2. Epigenetics
  3. Epigenetic Reader Domain
  4. WWL0245

WWL0245 是一种有效的选择性 BRD4 PROTAC。WWL0245 选择性降解 BRD4 的 DC50 <1 nM, 降解 BRD2/3 和 PLK1 的 DC50 >1 μM)。WWL0245 在 BETi 敏感的癌细胞系，包括 AR 阳性前列腺癌细胞系中表现出优异的选择性细胞毒性。WWL0245 是 AR 阳性前列腺癌研究中有前景的候选药物，也是研究 BRD4 生物学功能的有价值的工具化合物。

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WWL0245 Chemical Structure

WWL0245 Chemical Structure

CAS No. : 2869057-11-2

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WWL0245 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

WWL0245 is a potent and seletive BRD4 PROTAC. WWL0245 selectively degrades BRD4 with sub-nanomolar DC50 (<1 nM) than BRD2/3 and PLK1 ( DC50>1 μM). WWL0245 shows excellent selective cytotoxicity in the BETi sensitive cancer cell lines, including AR-positive prostate cancer cell lines. WWL0245 is a promising drug candidate for AR-positive prostate cancer research and a valuable tool compound to study the biological function of BRD4[1].

IC50 & Target[1]

BRD4

1 nM (IC50)

体外研究
(In Vitro)

WWL0245 (0-1 μM; 96h) 抑制 AR 阳性前列腺癌细胞的增殖，IC50值范围为 0.0159 μM ~ 10 μM。在 [1]时，对 AR 阳性细胞株 VCaP、LNCaP、22Rv1 表现出较强的抗增殖活性, IC50 值分别为 0.016 μM、0.021 μM、0.053 μM。
WWL0245 (1 μM; 24 h) 导致 LNCaP、22Rv1、VCaP 细胞系 BRD4 和 c-Myc 呈时间依赖性下调，导致 22Rv1 和 VCaP 细胞 BRD4 水平和 c-Myc 水平呈浓度依赖性降低。WWL0245 也可以下调 DU145 细胞中的 BRD4 水平，但对 c-Myc 水平的影响可以忽略不计[1]。
WWL0245 (100 nM-1 μM; 24小时) 不同程度地抑制 AR 调控基因 (PSA、TMPRSS2、ERG、FKBP5、BMPR1B) 的转录[1]。

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

WWL0245 相关抗体:

Cell Proliferation Assay[1]

Cell Line: HL60, SU-DHL-6, RS4;11, JURKAT, A2780, MDA-MB-468, BT549, LNCaP, 22Rv1, and VCaP cells
Concentration: 0 μM -10 μM
Incubation Time: 96 h
Result: Inhibited HL60, SU-DHL-6, RS4;11, JURKAT, A2780, MDA-MB-468, BT549, LNCaP, 22Rv1, and VCaP growth with IC50 values of 0.0961, 0.0734, 0.0247, 0.5018, 0.0153, 0.2460, and 0.1732 μM, respcetively[1].

Western Blot Analysis[1]

Cell Line: Prostate cancer cell lines: LNCaP, 22Rv1, VCaP, DU145
Concentration: 1 nM, 10 nM, 100 nM, 1000 nM, 10000 nM
Incubation Time: 1 hour, 2 hours, 4 hours,12 hours, 24 hours,48 hours
Result: Resulted in the downregulation of BRD4 and c-Myc in a time/concentration-dependent manner in 22Rv1 and VCaP cells.

RT-PCR[1]

Cell Line: Prostate cancer: VCaP cell
Concentration: 100 nM-1 μM
Incubation Time: 24 h
Result: Suppressed the expression of AR-regulated genes in prostate cancer.
分子量

873.96

Formula

C45H51N11O8
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

WWL0245 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:

WWL02452869057-11-2WWL 0245WWL-0245Epigenetic Reader DomainBRD4PROTACAR-positiveprostate cancerInhibitorinhibitorinhibit

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