2. Epigenetics
  3. DNA Methyltransferase
  4. DNMT-IN-5

DNMT-IN-5 是一种稳定高效的 DNA 甲基转移酶 (DNMT) 抑制剂,其 IC50 为 0.78 nM。DNMT-IN-5 对 DNMT3A 的抑制活性可达到亚微摩尔水平，能够上调靶向基因的表达，抑制细胞增殖，并引发关键的细胞周期停滞。DNMT-IN-5 可用于研究 p53 缺失型结直肠癌。

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DNMT-IN-5 Chemical Structure

DNMT-IN-5 Chemical Structure

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DNMT-IN-5 相关抗体

Top Publications Citing Use of Products

查看 DNA Methyltransferase 亚型特异性产品:

查看所有亚型
DNA Methyltransferase DNMT1 DNMT3 MGMT

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DNMT-IN-5 is a stable and efficient DNA methyltransferase (DNMT) inhibitor with high stability and high activity with an IC50 of 0.78 nM. DNMT-IN-5 exhibits sub-micromolar DNMT3A inhibitory activity, upregulates the expression of DNMT-targeted genes, impairs cell proliferation, and triggers a critical cell cycle arrest. DNMT-IN-5 can be used for the study of p53-depleted colorectal cancer[1].

体外研究
(In Vitro)

DNMT-IN-5 (Compound 34b) (0.1-30 μM; 3 days) 在纳摩尔水平仍具备DNMT 3A抑制剂的活性，在 HCT-116 细胞的 IC50 值为9.15 μM[1]。

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

DNMT-IN-5 相关抗体:

Cell Viability Assay[1]

Cell Line: HCT-116
Concentration: 0.1 μM; 1 μM; 10 μM; 100 μM
Incubation Time: 3 days
Result: Showed very similar cytotoxicity (IC50 = 9.15 μM) among themselves and reference compound MLo1506 (IC50 = 8.18 μM).

RT-PCR[1]

Cell Line: HCT-116
Concentration: 5 μM
Incubation Time: 0 d; 2 d; 5d
Result: Significantly induced the upregulation of p15 expression by 1.76 (88%)-fold, compared to nontreated cells.
Increased p16 expression by 1.34 (67%)-fold.

Cell Cycle Analysis[1]

Cell Line: HCT-116, DU-145, U2OS
Concentration: 5 μM
Incubation Time: 5 days
Result: Did not alter p15 expression in p53-KO cells but successfully induced p16 re-expression.
Strongly impaired the G1/S transition in the absence of p53 and led to a substantial population of defective replicating cells.
分子量

367.62

Formula

C16H12BrClO3
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

DNMT-IN-5 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:

DNMT-IN-5DNA MethyltransferaseDNMTsDNA MTasesInhibitorinhibitorinhibit

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