KDM5-C70 是一种 KDM5-C49 的乙酯衍生物,是一种有效的,细胞可渗透的泛KDM5组蛋白脱甲基酶抑制剂。KDM5-C70 在骨髓瘤细胞中具有抗增殖作用,从而导致 H3K4me3 水平在全基因组范围内升高。
生物活性 | KDM5-C70 is an ethyl ester derivative of KDM5-C49 and a potent, cell-permeable and pan-KDM5histone demethylaseinhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels[1][2]. |
IC50& Target | KDM5 histone demethylase[1][2] |
体外研究 (In Vitro) | KDM5-C70 (10-9-10-5M; 7 days; MM.1S myeloma cells) treatment shows antiproliferative effects after 7 days of treatment at elevated concentrations (estimated 50% reduction of viability/proliferation for KDM5-C70 at ~20 μM)[1]. KDM5-C70 (50 μM; 7 days; MM.1S myeloma cells) treatment decreases the level of phosphorylation of retinoblastoma protein (Rb), while leaving the total level of phosphorylated Rb (pRb) unchanged, indicating impairment of cell cycle progression[1]. Chromatin immunoprecipitation followed by next-generation sequencing shows an increase in H3K4me3 levels around transcription start sites with KDM5-C70 but little change with GSK467A at 50 μM inhibitor concentrations[1].
Cell Viability Assay[1] Cell Line: | MM.1S myeloma cells | Concentration: | 10-9-10-5M | Incubation Time: | 7 days | Result: | Showed antiproliferative effects after 7 days of treatment at elevated concentrations. |
Western Blot Analysis[1] Cell Line: | MM.1S myeloma cells | Concentration: | 50 μM | Incubation Time: | 7 days | Result: | Decreased the level of phosphorylation of retinoblastoma protein (Rb). |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | -20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
溶解性数据 | In Vitro: DMSO : 100 mg/mL(297.24 mM;Need ultrasonic) 配制储备液 1 mM | 2.9724 mL | 14.8619 mL | 29.7239 mL | 5 mM | 0.5945 mL | 2.9724 mL | 5.9448 mL | 10 mM | 0.2972 mL | 1.4862 mL | 2.9724 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 (stored under nitrogen)。-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 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (7.43 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.43 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (7.43 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.43 mM,饱和度未知) 的澄清溶液。 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 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (7.43 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.43 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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