BML-210 是一种有效的HDAC抑制剂。BML-210 可以抑制 HDAC4-VP16 驱动的报告信号，IC50为 ~5 μM。BML-210 对 HDAC4:MEF2 交互具有特定的破坏性影响。BML-210 导致 G0/G1 期增加。BML-210 诱导细胞凋亡，并在小鼠原位乳腺肿瘤中显示出抗肿瘤活性。
| 生物活性 | BML-210 is a potentHDACinhibitor. BML-210 can inhibit the HDAC4-VP16-driven reporter signal with an apparent IC50of ~5 μM. BML-210 has a specific disruptive effect on the HDAC4:MEF2 interaction. BML-210 causes an increase in the G0/G1 phase. BML-210 inducesapoptosisand displays antitumour activities in orthotopic mammary tumours in mice[1][2][3]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | BML-210 (10, 20 μM; 24, 48小时) 抑制 NB4 细胞的增殖和生长[2]。
BML-210 (10, 20 μM; 24, 48小时) 导致 NB4 细胞在 S 期的比例降低，G0/G1 期的比例增加[2]。
BML-210 (10, 20 μM; 24, 48小时) 在 20μM 时对NB4细胞产生细胞毒性作用。BML-210 以 10μM 剂量可以诱导凋亡细胞死亡[2]。
BML-210 (10, 20 μM; 24, 48小时) 抑制 NB4 细胞中 HDAC 的表达和活性[2]。
BML-210 不降低 HDAC4-VP16 的表达[1]。
Cell Proliferation Assay[2] | Cell Line: | NB4 cells | | Concentration: | 10, 20 μM | | Incubation Time: | 24, 48 hours | | Result: | Inhibited cell proliferation and growth inhibition of NB4 cells in a dose- and time-dependent manner. |
Cell Cycle Analysis[2] | Cell Line: | NB4 cells | | Concentration: | 10, 20 μM | | Incubation Time: | 24, 48 hours | | Result: | Caused a decrease in the proportion of NB4 cells in the S phase and an increase in the G0/G1 phase.
Caused an increase in the G0/G1 phase up to 70% at 24 and 48 h with 10 μM. |
Cell Cytotoxicity Assay[2] | Cell Line: | NB4 cells | | Concentration: | 10, 20 μM | | Incubation Time: | 24, 48 hours | | Result: | Caused cytotoxic effects on NB4 cells in a dose- and time-dependent manner. |
Apoptosis Analysis[2] | Cell Line: | NB4 cells | | Concentration: | 10, 20 μM | | Incubation Time: | 24, 48 hours | | Result: | At a dose of 10 μM induced apoptotic cell death. |
Western Blot Analysis[2] | Cell Line: | NB4 cells | | Concentration: | 10, 20 μM | | Incubation Time: | 24, 48 hours | | Result: | At 10 μM dose inhibited HDAC1 gene expression up to 36% after 48 h of treatment
Inhibited HDAC expression up to 74% at 8 h point at 20 μM.
Had very low effect on HDAC 2 and HDAC 3 expression. |
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体内研究
(In Vivo) | BML-210 (20 mg/kg; 腹腔给药; 每周 3 次，持续两周) 显着抑制肿瘤生长和重量。BML-210 对免疫缺陷裸鼠 (Nu/J) 的肿瘤生长和体重没有影响[3]。
| Animal Model: | Female C57BL/6 mice with mouse breast cancer EO771 cells[3] | | Dosage: | 20 mg/kg | | Administration: | IP; three times per week for two weeks | | Result: | Notably suppressed the tumour growth and weight. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 30 mg/mL(88.38 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.9461 mL | 14.7306 mL | 29.4612 mL | | 5 mM | 0.5892 mL | 2.9461 mL | 5.8922 mL | | 10 mM | 0.2946 mL | 1.4731 mL | 2.9461 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (7.37 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.37 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
*以上所有助溶剂都可在本网站选购。 |
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