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Methylstat
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Methylstat图片
CAS NO:1310877-95-2
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
Methylstat 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。
生物活性

Methylstat is a potenthistone demethylasesinhibitor. Methylstat shows anti-proliferative activity with low cytotoxicity. Methylstat inducesapoptosisand cell cycle arrest at G0/G1 phase. Methylstat increases the expression ofp53and 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].

体外研究
(In Vitro)

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 and G2/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.
分子量

505.56

性状

Solid

Formula

C28H31N3O6

CAS 号

1310877-95-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 100 mg/mL(197.80 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.9780 mL9.8900 mL19.7800 mL
5 mM0.3956 mL1.9780 mL3.9560 mL
10 mM0.1978 mL0.9890 mL1.9780 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 (protect from light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。