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，K_i 为 5 nM，选择性比其它 PMTs 高 20,000多倍。

规格

价格

库存

购买数量

5mg	RMB 1602.26	现货
25mg	RMB 4906.16	现货
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全国免费电话：400-668-6834 | Email：info@selleck.cn

客户使用Selleck生产的EPZ015666 (GSK3235025)发表文献14篇：

Cancer Cell, 2017, 32(4):411-426

PubMed: 28966034 ( click the link to review the publication )

Sci Adv, 2021, 7(13)eabc1834

PubMed: 33762328 ( click the link to review the publication )

Proc Natl Acad Sci U S A, 2020, 117(45):28068-28079

PubMed: 33097661 ( click the link to review the publication )

Signal Transduct Target Ther, 2020, 5(1):197

PubMed: 32994405 ( click the link to review the publication )

Theranostics, 2019, 9(9):2606-2617

PubMed: 31131056 ( click the link to review the publication )

EBioMedicine, 2019, 44:98-111

PubMed: 31101597 ( click the link to review the publication )

Front Immunol, 2019, 10:174

PubMed: 30800128 ( click the link to review the publication )

Osteoarthritis Cartilage, 2019, 27(6):932-944

PubMed: 30858101 ( click the link to review the publication )

Oxid Med Cell Longev, 2019, 2019:2345658

PubMed: 31885778 ( click the link to review the publication )

BMC Cancer, 2019, 19(1):1056

PubMed: 31694585 ( click the link to review the publication )

Cancer Res, 2018, 78(20):5731-5740

PubMed: 30135193 ( click the link to review the publication )

J Cell Mol Med, 2017, 21(4):781-790

PubMed: 27860244 ( click the link to review the publication )

Cell Signal, 2017, 34:55-65

PubMed: 28302565 ( click the link to review the publication )

Sci Signal, 2016, 9(443):rs9

PubMed: 27577262 ( click the link to review the publication )

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，K_i 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	Incubation Time	Activity Description	PMID
MDA-MB-468	M{nOcmZ2dmO2aX;uJIF{e2G7	NEGxN3k1QCCq	NGTlWFlqdmirYnn0d{BRWk2WNTDhZ5Rqfmm2eR?=	NI\EVGc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEm1O\|k5QCd-M{C5OVc6QDh:L3G+
HCC1954	M{PmZWNmdGxidnnhZoltcXS7IHHzd4F6		NHfwZWxKSzVyPUCuPEDPxE1?	NXLweW5DRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C5OVc6QDhpPkOwPVU4QTh6PD;hQi=>
MDA-MB-453	M1HSV2NmdGxidnnhZoltcXS7IHHzd4F6		NHntNIZKSzVyPUGg{txO	M1;xbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyOUW3PVg5Lz5\|MEm1O\|k5QDxxYU6=
HCC38	MYTD[YxtKH[rYXLpcIl1gSCjc4PhfS=>		MmHTTWM2OD1{LkKg{txO	MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODl3N{m4PEc,OzB7NUe5PFg9N2F-
MDA-MB-468	M1HISmNmdGxidnnhZoltcXS7IHHzd4F6		NV7z[Zh7UUN3ME2yMlIh\|ryP	NYfEWWZpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C5OVc6QDhpPkOwPVU4QTh6PD;hQi=>
MCF7	NUfaVHlGS2WubDD2bYFjcWyrdImgZZN{[Xl?		M2DucWlEPTB;Mj62JO69VQ>?	M1fmeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyOUW3PVg5Lz5\|MEm1O\|k5QDxxYU6=
SKBR3	MUXD[YxtKH[rYXLpcIl1gSCjc4PhfS=>		MoLUTWM2OD1\|Lkmg{txO	M1yzN\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyOUW3PVg5Lz5\|MEm1O\|k5QDxxYU6=
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Sf9	MX;GeY5kfGmxbjDhd5NigQ>?		M4fheGlvcGmkaYTpc44hd2ZiZoXscEBt\W6pdHigdoVkd22kaX7hcpQhcHWvYX6gSmxCTy22YXfn[YQhWFKPVEWv[pVtdCCuZX7neIghemWlb33ibY5idnRiaIXtZY4hUGm\|Nj30ZYdo\WRiTVXQOVAh\XiycnXzd4VlKGmwIHLhZ5Vtd3[rcoXzJIlv\mWldHXkJHNnQSCrboPlZ5Qh[2WubIOgeZNqdmdiYnnveIlvgWyjdHXkJIhqe3SxbnWgdIVxfGmmZTDhd{B{fWK\|dILheIUhcW5icILld4Vv[2Vib3[gX\|ZJZS2VQV2gZpkhXG:yY3;1cpQhdWW2aH;kMEBKSzVyPUCuNFIz\|ryP	MlHzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB\|Nk[2NVcoRjNyM{[2OlE4RC:jPh?=
Sf9	NGnPc3hHfW6ldHnvckBie3OjeR?=		M33lOWlvcGmkaYTpc44hd2ZiZoXscEBt\W6pdHigdoVkd22kaX7hcpQhcHWvYX6gSmxCTy22YXfn[YQhWFKPVEWv[pVtdCCuZX7neIghemWlb33ibY5idnRiaIXtZY4hUGm\|Nj30ZYdo\WRiTVXQOVAh\XiycnXzd4VlKGmwIHLhZ5Vtd3[rcoXzJIlv\mWldHXkJHNnQSCrboPlZ5Qh[2WubIOgeZNqdmdiYnnveIlvgWyjdHXkJIhqe3SxbnWgdIVxfGmmZTDhd{B{fWK\|dILheIUhcW5icILld4Vv[2Vib3[gX\|dJZS2VQV2gZpkhXG:yY3;1cpQhdWW2aH;kMEBKSzVyPUCuNFQ4\|ryP	NVXJTmtkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOlY3OTdpPkOwN\|Y3PjF5PD;hQi=>
Sf9	MkLMSpVv[3Srb36gZZN{[Xl?		M4rzRmlvcGmkaYTpc44hd2ZiZoXscEBt\W6pdHigdoVkd22kaX7hcpQhcHWvYX6gSmxCTy22YXfn[YQhWFKPVEWv[pVtdCCuZX7neIghemWlb33ibY5idnRiaIXtZY4hUGm\|Nj30ZYdo\WRiTVXQOVAh\XiycnXzd4VlKGmwIHLhZ5Vtd3[rcoXzJIlv\mWldHXkJHNnQSCrboPlZ5Qh[2WubIOgeZNqdmdiYnnveIlvgWyjdHXkJIhqe3SxbnWgdIVxfGmmZTDhd{B{fWK\|dILheIUhcW5icILld4Vv[2Vib3[gX\|hJZS2VQV2gZpkhXG:yY3;1cpQhdWW2aH;kMEBKSzVyPUCuNFQ4\|ryP	NIHwbGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEO2OlYyPyd-M{CzOlY3OTd:L3G+
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Sf9	MmHhSpVv[3Srb36gZZN{[Xl?		MWHJcohq[mm2aX;uJI9nKG[3bHygcIVv\3SqIILlZ49u[mmwYX70JIh2dWGwIF\MRWcufGGpZ3XkJHBTVVR3L3\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KGi3bXHuJGhqezZvdHHn[4VlKE2HUEWwJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDT[lkhcW6\|ZXP0JINmdGy\|IIXzbY5oKGKrb4Tpcplt[XSnZDDobZN1d26nIIDldJRq\GViYYOgd5Vje3S{YYTlJIlvKHC{ZYPlcoNmKG:oIGuxNmheNVODTTDifUBVd3Clb4XueEBu\XSqb3SsJGlEPTB;MD6wOFfPxE1?	NHH1Too9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|ME[wOVg{OCd-M{C2NFU5OzB:L3G+
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Sf9	NG\RdnpHfW6ldHnvckBie3OjeR?=		MUnJcohq[mm2aX;uJI9nKG[3bHygcIVv\3SqIILlZ49u[mmwYX70JIh2dWGwIF\MRWcufGGpZ3XkJHBTVVR3L3\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KGi3bXHuJGhqezZvdHHn[4VlKE2HUEWwJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDT[lkhcW6\|ZXP0JINmdGy\|IIXzbY5oKGKrb4Tpcplt[XSnZDDobZN1d26nIIDldJRq\GViYYOgd5Vje3S{YYTlJIlvKHC{ZYPlcoNmKG:oIGuxPGheNVODTTDifUBVd3Clb4XueEBu\XSqb3SsJGlEPTB;MD60Oe69VQ>?	NYXBVJdbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm4O\|AzPThpPkK5PFcxOjV6PD;hQi=>
