2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. Polo-like Kinase (PLK) Epigenetic Reader Domain Apoptosis
  4. PLK1/BRD4-IN-1

PLK1/BRD4-IN-1 (9b) 是一个具有口服活性的 PLK1 和 BRD4 双重抑制剂，对 PLK1 和 BRD4 的 IC50 值分别为 22 nM 和 109 nM。PLK1/BRD4-IN-1 诱导细胞周期阻滞 (cell cycle arrest) 和凋亡 (apoptosis)，下调几种增殖相关癌基因的转录，并表现出良好的体内抗肿瘤活性。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

PLK1/BRD4-IN-1 Chemical Structure

PLK1/BRD4-IN-1 Chemical Structure

CAS No. : 2412707-81-2

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

PLK1/BRD4-IN-1 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-1 (9b) is an orally active dual PLK1 and BRD4 inhibitor with IC50 values of 22 nM and 109 nM against PLK1 and BRD4, respectively. PLK1/BRD4-IN-1 induces cell cycle arrest and apoptosis, downregulates the transcription of several proliferation-related oncogenes, and exhibits favorable in vivo antitumor activity[1].

IC50 & Target

BRD4

109 nM (IC50)

PLK1

22 nM (IC50)

体外研究
(In Vitro)

PLK1/BRD4-IN-1 (9b) (72 h) shows broad-spectrum antiproliferative activities[1].
PLK1/BRD4-IN-1 (0-9 µM, 24 h) induces cell cycle arrest[1].
PLK1/BRD4-IN-1 (0-9 µM, 48 h) induces cell apoptosis[1].
PLK1/BRD4-IN-1 inhibits the proliferative of cancer cells by exerting its inhibitory activity on both PLK1 and BRD4[1].

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

PLK1/BRD4-IN-1 相关抗体:

Cell Viability Assay[1]

Cell Line: MV4-11, LnCap, HT-29, A375, SKOV-3
Concentration: Cells were maintained in RPMI 1640 or DMEM medium supplemented with 10% FBS (v/v) in 5% CO2, except for MV4-11 cells, which were cultured in IMDM medium.
Incubation Time: 72 h
Result: Showed broad-spectrum antiproliferative activities with IC50 values of 0.13, 0.14, 1.10, 2.82 and 2.51 µM against MV4-11, LnCap, SKOV-3, A375 and HT29 cells, respectively.

Cell Cycle Analysis[1]

Cell Line: MV4-11
Concentration: 0.1, 0.3, 1, 3, 9 µM
Incubation Time: 24 h
Result: Induced obvious G2/M arrest in a concentration-dependent manner

Apoptosis Analysis[1]

Cell Line: MV4-11
Concentration: 0.1, 0.3, 1, 3, 9 µM
Incubation Time: 48 h
Result: Significantly increased the number of Annexin V/PI-positive MV4-11 cells in a concentration-dependent manner.

RT-PCR[1]

Cell Line: MV4-11
Concentration: 0.1, 0.3, 1, 3, 9 µM
Incubation Time: 24 h
Result: Reduced the transcription of c-MYC and MYCN as well as BCL-2, in a concentration-dependent manner.

Western Blot Analysis[1]

Cell Line: MV4-11
Concentration: 0.1, 0.3, 1, 3, 9 µM
Incubation Time: 48 h
Result: Decreased the expression of c-Myc and Bcl-2 in a concentration dependent-manner and upregulated cleaved caspase-3 and cleaved PARP.
体内研究
(In Vivo)

PLK1/BRD4-IN-1 (9b) (60 mg/kg/d; IG; 18 days) results in a significant decrease in average tumor size, with no obvious toxicity[1].

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

Animal Model: Five weeks old male NOD-SCID mice[1].
Dosage: 60 mg/kg/d
Administration: Oral gavage, 18 days; tumor xenograft models were established by subcutaneously injecting 100 µL of 1×108 cell/mL MV4-11 cell suspension into NOD-SCID mice.
Result: Resulted in a significant decrease in average tumor size, with 66% tumor growth inhibition, and didn’t obviously affect the body weight of mice.
分子量

573.73

Formula

C31H43N9O2
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

PLK1/BRD4-IN-1 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-12412707-81-2Polo-like Kinase (PLK)Epigenetic Reader DomainApoptosisMV4-11NOD-SCIDkinase inhibitorsInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
PLK1/BRD4-IN-1
目录号：
HY-143471
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z