Methylstat

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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。

CAS NO:

1310877-95-2

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 mg

5 mg

10 mg

1 mM	1.9780 mL	9.8900 mL	19.7800 mL
5 mM	0.3956 mL	1.9780 mL	3.9560 mL
10 mM	0.1978 mL	0.9890 mL	1.9780 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。