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CPI-455 mediated KDM5 inhibition, elevated global levels of H3K4 trimethylation (H3K4me3) and decreased the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents. CPI-455 inhibits KDM5A, KDM5B and KDM5C to similar extents but showed substantially weaker potency toward KDM4C and KDM7B (~200- and 770-fold, respectively).
CPI-455 specifically alters H3K4 methylation in cells and binds at the demethylase active site. Pretreatment of cancer cells with a KDM5-specific inhibitor results in the ablation of a subpopulation of cancer cells that can serve as the founders for therapeutic relapse.
| Cell Experiment | |
|---|---|
| Cell lines | melanoma (M14), breast cancer (SKBR3) and NSCLC (PC9) cell lines |
| Preparation method | All cell lines were treated with DMSO, CPI-4203 or CPI-455 for 5 d with two changes of medium and drug. Thereafter, the cells (PC9, Colo205, Hs888, M14, SKBR3 and EVSA-T) were plated at 2×105 cells in six-well plates in triplicate and treated for an additional 9-15 d, depending on the cell line model. The Incucyte HD imaging system was used to monitor numbers of drug-tolerant cells after cells were stained with Nuclear-ID Red stain. |
| Concentrations | 0-25 μM |
| Incubation time | 14-20 days |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 278.31 |
| Formula | C16H14N4O |
| CAS Number | 1628208-23-0 |
| Solubility (25°C) | DMSO 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Histone demethylase Products |
|---|
| PFI-90
PFI-90 is a selective inhibitor of histone demethylase (KDM3B) that inhibits PAX3-FOXO1 action. |
| CPI-4203
CPI-4203 is a potent KDM5A inhibitor with an IC50 of 250 nM. |
| KDM2B-IN-4
KDM2B-IN-4 is a histone demethylase KDM2B inhibitor. |
| Zavondemstat
Zavondemstat (QC8222; TACH 101) is an inhibitor of histone lysine demethylase 4D (KDM4D) with antineoplastic activity. |
| Zavondemstat L-lysine
Zavondemstat (QC8222; TACH 101) (L-lysine) is an inhibitor of histone lysine demethylase 4D (KDM4D) with antineoplastic activity. |
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