KDM5-C70
目录号 : KM6975 CAS No. : 1596348-32-1 纯度 : ≥98%

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。

规格 价格 是否有货 数量
25mg
In-stock
100mg
In-stock
250mg
In-stock
500mg 询价 In-stock
1g 询价 In-stock

Other Forms of Rapamycin:

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生物活性

KDM5-C70 is an ethyl ester derivative of KDM5-C49 and a potent, cell-permeable and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels.

体外研究

KDM5-C70 (10-10 M; 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).
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.
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.

Cell Viability Assay

Cell Line: MM.1S myeloma cells
Concentration: 10-10 M
Incubation Time: 7 days
Result: Showed antiproliferative effects after 7 days of treatment at elevated concentrations.

Western Blot Analysis

Cell Line: MM.1S myeloma cells
Concentration: 50 μM
Incubation Time: 7 days
Result: Decreased the level of phosphorylation of retinoblastoma protein (Rb).
分子式
C17H28N4O3
分子量
336.43
CAS号
1596348-32-1
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (743.10 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 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: ≥ 6.25 mg/mL (18.58 mM); Clear solution

    此方案可获得 ≥ 6.25 mg/mL (18.58 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 62.5 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-CD in saline)

    Solubility: ≥ 6.25 mg/mL (18.58 mM); Clear solution

    此方案可获得 ≥ 6.25 mg/mL (18.58 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 62.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 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: ≥ 6.25 mg/mL (18.58 mM); Clear solution

    此方案可获得 ≥ 6.25 mg/mL (18.58 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 62.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

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