2. Cell Cycle/DNA Damage Epigenetics Apoptosis Neuronal Signaling Immunology/Inflammation GPCR/G Protein
  3. CDK HDAC Apoptosis Histamine Receptor
  4. MFDCH016

MFDCH016 是一种强效的 HDAC1/6 (IC50 = 38/59 nM) 和 CDK4/6 (IC50 = 680/720nM) 抑制剂。MFDCH016 可诱导 MCF-7 细胞凋亡 (apoptosis)，并使细胞周期阻滞于 G2/M 期和 G0/G1 期。MFDCH016 可调节 HDAC-p21-CDK 信号通路，增加乙酰化 H3 和 p21 的水平。MFDCH016 可用于乳腺癌的研究。

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MFDCH016

MFDCH016 Chemical Structure

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MFDCH016 相关抗体

Top Publications Citing Use of Products

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MFDCH016 is a potent HDAC1/6 (IC50 = 38/59 nM) and CDK4/6 (IC50 = 680/720nM) inhibitor. MFDCH016 induces apoptosis and cell cycle arrest in G2/M and G0/G1 phases in MCF-7 cells. MFDCH016 can modulate the HDAC-p21-CDK signaling pathway, increasing the levels of acetylated H3 and p21. MFDCH016 can be used for the study of breast cancer[1].

体外研究
(In Vitro)

MFDCH016 (1 μM、10 μM，72 小时) 对 MCF-7 细胞的增殖抑制率分别为 55% 和 86% (浓度分别为 1 μM 和 10 μM)[1]。
MFDCH016 (1 μM、10 μM) 呈剂量依赖性地抑制多种癌细胞系的活性，包括 MCF-7、T47D、A549、NCI-H460、NCI-H1299、FaDu、UDSCC-2、MC38 和 CT26[1]。
MFDCH016 (0.001-100 μM) 对 MCF-7 乳腺癌细胞具有良好的抑制作用 (GI50 = 2.476 μM)[1]。
MFDCH016 (12-72 小时) 能有效抑制 MCF-7 细胞的增殖，其特征是细胞周期阻滞于 G0/G1 期，S 期和 G2/M 期细胞比例显著降低，最终导致细胞凋亡。此外，还能显著上调乙酰化 H3 和 p21 蛋白水平，并下调细胞周期蛋白 D1 的表达，这些作用随时间推移而增强，并在 72 小时达到峰值[1]。
MFDCH016 (10 μM) 对 hERG-HEK 稳定细胞系中的所有 hERG 通道均表现出较低的心脏毒性，在 10 μM 浓度下平均抑制率为 [1]。
MFDCH016 对其他 CDK 的活性可忽略不计 (大多数亚型的 IC50 > 5000 nM，CDK1、CDK2、CDK7 和 CDK10 的 IC50 > 10,000 nM) ，对非靶向 CDK 的选择性倍数超过 700 倍[1]。
MFDCH016 对 CYP1A2 (20.7%)、CYP2C9 (29.2%) 和 CYP2C19 (26.5%) 表现出中等程度的抑制作用，而对 CYP2D6 (14.8%) 的抑制作用较弱[1]。

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

MFDCH016 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: MCF-7 human breast cancer cell line
Concentration: 1 μM, 10 μM
Incubation Time: 72 h
Result: Showed a proliferation inhibition rate of 55% and 86% against MCF-7 cells at concentrations of 1 μM and 10 μM, respectively.
体内研究
(In Vivo)

MFDCH016 (40 mg/kg，腹腔注射，每日一次，持续 14 天) 是一种有效的体内抗肿瘤药物，在 MCF-7 荷瘤小鼠中具有显著的抗肿瘤作用，且无明显毒性[1]。

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

Animal Model: MCF-7 xenograft model using BALB/c female mice (n = 4/6 per group)[1].
Dosage: 40 mg/kg
Administration: I.p., once daily for 14 days
Result: Exhibited a strong antitumor effect, with a low average tumor weight.
Body weight remained stable, with no evidence of toxicity or weight loss.
分子量

534.61

Formula

C27H34N8O4
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

MFDCH016 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:

MFDCH016MFDCH 016MFDCH-016CDKHDACApoptosisHistamine ReceptorCyclin dependent kinaseHistone deacetylasesAntiproliferative activityCyclin-dependent kinaseHistone deacetylaseIn vivo antitumor activityPharmacokinetic propertiesInhibitorinhibitorinhibit

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