C |
| Index of Refraction | 1.670 |
| Storage condition | -20℃ |