2. Epigenetics Apoptosis Cell Cycle/DNA Damage
  3. DNA Methyltransferase Caspase MDM-2/p53 DNA/RNA Synthesis Apoptosis
  4. MC3817

MC3817 是一种选择性 DNMT 抑制剂。MC3817对 DNMT1和 DNMT3A/3L 的IC50 值分别为 0.044 μM 和 > 10 μM。MC3817 可抑制 P53 依赖性的癌细胞增殖，诱导细胞凋亡和DNA损伤，并提高 cleaved Caspase 3、P53 与 γH2AX 的水平。MC3817 可用于非小细胞肺癌、结肠癌、宫颈癌、三阴性乳腺癌以及组织细胞淋巴瘤的相关研究。

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MC3817

MC3817 Chemical Structure

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Customer Review

Other Forms of MC3817:

MC3817 相关抗体

Top Publications Citing Use of Products

查看 DNA Methyltransferase 亚型特异性产品:

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DNA Methyltransferase DNMT1 DNMT3 MGMT

查看 Caspase 亚型特异性产品:

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MC3817 is a selective DNMT1 inhibitor. MC3817 inhibits DNMT1 and DNMT3A/3L with IC50s of 0.044 μM and > 10μM, respectively. MC3817 inhibits P53-dependent cancer cell proliferation, induces apoptosis and DNA damage MC3817 elevates cleaved Caspase 3, P53, and γH2AX. MC3817 can be used in non-small cell lung cancer, colon cancer, cervical cancer, triple-negative breast cancer and histiocytic lymphoma research[1].

IC50 & Target

DNMT1

0.044 μM (IC50)

DNMT3a/3L

> 10 μM (IC50)

体外研究
(In Vitro)

MC3817 (compound 14) (0.05-100 μM, 48 h) 对 A549 与 H460 (非小细胞肺癌和肺癌细胞)、HCT-116 (结肠癌) 、HeLa (宫颈癌) 、MDA-MB-231 (三阴性乳腺癌) 以及 U937 (组织细胞淋巴瘤) 细胞均具有抗癌作用[1]。
MC3817 (2 μM, 24 和 48 h) 可阻滞 HCT-116 细胞于 S/G2M 期，并伴随凋亡性细胞死亡[1]。
MC3817 (0.5-5 μM, 16-48 h) 可触发 DNA 损伤并激活 p53/γH2AX 通路，从而导致 HCT-116 细胞发生细胞周期阻滞和凋亡[1]。
MC3817 (2.5 μM, 48 h) 在 HCT-116 P53 WT 细胞中诱导的细胞凋亡水平远高于在 HCT-116 P53−/− 细胞中诱导的水平[1]。

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

MC3817 相关抗体:

Cell Viability Assay[1]

Cell Line: A549 , H460, HCT-116, HeLa , MDA-MB 231, and U937
Concentration: 0.05-100 μM
Incubation Time: 48 h
Result: Had IC50 of 5.5 μM, 6.8 μM, 0.4 μM, 4.2 μM, 1.9 μM and 5.5μM for A549 cells, H460 cells, HCT-116 cells, HeLa cells, MDA-MB 231 cells, and U937 cells.

Cell Cycle Analysis[1]

Cell Line: HCT-116 cells
Concentration: 2 μM
Incubation Time: 48 h
Result: Caused a block in the S/G2M phase associated with apoptotic cell death, affecting over 50% of the cells after 48 h.

Western Blot Analysis[1]

Cell Line: HCT-116 cells
Concentration: 0.5, 1, 2.5, 5 μM
Incubation Time: 48 h
Result: Induced the accumulation of γH2AX and elevated p53 levels, indicating p53 stabilization and activation in response to DNA damage.

Apoptosis Analysis[1]

Cell Line: HCT-116 P53−/− cells and HCT-116 P53 WT cells.
Concentration: 2.5 μM
Incubation Time: 48 h
Result: Induced apoptotic cell death, as evidenced by significant PI/Annexin V fluorescence and extensive membrane blebbing in both cell lines.
分子量

721.55

Formula

C33H41Cl4N9O
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

MC3817 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:

MC3817MC 3817MC-3817DNA MethyltransferaseCaspaseMDM-2/p53DNA/RNA SynthesisApoptosisDNMTsDNA MTasesDNMTDNMT3A/3Lcleaved Caspase 3P53γH2AXnon-small cell lung cancercolon cancercervical cancertriple-negative breast cancerhistiocytic lymphoma researchInhibitorinhibitorinhibit

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