2. Epigenetics
  3. DNA Methyltransferase
  4. DNMT1-IN-3

DNMT1-IN-3 (compound 7t-S) 是一种强效的 DNA 甲基转移酶 1 (DNMT1) 抑制剂，IC50 值为 0.777 μM，KD 值为 0.183 μM。DNMT1-IN-3 可与 DNMT1 中的 S - 腺苷甲硫氨酸 (SAM) 位点结合。DNMT1-IN-3 可通过诱导细胞凋亡和引起细胞 G0 / G1 期阻滞来抑制 K562 细胞的增殖，有潜力用于血液肿瘤的研究。

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DNMT1-IN-3 Chemical Structure

DNMT1-IN-3 Chemical Structure

CAS No. : 3025012-68-1

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DNMT1-IN-3 相关抗体

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DNA Methyltransferase DNMT1 DNMT3 MGMT

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DNMT1-IN-3 (compound 7t-S) is an effective DNA methyltransferase 1 (DNMT1) inhibitor with an IC50 value of 0.777 μM and a KD value of 0.183 μM. DNMT1-IN-3 can bind to the methyl donor S-adenosyl-l-methionine (SAM) site in DNMT1. DNMT1-IN-3 can inhibit cell proliferation in K562 cells by inducing cells apoptosis and arresting cell cycle at G0 / G1 phase, which has the potential to be used for the research of hematologic tumor[1].

IC50 & Target

DNMT1

0.777 μM (IC50)

体外研究
(In Vitro)

DNMT1-IN-3 (compound 7t-S) (0-400 μM; 48 h) 对包括 A2780、HeLa、K562 和 SiHa 在内的多种肿瘤细胞系表现出潜在的抗增殖活性[1]。
DNMT1-IN-3 (20-60 μM; 48 h) 通过流式细胞仪测定发现能以浓度依赖的方式诱导 K562 细胞停滞在 G0 / G1期[1]。
DNMT1-IN-3 (43.89 μM) 可以通过上调甲基化抑制的凋亡相关基因 (如死亡受体 TRAIL-R2/Dr5 和 TNFR-1 ) 的表达来诱导 K562 细胞凋亡。TRAIL-R2 可以通过募集 Caspase-8 或 Caspase-10 来启动下游 Caspase 级联反应来激发细胞凋亡信号。[1].

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

DNMT1-IN-3 相关抗体:

Cell Proliferation Assay[1]

Cell Line: A2780, HeLa, K562, SiHa cells
Concentration: 0-400 μM
Incubation Time: 48 hours
Result: Showed antiproliferative activity with IC50s of 78.88, 96.83, 43.89, 58.55 μM for A2780, HeLa, K562, SiHa cells, respectively.

Apoptosis Analysis[1]

Cell Line: K562 cells
Concentration: 20 μM, 40 μM, 60 μM
Incubation Time: 48 hours
Result: Demonstrated a concentration-dependent increase in apoptosis of K562 cells, with apoptotic rates of 7.06 %, 6.00 %, and 81.52 % at 20, 40, and 60 μM, respectively.

Cell Cycle Analysis[1]

Cell Line: K562 cells
Concentration: 20 μM, 40 μM, 60 μM
Incubation Time: 48 hours
Result: The percentage of cells in the G0 / G1 phase was significantly increased from 30.58 % to 61.74 % with DNMT1-IN-3 at 60 μM.
分子量

487.72

Formula

C23H13Cl3N2O4
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

DNMT1-IN-3 相关分类

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  • 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:

DNMT1-IN-33025012-68-1DNA MethyltransferaseDNMTsDNA MTasesA2780HeLaK562SiHaDNMT1 inhibitorCancerHematologic tumorInhibitorinhibitorinhibit

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