Sf9	MWLGeY5kfGmxbjDhd5NigQ>?		MX3Jcohq[mm2aX;uJI9nKG[3bHygcIVv\3SqIILlZ49u[mmwYX70JIh2dWGwIF\MRWcufGGpZ3XkJHBTVVR3L3\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KGi3bXHuJGhqezZvdHHn[4VlKE2HUEWwJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDT[lkhcW6\|ZXP0JINmdGy\|IIXzbY5oKGKrb4Tpcplt[XSnZDDobZN1d26nIIDldJRq\GViYYOgd5Vje3S{YYTlJIlvKHC{ZYPlcoNmKG:oIGuxPWheNVODTTDifUBVd3Clb4XueEBu\XSqb3SsJGlEPTB;MD65Ou69VQ>?	MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN4Nk[xO{c,OzB\|Nk[2NVc9N2F-
Sf9	NGXEXpVHfW6ldHnvckBie3OjeR?=		NXm3UWZMUW6qaXLpeIlwdiCxZjDmeYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBHVEGJLYTh[4dm\CCSUl3UOU9nfWyuIHzlcod1cCC{ZXPvcYJqdmGwdDDoeY1idiCKaYO2MZRi\2enZDDNSXA2OCCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW2Z7IHnud4VkfCClZXzsd{B2e2mwZzDibY91cW67bHH0[YQhcGm\|dH;u[UBx\XC2aXTlJIF{KHO3YoP0doF1\SCrbjDwdoV{\W6lZTDv[kBcOjCKXT3TRW0h[nliVH;wZ492dnRibXX0bI9lNCCLQ{WwQVEvOc7:TR?=	NVixcGNmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOlY3OTdpPkOwN\|Y3PjF5PD;hQi=>
Sf9	M{OwUGZ2dmO2aX;uJIF{e2G7		Mn7wTY5pcWKrdHnvckBw\iCodXzsJIxmdme2aDDy[YNwdWKrbnHueEBpfW2jbjDGUGFINXSjZ3fl[EBRWk2WNT;meYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBJcXN4LYTh[4dm\CCPRWC1NEBmgHC{ZYPz[YQhcW5iYnHjeYxwfmm{dYOgbY5n\WO2ZXSgV4Y6KGmwc3XjeEBk\WyuczD1d4lv\yCkaX;0bY56dGG2ZXSgbIl{fG:wZTDw[ZB1cWSnIHHzJJN2[nO2cnH0[UBqdiCycnXz[Y5k\SCxZjDbNlFJZS2VQV2gZpkhXG:yY3;1cpQhdWW2aH;kMEBKSzVyPUGuPO69VQ>?	MoDUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB\|Nk[2NVcoRjNyM{[2OlE4RC:jPh?=
Sf9	MXXGeY5kfGmxbjDhd5NigQ>?		NXToc5BNUW6qaXLpeIlwdiCxZjDmeYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBHVEGJLYTh[4dm\CCSUl3UOU9nfWyuIHzlcod1cCC{ZXPvcYJqdmGwdDDoeY1idiCKaYO2MZRi\2enZDDNSXA2OCCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW2Z7IHnud4VkfCClZXzsd{B2e2mwZzDibY91cW67bHH0[YQhcGm\|dH;u[UBx\XC2aXTlJIF{KHO3YoP0doF1\SCrbjDwdoV{\W6lZTDv[kBcOjKKXT3TRW0h[nliVH;wZ492dnRibXX0bI9lNCCLQ{WwQVIvPs7:TR?=	MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN4Nk[xO{c,OzB\|Nk[2NVc9N2F-

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	H4R3me2s; PubMed: 28945229 Oncogene 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. PRMT5 / H3R8me2s ; PubMed: 30957988 Cancer Med 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.	28945229 30957988
Immunofluorescence	IKKβ; PubMed: 29158558 Leukemia 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 Cancer Med 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]

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)

参考文献

[1] Penebre et al. Epizyme, Inc.

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 Download EPZ015666 (GSK3235025) SDF

分子量	383.44
化学式	C₂₀H₂₅N₅O₃
CAS号	1616391-65-1
储存条件	3年-20°C 粉状 2年-80°C 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

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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、MSDS / 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

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、MSDS / 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
初始浓度:
稀释倍数:

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

通过输入化合物的化学式来计算其分子量：

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

研究领域

产品类型

定制您的化合物库

EPZ015666 (GSK3235025)

客户使用Selleck生产的EPZ015666 (GSK3235025)发表文献14篇：

客户使用该产品的1个实验数据：

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

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)

参考文献

溶解度 (25°C)

化学数据 Download EPZ015666 (GSK3235025) SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

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

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

技术支持

常见问题及建议解决方法

Histone Methyltransferase Signaling Pathway Map