Home>>Signaling Pathways>> DNA Damage/DNA Repair>> DNA Methyltransferase>>DC_517

DC_517 Sale

目录号 : GC32872

DC_517是一种DNMT1抑制剂,IC50和Kd值分别为1.7μM和0.91μM。

DC_517 Chemical Structure

Cas No.:500017-70-9

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥3,476.00
现货
2mg
¥2,082.00
现货
5mg
¥3,124.00
现货
10mg
¥5,355.00
现货
50mg
¥16,065.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

实验参考方法

Kinase experiment:

To measure the effects of DC_517 on mouse DNMT1 activity, 200 nM purified DNMT1 is incubated with 200 μM of DC_517 and S-adenosylmethionine (AdoMet) in the DNMT assay buffer in the assay plate at 37°C for 2 h. Next, every sample is incubated with the capture and detection antibody, followed by incubation with developer solution for 10 min at room temperature. The absorbance is measured at 450 nm using a microplate reader. S-Adenosylhomocysteine (AdoHcy) is used as a positive control[1].

References:

[1]. Chen S, et al. Identifying novel selective non-nucleoside DNA methyltransferase 1 inhibitors through docking-based virtual screening. J Med Chem. 2014 Nov 13;57(21):9028-9041.

产品描述

DC_517 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 1.7 μM and 0.91 μM, respectively.

DC_517 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 1.7 μM and 0.91 μM, respectively. DC_517 (1.25, 2.5, 5, and 10 μM) potently inhibits the proliferation of HCT116 (human colon cancer) and Capan-1 (human pancreatic adenocarcinoma cells) after treatment for 24, 48, and 72 h. DC_517 (0, 0.75, 1.5, and 3 μM) also dose-dependently induces apoptotic cell death in HCT116 cells[1].

[1]. Chen S, et al. Identifying novel selective non-nucleoside DNA methyltransferase 1 inhibitors through docking-based virtual screening. J Med Chem. 2014 Nov 13;57(21):9028-9041.

Chemical Properties

Cas No. 500017-70-9 SDF
Canonical SMILES OC(CNC(C)C)COC(CN1C(C=CC=C2)=C2C3=C1C=CC=C3)CN(C4=CC=CC=C45)C6=C5C=CC=C6
分子式 C33H35N3O2 分子量 505.65
溶解度 DMSO : ≥ 50 mg/mL (98.88 mM);Water : < 0.1 mg/mL (insoluble) 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 1.9777 mL 9.8883 mL 19.7765 mL
5 mM 0.3955 mL 1.9777 mL 3.9553 mL
10 mM 0.1978 mL 0.9888 mL 1.9777 mL
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % saline
计算重置

Research Update

DNMT1 involved in the analgesic effect of folic acid on gastric hypersensitivity through downregulating ASIC1 in adult offspring rats with prenatal maternal stress

CNS Neurosci Ther 2023 Feb 27.PMID:36852448DOI:10.1111/cns.14131

Aims: Gastric hypersensitivity (GHS) is a characteristic pathogenesis of functional dyspepsia (FD). DNA methyltransferase 1 (DNMT1) and acid-sensing ion channel 1 (ASIC1) are associated with GHS induced by prenatal maternal stress (PMS). The aim of this study was to investigate the mechanism of DNMT1 mediating the analgesic effect of folic acid (FA) on PMS-induced GHS. Methods: GHS was quantified by electromyogram recordings. The expression of DNMT1, DNMT3a, DNMT3b, and ASIC1 were detected by western blot, RT-PCR, and double-immunofluorescence. Neuronal excitability and proton-elicited currents of dorsal root ganglion (DRG) neurons were determined by whole-cell patch clamp recordings. Results: The expression of DNMT1, but not DNMT3a or DNMT3b, was decreased in DRGs of PMS rats. FA alleviated PMS-induced GHS and hyperexcitability of DRG neurons. FA also increased DNMT1 and decreased ASIC1 expression and sensitivity. Intrathecal injection of DNMT1 inhibitor DC-517 attenuated the effect of FA on GHS alleviation and ASIC1 downregulation. Overexpression of DNMT1 with lentivirus not only rescued ASIC1 upregulation and hypersensitivity, but also alleviated GHS and hyperexcitability of DRG neurons induced by PMS. Conclusions: These results indicate that increased DNMT1 contributes to the analgesic effect of FA on PMS-induced GHS by reducing ASIC1 expression and sensitivity.