| Name | CPI-360 |
| Description | CPI-360 is a small molecule EZH2 inhibitor (IC50: 0.002 μM, EC50: 0.080 μM) that shows antitumor activity in an EZH200-dependent tumor xenograft model. |
| In vitro | In KARPAS-422 cells, CPI-360 potently reduces global H3K27me3 and H3K27me2 levels with EC50 of 56 nM and 65 nM, respectively. CPI-360 also causes time-dependent transcriptional changes, and affects the viability of Y641N mutant EZH2-containing KARPAS-422 cells. In addition, CPI-360 gradually arrests KARPAS-422 cells in the G1 cell cycle stage followed by the induction of apoptosis. [1] |
| In vivo | In mice bearing KARPAS-422 xenografts, CPI-360 (200 mg/kg, s.c.) reduces tumor growth by 44%. [1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 22.5 mg/mL (51.43 mM), Sonication is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble) DMF : 9 mg/mL (20.57 mM), Sonication is recommended. Ethanol : 27 mg/mL (61.71 mM), Sonication is recommended.
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| Keywords | HistoneMethyltransferase | Histone Methyltransferase | EZH2 | CPI-360 | Apoptosis |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Formamide | Dimethyl phthalate | Alginic acid | Sodium Molybdate | Sildenafil citrate |
| Related Compound Libraries | Apoptosis Compound Library | Histone Modification Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Epigenetics Compound Library | Hematonosis Compound Library | Inhibitor Library | Anti-Prostate Cancer Compound Library | Bioactive Compounds Library Max | Preclinical Compound Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |