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Antitumor agent-153 (compound 11b) is an inhibitor of H2A histone ubiquitination, optimized from PRT4165. It can reduce the viability of human osteosarcoma U2OS cells and decrease monoubiquitination of histone H2A, demonstrating anticancer activity.
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| Description | Antitumor agent-153 (compound 11b) is an inhibitor of H2A histone ubiquitination, optimized from PRT4165. It can reduce the viability of human osteosarcoma U2OS cells and decrease monoubiquitination of histone H2A, demonstrating anticancer activity. |
| In vitro | Antitumor agent-153 shows significant inhibitory activity against U2O cells with an IC50 of 5.86 μM and completely inhibits proliferation at 30 μM. A reduction in H2AK119ub1 levels interferes with tumor progression and cancer cell growth. Antitumor agent-153 (24-96 μM; 1 h) drastically reduces H2AK119ub1 levels in U2O cells in a dose-dependent manner. |
| Formula | C16H8N2O6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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