2. Apoptosis Cell Cycle/DNA Damage Epigenetics
  3. Apoptosis Polo-like Kinase (PLK) Epigenetic Reader Domain
  4. PLK1/BRD4-IN-5

PLK1/BRD4-IN-5 (Compound SC10) 是一种具有口服活性的的 PLK1 和 BRD4 抑制剂，对 PLK1 和 BRD4 的 IC50 值分别为 0.3  nM 和 60.8  nM。PLK1/BRD4-IN-5 可诱导 MV4-11 细胞阻滞 (cell cycle arrest) 于 S 期并呈剂量依赖性地诱导凋亡 (apoptosis)。PLK1/BRD4-IN-5 可用于癌症研究。

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PLK1/BRD4-IN-5 Chemical Structure

PLK1/BRD4-IN-5 Chemical Structure

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3.  试用装只面向终端客户。

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PLK1/BRD4-IN-5 相关抗体

Top Publications Citing Use of Products

查看 Polo-like Kinase (PLK) 亚型特异性产品:

查看所有亚型
PLK1 PLK2 PLK3 PLK4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PLK1/BRD4-IN-5 (Compound SC10) is an orally active PLK1 and BRD4 inhibitor with IC50 values of 0.3  nM and 60.8  nM, respectively. PLK1/BRD4-IN-5 can induce MV4-11 cell block in S phase and apoptosis) in a dose-dependent manner. PLK1/BRD4-IN-5 can be used in cancer research[1].

IC50 & Target

PLK1

0.3 nM (IC50)

BRD4

60.8 nM (IC50)

体外研究
(In Vitro)

PLK1/BRD4-IN-5 (Compound SC10) 对三种肿瘤细胞系都具有显著的抗增殖活性 (MDA-MB-231 IC50 = 17.3  nM, MDA-MB-361 IC50 = 8.4  nM, MV4-11 IC50 = 5.4  nM)[1]。

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

PLK1/BRD4-IN-5 相关抗体:

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.675 nM, 1.35 nM, 2.7 nM, 5.4 nM and 10.8 nM
Incubation Time: 72 h
Result: Exhibited an increasing rate of apoptosis ranging from 6.65 to 58.35 % in a concentration-dependent manner.
体内研究
(In Vivo)


PLK1/BRD4-IN-5 在 Sprague-Dawley 大鼠体内的药动学参数[1]

Route Dose (mg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (ng•h/mL) Cl (mL•min/kg) MRT0-t (h) Vdss (L/kg) F (%)
i.g. 10 3.75 2.00 108 657 / 5.26 / 21.4
i.v. 1 4.9 / / 303 53.6 4.39 16.4 /

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

576.73

Formula

C31H44N8O3
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

PLK1/BRD4-IN-5 相关分类

  • 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)

质量   浓度   体积   分子量 *
= × ×

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)
× = ×
C1   V1   C2   V2
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:

PLK1/BRD4-IN-5ApoptosisPolo-like Kinase (PLK)Epigenetic Reader DomainDihydropteridone derivativesIsoindolin-1-one or isoindoline moietiesMV4-11 cellsInhibitorinhibitorinhibit

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目录号：
HY-158031
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