DCH36_06是一种高效选择性的 p300/CBP 抑制剂,IC50 值分别为 0.6 μM (p300) 和 3.2 μM (CBP)。该抑制作用导致白血病细胞中H3K18的低乙酰化,具有抗肿瘤活性。
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描述 | DCH36_06, a potent and selective p300/CBP inhibitor, exhibits IC50s of 0.6 μM for p300 and 3.2 μM for CBP. It induces hypoacetylation of H3K18 in leukemic cells and demonstrates anti-tumor activity [1]. |
体内研究 | DCH36_06 (25-50 mg/kg; intraperitoneal injection; every two days; for 20 days) effectively halts leukemic xenograft growth in mice [1]. |
体外研究 | DCH36_06 treatment (6.7-20 μM; 24-48 hours) arrests the cell cycle in the G1 phase and induces apoptosis dose-dependently in leukemic cells [1]. DCH36_06 (5-10 μM, 24h) significantly activates the cleavage of pro-caspase 3, pro-caspase 9, and PARP1 in a dose-dependent manner [1]. DCH36_06 demonstrates strong antiproliferative effects on various leukemia cell lines (CEM, MOLT3, MOLT4, Jurkat, MV4-11, THP-1, RS4; 11, KOPN8, Kasumi-1, and K562 cells), exhibiting dose-dependent activity with IC50 values in the single-digit micromolar range [1]. |
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存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.68mL 0.54mL 0.27mL |
13.41mL 2.68mL 1.34mL |
26.82mL 5.36mL 2.68mL |
CAS号 | 593273-05-3 |
分子式 | C18H13ClN2O3S |
分子量 | 372.825 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Sealed in dry,2-8°C |
溶解度 |
DMSO: 120 mg/mL(321.87 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |