2. Cell Cycle/DNA Damage Cytoskeleton
  3. Kinesin
  4. EMD534085

EMD534085是有效选择性的有丝分裂驱动蛋白-5 (kinesin-5)的抑制剂，IC50值为8 nM。

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EMD534085 Chemical Structure

EMD534085 Chemical Structure

CAS No. : 858668-07-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4718
In-stock
1 mg ￥2045
In-stock
5 mg ￥4500
In-stock
10 mg 现货 询价
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

EMD534085 相关抗体

Top Publications Citing Use of Products

查看 Kinesin 亚型特异性产品:

查看所有亚型
Kinesin-5/Eg5/KSP Kinesin-6 Kinesin-7/CENP-E Kinesin-12 Kinesin-14

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

EMD534085 is a potent and selective inhibitor of the mitotic kinesin-5 with an IC50 of 8 nM.

IC50 & Target[1]

Kinesin-5

8 nM (IC50)

体外研究
(In Vitro)

EMD 534085 does not inhibit any other tested kinesins (BimC, CEN-PE, Chromokinesin, KHC, KIF3C, KIFC3, MKLP-1, and MCAK) at 1 μM or 10 μM concentration, showing selectively over kinesin-5. EMD 534085 binds to the allosteric pocket of kinesin-5[1]. EMD534085 induces rapid cell death in HL60 during mitotic arrest. Caspase-8, −9, −3, −7 are activated; Parp1 is cleaved; Mcl1 and XIAP are degraded in EMD534085-treated HL60 cells. EMD534085 treated HL60 cells also shows significantly accumulated phospho-Histone H3 level starting at 6 hrs post thymidine release[2].

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

EMD534085 相关抗体:
体内研究
(In Vivo)

In a low dose PK of EMD 534085 in mice the clearance is 1.8 L/h/kg on average, the volume of distribution is 7.4 L/kg and the half life around 2.5 h. The bioavailability in high dose experiments (>10 mg/kg) is always above 50% in mice. Intraperitonal administration of EMD 534085 enables significant systemic exposure in mice leading to a significant tumor growth reduction without toxic side effects[1].

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

476.53

Formula

C25H31F3N4O2
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 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : ≥ 26 mg/mL (54.56 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0985 mL 10.4925 mL 20.9850 mL
5 mM 0.4197 mL 2.0985 mL 4.1970 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 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

纯度: 99.55%

COA (196 KB) LCMS (266 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[2]

Epithelial cell lines HeLa and MCF7 are synchronized in G2-phase using RO-3306. Cells are treated with 10 µM RO-3306 for 16 hrs, and then are ished and released to either warm growth medium or medium supplemented with 500 nM EMD534085[2].

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

EMD534085 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0985 mL 10.4925 mL 20.9850 mL 52.4626 mL
5 mM 0.4197 mL 2.0985 mL 4.1970 mL 10.4925 mL
10 mM 0.2099 mL 1.0493 mL 2.0985 mL 5.2463 mL
15 mM 0.1399 mL 0.6995 mL 1.3990 mL 3.4975 mL
20 mM 0.1049 mL 0.5246 mL 1.0493 mL 2.6231 mL
25 mM 0.0839 mL 0.4197 mL 0.8394 mL 2.0985 mL
30 mM 0.0700 mL 0.3498 mL 0.6995 mL 1.7488 mL
40 mM 0.0525 mL 0.2623 mL 0.5246 mL 1.3116 mL
50 mM 0.0420 mL 0.2099 mL 0.4197 mL 1.0493 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:

EMD534085858668-07-2EMD 534085EMD-534085KinesinInhibitorinhibitorinhibit

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目录号：
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