2. Epigenetics Apoptosis
  3. Epigenetic Reader Domain Necroptosis
  4. DW34

DW34 是一种有口服活性的泛 BRD4-D1 偏向性抑制剂，同时具有额外的 BRD4-D2 活性。DW34 展现出与 I-BET151 (HY-13235) (EC50 值为 0.16 μM) 相当的低纳摩尔抑制效应，其 EC50 值为 0.14 μM。DW34 通过降低趋化因子表达和细胞坏死，显著减轻脂多糖 (LPS) (HY-D1056) 诱导的肝脏炎症以及对乙酰氨基酚 (APAP) (HY-66005) 诱导的毒性。

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DW34 Chemical Structure

DW34 Chemical Structure

CAS No. : 2758171-54-7

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DW34 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

DW34 is an orally active pan-BRD4-D1 biased inhibitor with additional BRD4-D2 inhibitive activity. DW34 displays comparable inhibitive efficacy to I-BET151 (HY-13235) (EC50 = 0.16 μM) with low nanomolar EC50 values of 0.14 μM. DW34 significantly reduces liver inflammation induced by LPS (HY-D1056) and APAP (HY-66005) via reducing chemokine expression and cellular necrosis[1].

体外研究
(In Vitro)

DW34 (Compound 3) (0.31-5 μM, 5 h) 可抑制 LPS (HY-D1056) (200 ng/mL, 4 h) 诱导的转化型肝窦内皮细胞 (TSECs) 中 CXCL1 和 CCL2 的表达[1]。

DW34 (0.5-5 μM, 2 h) 在 HEK293T 细胞中，稳定 BRD4 的作用与 I-BET151 (HY-13235) 相当[1]。

DW34 (0.1-200 μM, 4 h) 在转化型肝窦内皮细胞 (TSECs) 中显示出良好的耐受性[1]。

DW34 在巨核细胞中诱导出毒性反应，EC50 值为 90 nM[1]。

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

DW34 相关抗体:

Real Time qPCR[1]

Cell Line: Transformed sinusoidal endothelial cells
Concentration: 0.31, 1.25 and 5μM
Incubation Time: 1 h, following by 200 ng/mL LPS (HY-D1056) for 4 h
Result: Decreased CXCL1 and CCL2 expression.

Western Blot Analysis[1]

Cell Line: HEK293T cells
Concentration: 0.5 and 5μM
Incubation Time: 2 h
Result: Stabilized BRD4 at comparable concentrations to I-BET151 (HY-13235 ) (EC50 = 0.16 μM).
体内研究
(In Vivo)

DW34 (30 mg/kg；口服；9 或 12 小时) 通过降低趋化因子表达和细胞坏死，显著减轻 LPS (HY-D1056) 诱导的肝脏炎症以及 APAP (HY-66005) 诱导的毒性[1]。

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

Animal Model: N-acetyl-p-aminophenol (APAP) (HY-66005)-induced acute liver toxicity mice models (Wild-type C57BL/6J, male, 8-10 weeks)[1]
Dosage: 30 mg/kg
Administration: Orally administration; 12 h after 1 h of 500 mg/ kg APAP administration
Result: Led to significant reduction of chemokine expression of CXCL1, CXCL2, and CCL2.
Reduced level of neutrophil marker Ly6G.
Reduced cellular necrosis (H&E staining).
Animal Model: LPS (HY-D1056)-induced acute liver toxicity mice models (Wild-type C57BL/6J, male, 8-10 weeks)[1]
Dosage: 30 mg/kg
Administration: Orally administration; 9 h (1 h before 8 h of 4 mg/kg LPS injection)
Result: Induced a significant reduction in expression of the inflammatory chemokines CXCL1, CXCL2, and CCL2.
Reduced goblet cell.
分子量

434.58

Formula

C25H34N6O
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

DW34 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:

DW342758171-54-7DW 34DW-34Epigenetic Reader DomainNecroptosisBRD4 inhibitorLiver inflammationLPSAPAPHEK293T cellsTransformed sinusoidal endothelial cells (TSECs)Inhibitorinhibitorinhibit

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