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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Top Publications Citing Use of Products
  • 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 BAK 的 mRNA 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
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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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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MC2590
目录号:
HY-152226
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