Methylstat
目录号 : GC67966Methylstat 是一种有效的组蛋白去甲基化酶 (histone demethylases) 抑制剂。Methylstat 具有抗增殖活性，低细胞毒性。Methylstat 诱导细胞凋亡 (Apoptosis) 和细胞周期停滞在 G0/G1 期。Methylstat 增加 p53 和 p21 蛋白水平的表达。Methylstat 抑制由各种细胞因子诱导的血管生成。Methylstat 可用作化学探针以解决其在血管生成中的作用。
Cas No.:1310877-95-2
Sample solution is provided at 25 µL, 10mM.
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Methylstat is a potent histone demethylases inhibitor. Methylstat shows anti-proliferative activity with low cytotoxicity. Methylstat induces Apoptosis and cell cycle arrest at G0/G1 phase. Methylstat increases the expression of p53 and p21 protein levels. Methylstat inhibits angiogenesis induced by various cytokines. Methylstat can be used as a chemical probe for addressing its role in angiogenesis[1][2].
Methylstat (0-5 µM; 48, 72 h) shows anti-proliferative activity with no cytotoxicity on HUVECs at 1-2 µM[1].
Methylstat (0, 1, 2 µM; 48 h) induces cell cycle arrest at G0/G1 phase in a dose-dependent manner[1].
Methylstat (0, 1, 2 µM; 48 h) increases the expression of p53 mRNA levels, the H3K27 methylation levels and the accumulation of p53 and p21 protein levels, but suppresses the protein level of cyclinD1[1].
Methylstat (0, 1, 2 µM) shows anti-angiogenic activity induced by VEGF, bFGF and TNF-α in HUVEC cells, and inhibits the f capillary formation during CAM (chick embryo chorioallantoic membrane) development without any sign of thrombosis and hemorrhage[1].
Methylstat (1.1, 2.2 mM for U266 cells, 2.1, 4.2 mM for ARH77 cells; 72 h) induces apoptosis significantly in U266 and ARH77 cells[2].
Cell Cytotoxicity Assay[1]
| Cell Line: | HUVEC cells |
| Concentration: | 0-5 µM |
| Incubation Time: | 48, 72 h |
| Result: | Did not exhibit cytotoxicity on HUVECs at 1-2 µM. |
Cell Viability Assay[1]
| Cell Line: | HUVEC, HepG2, HeLa, CHANG cells |
| Concentration: | 0-5 µM |
| Incubation Time: | 72 h |
| Result: | Showed anti-proliferative activity with IC50s of 4, 10, 5, 7.5 µM for HUVEC, HepG2, HeLa, CHANG cells, respectively. |
Cell Cycle Analysis[1]
| Cell Line: | HUVEC cells |
| Concentration: | 0, 1, 2 µM |
| Incubation Time: | 48 h |
| Result: | G0/G1 phase increased 16.8% compared to non-treated cells, whereas S andG2/M decreased 5.5% and 6.1% respectively. |
Western Blot Analysis[1]
| Cell Line: | HUVEC cells |
| Concentration: | 0, 1, 2 µM |
| Incubation Time: | 0-48 h |
| Result: | Resulted in accumulation of p53 and p21 protein levels in a time- and dose-dependent manner and increased the H3K27 methylation levels, the but suppressed the protein level of cyclinD1. |
Apoptosis Analysis[2]
| Cell Line: | U266, ARH77 cells |
| Concentration: | 1.1, 2.2 mM for U266 cells, 2.1, 4.2 mM for ARH77 cells |
| Incubation Time: | 72 h |
| Result: | Induced apoptosis in U266, ARH77 cells. |
[1]. Yumi Cho, et al. A histone demethylase inhibitor, methylstat, inhibits angiogenesis in vitro and in vivo. RSC Advances, 2014.
[2]. Kac? FN, et al. Synergistic Apoptotic Effects of Bortezomib and Methylstat on Multiple Myeloma Cells. Arch Med Res. 2020 Apr;51(3):187-193.
| Cas No. | 1310877-95-2 | SDF | Download SDF |
| 分子式 | C28H31N3O6 | 分子量 | 505.56 |
| 溶解度 | DMSO : 100 mg/mL (197.80 mM; Need ultrasonic) | 储存条件 | 4°C, protect from light |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.978 mL | 9.89 mL | 19.78 mL |
| 5 mM | 0.3956 mL | 1.978 mL | 3.956 mL |
| 10 mM | 0.1978 mL | 0.989 mL | 1.978 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet