2. Epigenetics Apoptosis
  3. Histone Methyltransferase Epigenetic Reader Domain Apoptosis
  4. YM458

YM458 是一种有效的 EZH2 和 BRD4 双重抑制剂，对 EZH2 和 BRD4 的 IC50 分别为490 nM 和 34 nM。YM458 可抑制实体癌细胞增殖和集落形成，诱导细胞周期阻滞与细胞凋亡 (apoptosis)。YM458 可用于抗癌研究。

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YM458 Chemical Structure

YM458 Chemical Structure

CAS No. : 2770108-93-3

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YM458 相关抗体

Top Publications Citing Use of Products

查看 Histone Methyltransferase 亚型特异性产品:

查看所有亚型
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

YM458 is a potent EZH2 and BRD4 dual inhibitor with IC50s of 490 nM and 34 nM, respectively. YM458 inhibits cell proliferation and colony formation and induces cell cycle arrest and apoptosis in solid cancer cells. YM458 can be used for researching anticancer[1].

IC50 & Target[1]

EZH2

 

EZH2

490 nM (IC50)

BRD4

34 nM (IC50)

体外研究
(In Vitro)

YM458 (compound D7) (0-30 μM; 6 days) has antiproliferative activities against AsPC-1 cells with an IC50 of 0.69 ± 0.16 μM; and (1 μM; 72 hours) significantly decreases the degree of H3K27me3 and c-Myc in AsPC-1[1].
YM458 (0-30 μM; 4 or 6 days) inhibits cell proliferation on a broad range of solid cancer cells, and significantly suppresses proliferation of A549 lung cancer cells and HCT116 colorectal cancer cells at 1 μM[1].
YM458 (0.05-0.4 μM; 12-20 days) inhibits colony formation of AsPC-1, HCT116, and A549 cancer cells in a dose-dependent manner[1].

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

YM458 相关抗体:

Western Blot Analysis

Cell Line: AsPC-1[1]
Concentration: 1 μM
Incubation Time: 72 hours
Result: Decreased the degree of H3K27me3 and c-Myc significantly.

Cell Proliferation Assay

Cell Line: AsPC-1, SW1990, CFPAC-1, A549, HCC827, H1650, H292, H460, DLD1, HCT116, and RKO[1]
Concentration: 0-30 μM
Incubation Time: 4 or 6 days
Result: Inhibited cell proliferation on a broad range of solid cancer cells, and significantly suppressed proliferation of A549 lung cancer cells and HCT116 colorectal cancer cells at 1 μM.
体内研究
(In Vivo)

YM458 (60 mg/kg; IP; every other day, for 38 days) prevents tumor growth with inhibitory rates of 38.6% in AsPC-1 cells and 62.3% in A549 cells[1].
Pharmacokinetic Parameters of YM458 in Female BALB/c mice[1].

IP (80 mg/kg) PO (80 mg/kg)
t1/2 (h) 3.81 4.16
Tmax (h) 1 1
Cmax (ng/mL) 27126.3 4383.6
AUC0-24 (ng/mL·h) 273220.1 13509.1
CL (mL/min/kg) 4.88
F (%) 4.94

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

Animal Model: BALB/c nude mice (injected with A549 or AsPC-1)[1]
Dosage: 60 mg/kg
Administration: IP; every other day, for 38 days
Result: Prevented tumor growth with inhibitory rates of 38.6% in AsPC-1 cells and 62.3% in A549 cells.
分子量

957.62

Formula

C53H61ClN8O5S
CAS 号
性状

固体

颜色

White to off-white

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 : 125 mg/mL (130.53 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 1.0443 mL 5.2213 mL 10.4426 mL
5 mM 0.2089 mL 1.0443 mL 2.0885 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

只
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

YM458 相关分类

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 1.0443 mL 5.2213 mL 10.4426 mL 26.1064 mL
5 mM 0.2089 mL 1.0443 mL 2.0885 mL 5.2213 mL
10 mM 0.1044 mL 0.5221 mL 1.0443 mL 2.6106 mL
15 mM 0.0696 mL 0.3481 mL 0.6962 mL 1.7404 mL
20 mM 0.0522 mL 0.2611 mL 0.5221 mL 1.3053 mL
25 mM 0.0418 mL 0.2089 mL 0.4177 mL 1.0443 mL
30 mM 0.0348 mL 0.1740 mL 0.3481 mL 0.8702 mL
40 mM 0.0261 mL 0.1305 mL 0.2611 mL 0.6527 mL
50 mM 0.0209 mL 0.1044 mL 0.2089 mL 0.5221 mL
60 mM 0.0174 mL 0.0870 mL 0.1740 mL 0.4351 mL
80 mM 0.0131 mL 0.0653 mL 0.1305 mL 0.3263 mL
100 mM 0.0104 mL 0.0522 mL 0.1044 mL 0.2611 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.

Keywords:

YM4582770108-93-3YM 458YM-458Histone MethyltransferaseEpigenetic Reader DomainApoptosisAnticancerCell proliferationColony formationCell cycle arrestSolid cancer cellsA549Inhibitorinhibitorinhibit

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