1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. HDAC Apoptosis
  3. MC2590

MC2590 是一种有效的含吡啶的组蛋白脱乙酰酶 (HDAC) 抑制剂。MC2590 是 HDAC1-3、-6、-8 和 -10 的抑制剂 (I/IIb 类选择性抑制剂),IC50 为 0.015 μM-0.156 μM。MC2590 还抑制其他 HDAC 亚型, HDAC4、HDAC5、HDAC7 、HDAC9、HDAC11,IC50 为 1.35 μM-3.98 μM。MC2625 诱导 G2/M 细胞周期停滞并调节促凋亡和抗凋亡 microRNA 以诱导细胞凋亡。

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MC2590 Chemical Structure

MC2590 Chemical Structure

CAS No. : 2284460-01-9

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1 mg ¥8316
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MC2590 is a potent pyridine-containing histone deacetylase (HDAC) inhibitor. MC2590 is a inhibitor of HDAC1-3, -6, -8, and -10 (class I/IIb-selective inhibitor) with IC50s of 0.015 μM-0.156 μM. MC2590 also inhibits HDAC isoforms HDAC4, HDAC5, HDAC7, HDAC9, HDAC11 with IC50s of 1.35 μM-3.98 μM. MC2625 induces G2/M cell cycle arrest and modulates pro- and anti-apoptotic microRNAs towards apoptosis induction[1].

IC50 & Target[1]

HDAC1

0.098 μM (IC50)

HDAC2

0.156 μM (IC50)

HDAC3

0.039 μM (IC50)

HDAC6

0.015 μM (IC50)

HDAC8

0.047 μM (IC50)

HDAC10

0.071 μM (IC50)

HDAC4

2.73 μM (IC50)

HDAC5

1.35 μM (IC50)

HDAC7

2.06 μM (IC50)

HDAC9

2.79 μM (IC50)

HDAC11

3.98 μM (IC50)

体外研究
(In Vitro)

MC2625 (化合物5e; 72 小时) 抑制结直肠癌细胞 HCT116 (IC50=0.07 μM)、肺腺癌细胞 A549 (IC50=0.32 μM)、慢性粒细胞白血病 K562 (IC50=0.05 μM)[1]
MC2625 (1, 5 μM; 24, 48 小时) 诱导 G2/M 细胞周期停滞[1]
MC2625 (1, 5 μM; 24, 48 小时) 诱导 H3K9/14 过度乙酰化活性,增加乙酰-α-微管蛋白水平,显着上调 p21 蛋白[1]
MC2625 (1, 5 μM; 48 小时) 增加 p21、BAX 和 BAKmRNA 表达,下调细胞周期蛋白 D1 和 BCL-2,并调节促凋亡和抗凋亡 microRNA 以诱导细胞凋亡[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: Human acute myeloid leukaemia U937 cells
Concentration: 1, 5 μM
Incubation Time: 24, 48 h
Result: At 24 h, showed very low increase of the pre-G1 peak and led to a G2/M phase arrest at 1 μM; induced a 10% pre-G1 increase and displayed a block at the G2/M phase at 5 μM.
At 48 h, induced a 70-85% block of the cell cycle at the G1 phase.

Western Blot Analysis[1]

Cell Line: Human acute myeloid leukaemia U937 cells
Concentration: 1, 5 μM
Incubation Time: 24, 48 h
Result: At 1 μM revealed H3K9/14 hyperacetylation activity, increased the acetyl-α-tubulin level, markedly upregulated the p21 protein.

RT-PCR[1]

Cell Line: Human acute myeloid leukaemia U937 cells
Concentration: 1, 5 μM
Incubation Time: 48 h
Result: At 1 μM significantly induced the expression of BAX and BAK, dose-dependently downregulated the antiapoptotic factor BCL-2.
Downregulated miRNAs with antiapoptotic activity (miR-17-5p, miR-18-5p, miR-19b-3p, miR-20a-5p, miR-21-5p); induced the proapoptotic miRNAs (miR-let7a-5p, miR-125b-5p, miR-181a-5p, miR-181b-5p, miR-769-5p, miR-122-5p).
分子量

347.37

Formula

C20H17N3O3

CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (287.88 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8788 mL 14.3939 mL 28.7877 mL
5 mM 0.5758 mL 2.8788 mL 5.7575 mL
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8788 mL 14.3939 mL 28.7877 mL 71.9694 mL
5 mM 0.5758 mL 2.8788 mL 5.7575 mL 14.3939 mL
10 mM 0.2879 mL 1.4394 mL 2.8788 mL 7.1969 mL
15 mM 0.1919 mL 0.9596 mL 1.9192 mL 4.7980 mL
20 mM 0.1439 mL 0.7197 mL 1.4394 mL 3.5985 mL
25 mM 0.1152 mL 0.5758 mL 1.1515 mL 2.8788 mL
30 mM 0.0960 mL 0.4798 mL 0.9596 mL 2.3990 mL
40 mM 0.0720 mL 0.3598 mL 0.7197 mL 1.7992 mL
50 mM 0.0576 mL 0.2879 mL 0.5758 mL 1.4394 mL
60 mM 0.0480 mL 0.2399 mL 0.4798 mL 1.1995 mL
80 mM 0.0360 mL 0.1799 mL 0.3598 mL 0.8996 mL
100 mM 0.0288 mL 0.1439 mL 0.2879 mL 0.7197 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
MC2590
目录号:
HY-152226
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