2. Cell Cycle/DNA Damage Epigenetics Apoptosis Vitamin D Related/Nuclear Receptor
  3. Polo-like Kinase (PLK) Epigenetic Reader Domain Apoptosis Androgen Receptor c-Myc
  4. WNY0824

WNY0824  (Synonyms: PLK1/BRD4-IN-1)

目录号: HY-143471
产品使用指南

摩尔计算器

WNY0824 (PLK1/BRD4-IN-1) 是一个具有口服活性的 PLK1 和 BET 蛋白家族双重抑制剂，对 PLK1、BRD2、BRD3、BRD4 和 BRDT 的 IC50 值分别为 22、402.5、150.7、103.9 和 311.9 nmol/L。WNY0824 通过抑制 AR 和 MYC 介导的转录过程，来诱导细胞周期阻滞 (cell cycle arrest) 和凋亡 (apoptosis)。此外，WNY0824 还可抑制 Enzalutamide (HY-70002) 耐药 CRPC 异种移植瘤模型的肿瘤生长。

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WNY0824 Chemical Structure

WNY0824 Chemical Structure

CAS No. : 2412707-81-2

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WNY0824 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

WNY0824 (PLK1/BRD4-IN-1) is an orally active dual inhibitor of PLK1 and BET protein families, with IC50 values ​​of 22, 402.5, 150.7, 103.9, and 311.9 nmol/L for PLK1, BRD2, BRD3, BRD4, and BRDT, respectively. WNY0824 induces cell cycle arrest and apoptosis by inhibiting AR- and MYC-mediated transcriptional processes. In addition, WNY0824 also inhibits tumor growth in Enzalutamide (HY-70002) resistant CRPC xenograft tumor models[1][2].

IC50 & Target[2]

PLK1

22 nM (IC50)

BRD2

402.5 nM (IC50)

BRD3

150.7 nM (IC50)

BRD4

103.9 nM (IC50)

BRDT

311.9 nM (IC50)

体外研究
(In Vitro)

WNY0824 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)
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

WNY0824 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:

WNY08242412707-81-2PLK1/BRD4-IN-1WNY 0824WNY-0824Polo-like Kinase (PLK)Epigenetic Reader DomainApoptosisAndrogen Receptorc-MycMycMV4-11NOD-SCIDkinase inhibitorsInhibitorinhibitorinhibit

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