1. PROTAC Metabolic Enzyme/Protease
  2. PROTACs E1/E2/E3 Enzyme
  3. MS181

MS181 (compound 1) 是一种有效的 cereblon (CRBN) 募集和 EED 结合的泛素化复合体 1 (polycomb repressive complex 1 (PRC1)) PROTAC 降解剂。MS181 降低 EED、EZH2、SUZ12、BMI1 和 RING1B 的表达。MS181 显示出抗增殖活性 (Strtucture Note: Red, EED binder (HY-158771); Blue, CRBN ligand (HY-41547); Black, Linker HY-131717)。

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MS181 Chemical Structure

MS181 Chemical Structure

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规格 价格 是否有货 数量
1 mg ¥3200
In-stock
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10 mg 现货 询价
25 mg 现货 询价
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MS181 (compound 1) is a potent cereblon (CRBN)-recruiting and EED-binding polycomb repressive complex 1 (PRC1) PROTAC degrader. MS181 decreases the expression of EED, EZH2, SUZ12, BMI1 and RING1B. MS181 shows antiproliferative activity (Strtucture Note: Red, EED binder (HY-158771); Blue, CRBN ligand (HY-41547); Black, Linker HY-131717)[1].

体外研究
(In Vitro)

MS181 (compound 1) (0, 0.1, 0.3, 1, 3, 10 µM; 24 h) 以剂量依赖性方式降低 EED、EZH2、SUZ12、BMI1 和 RING1B 的表达[1]

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

Western Blot Analysis[1]

Cell Line: K562 cells
Concentration: 0, 0.1, 0.3, 1, 3, 10 µM
Incubation Time: 24 h
Result: Decreassed the expression of EED, EZH2, SUZ12, BMI1 and RING1B, H3K27me3 in a dose dependent manner, showed no changes in the histone H3 lysine 27 trimethylation (H3K27me3) mark catalyzed by the PRC2 complex.
体内研究
(In Vivo)

MS181 (50 mg/kg; i.p.; once) 在小鼠体内具有生物利用度[1]

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

Animal Model: Male swiss albino mice[1]
Dosage: 50 mg/kg
Administration: I.p.; once
Result: Showed above 1 μM for the first 2 h and maintained above 0.50 μM for 8 h post in the plasma concentration.
分子量

759.81

Formula

C39H41N11O6

性状

固体

颜色

Light yellow to 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 (131.61 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 1.3161 mL 6.5806 mL 13.1612 mL
5 mM 0.2632 mL 1.3161 mL 2.6322 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 1.3161 mL 6.5806 mL 13.1612 mL 32.9030 mL
5 mM 0.2632 mL 1.3161 mL 2.6322 mL 6.5806 mL
10 mM 0.1316 mL 0.6581 mL 1.3161 mL 3.2903 mL
15 mM 0.0877 mL 0.4387 mL 0.8774 mL 2.1935 mL
20 mM 0.0658 mL 0.3290 mL 0.6581 mL 1.6451 mL
25 mM 0.0526 mL 0.2632 mL 0.5264 mL 1.3161 mL
30 mM 0.0439 mL 0.2194 mL 0.4387 mL 1.0968 mL
40 mM 0.0329 mL 0.1645 mL 0.3290 mL 0.8226 mL
50 mM 0.0263 mL 0.1316 mL 0.2632 mL 0.6581 mL
60 mM 0.0219 mL 0.1097 mL 0.2194 mL 0.5484 mL
80 mM 0.0165 mL 0.0823 mL 0.1645 mL 0.4113 mL
100 mM 0.0132 mL 0.0658 mL 0.1316 mL 0.3290 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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Inquiry Information

产品名称:
MS181
目录号:
HY-158239
需求量: