EPZ015666 (GSK3235025)

For research use only. Not for use in humans.

目录号：S7748

EPZ015666 (GSK3235025) Chemical Structure

CAS No. 1616391-65-1

EPZ015666 (GSK3235025)是一种有效的，选择性且口服生物有效的 PRMT5 抑制剂，Ki 为 5 nM，选择性比其它 PMTs 高 20,000多倍。

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RMB 1602.26 现货
RMB 4906.16 现货
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客户使用Selleck生产的EPZ015666 (GSK3235025)发表文献18篇：

客户使用该产品的1个实验数据：

  • (B) Effect of EPZ015666 on nuclear translocation of p65. Middle panel showed a representative photo of IF staining of p65 localization (green). Nuclei were stained with DAPI.

    J Cell Mol Med, 2016, 1-10.. EPZ015666 (GSK3235025) purchased from Selleck.

质量管理及产品安全说明书

Histone Methyltransferase抑制剂选择性比较

生物活性

产品描述 EPZ015666 (GSK3235025)是一种有效的，选择性且口服生物有效的 PRMT5 抑制剂，Ki 为 5 nM，选择性比其它 PMTs 高 20,000多倍。
靶点
PRMT5 [1]
(Cell-free assay)
5 nM(Ki)
体外研究

EPZ015666(GSK3235025)表现出有效的细胞活性，阻断SmD3的对称二甲基化，并抑制MCL细胞系(Z-138，Granta-519，Maver-1，Mino，和 Jeko-1)的增殖，IC50 为96-904 nM。[1]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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HCC1954 MVzD[YxtKH[rYXLpcIl1gSCjc4PhfS=> NWS3TpFGUUN3ME2wMlgh|ryP M4G0UFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyOUW3PVg5Lz5|MEm1O|k5QDxxYU6=
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HCC38 M4[1emNmdGxidnnhZoltcXS7IHHzd4F6 NUXFTlFMUUN3ME2yMlIh|ryP NXX0Omp1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C5OVc6QDhpPkOwPVU4QTh6PD;hQi=>
MDA-MB-468 M3qxeGNmdGxidnnhZoltcXS7IHHzd4F6 Mk\jTWM2OD1{LkKg{txO Mm\QQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB7NUe5PFgoRjNyOUW3PVg5RC:jPh?=
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Sf9 NGfiOoZHfW6ldHnvckBie3OjeR?= NEK4Wm9KdmirYnn0bY9vKG:oIH\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KGi3bXHuJGZNSUdvdHHn[4VlKFCUTWS1M4Z2dGxibHXu[5RpKHKnY3;tZolv[W62IHj1cYFvKEirc{[teIFo\2WmIF3FVFUxKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EBU\jliaX7z[YN1KGOnbHzzJJV{cW6pIHLpc5RqdnmuYYTl[EBpcXO2b37lJJBmeHSrZHWgZZMhe3Wkc4TyZZRmKGmwIIDy[ZNmdmOnIH;mJHszOEifLWPBUUBjgSCWb4Djc5VvfCCvZYToc4QtKEmFNUC9NU4y|ryP NVTsTlhCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOlY3OTdpPkOwN|Y3PjF5PD;hQi=>
Sf9 NXvVbZV5TnWwY4Tpc44h[XO|YYm= MYXJcohq[mm2aX;uJI9nKG[3bHygcIVv\3SqIILlZ49u[mmwYX70JIh2dWGwIF\MRWcufGGpZ3XkJHBTVVR3L3\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KGi3bXHuJGhqezZvdHHn[4VlKE2HUEWwJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDT[lkhcW6|ZXP0JINmdGy|IIXzbY5oKGKrb4Tpcplt[XSnZDDobZN1d26nIIDldJRq\GViYYOgd5Vje3S{YYTlJIlvKHC{ZYPlcoNmKG:oIGuyNWheNVODTTDifUBVd3Clb4XueEBu\XSqb3SsJGlEPTB;MT64{txO M1;ucVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{[2OlE4Lz5|MEO2OlYyPzxxYU6=
Sf9 Ml3LSpVv[3Srb36gZZN{[Xl? MXTJcohq[mm2aX;uJI9nKG[3bHygcIVv\3SqIILlZ49u[mmwYX70JIh2dWGwIF\MRWcufGGpZ3XkJHBTVVR3L3\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KGi3bXHuJGhqezZvdHHn[4VlKE2HUEWwJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDT[lkhcW6|ZXP0JINmdGy|IIXzbY5oKGKrb4Tpcplt[XSnZDDobZN1d26nIIDldJRq\GViYYOgd5Vje3S{YYTlJIlvKHC{ZYPlcoNmKG:oIGuyNmheNVODTTDifUBVd3Clb4XueEBu\XSqb3SsJGlEPTB;Mj62{txO NFvtcYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO2OlYyPyd-M{CzOlY3OTd:L3G+

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
PRMT5 / H3R8me2s ; 

PubMed: 30957988     


EPZ015666 inhibits PRMT5 activity. MDA‐MB‐468 cells were treated with the indicated concentration of the PRMT5 inhibitor EPZ015666 or with vehicle (DMSO). PRMT5 activity was assessed 48 h later by Western‐Blot analysis using antibodies that recognize symmetric dimethyl‐arginine on histones H3 (H3R8me2s) and H4 (H4R3me2s). PRMT5 expression was verified. Actin was used as a loading control. Images are from a single experiment representative of three independent experiments.

H4R3me2s; 

PubMed: 28945229     


U937 (CALM-AF10), NB4 (PML-RARα), and MonoMac6 (MLL-AF9) cell lines were dosed with EPZ015666 at indicated concentrations. H4R3me2s is shown at Day 4 for the 10, 3, 1, and 0μM doses.

30957988 28945229
Immunofluorescence
IKKβ; 

PubMed: 29158558     


H929 were treated with EPZ015666. After treatment, samples dual stained with Cyto-ID Green dye and IKKβ antibody were analyzed by fluorescence microscopy. Arrows indicate colocalization of IKKβ in the autophagosome.

29158558
Growth inhibition assay
Cell viability; 

PubMed: 30957988     


Treatment of breast cell lines with PRMT5 inhibitor EPZ015666 identifies a group of sensitive cell lines and a group of resistant cell lines. Cell viability was determined by MTT assay after four doubling times. Results are expressed as the percentage of cell growth relative to vehicle‐treated cells. The mean of at least three independent experiments for each cell line is presented. Breast cancer subtypes are indicated as follows: green (ER+), blue (ER‐/HER2+), red (ER‐/PR‐/HER2‐). The non‐tumorigenic breast cells, MCF‐10A and MCF‐12A, are in black.

30957988
体内研究 EPZ015666 (200 mg/kg, p.o.)在MCL异种移植动物模型中表现出强的抗肿瘤活性。[1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验：

[1]
- 合并
  • Cell lines: MCL细胞系(Z-138，Granta-519，Maver-1，Mino，和 Jeko-1)
  • Concentrations: 5 μM
  • Incubation Time: 12天
  • Method:

    --


    (Only for Reference)
动物实验：

[1]
- 合并
  • Animal Models: MCL (Z-138，和 Maver-1) 异种移植模型
  • Dosages: 200 mg/kg BID
  • Administration: p.o.
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 60 mg/mL warmed (156.47 mM)
Water Insoluble
Ethanol '48 mg/mL warmed
体内 从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)：
2% DMSO+30% PEG 300+ddH2O
 5mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 383.44
化学式

C20H25N5O3
CAS号 1616391-65-1
储存条件 粉状
溶于溶剂
别名

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 只
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Selleck为您提供正确的澄清溶液配方）
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量：

总分子量：g/mol

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1：

    I want to use this compound for injection, how to reconstitute it?

  • 回答：

    S7748, EPZ015666 is a clear solution in 2% DMSO+30% PEG300+68% water and it can be used for tail vein injection.

Selleck产品目录册

Histone Methyltransferase Signaling Pathway Map
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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID