GSK126 (Synonyms: GSK2816126A)

目录号: HY-13470 纯度: 99.76%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

GSK126 (GSK2816126A) 是一种有效，选择性的 EZH2 甲基转移酶抑制剂，IC₅₀ 为 9.9 nM。

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GSK126 Chemical Structure

CAS No. : 1346574-57-9

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥905	In-stock
5 mg	￥781	In-stock
10 mg	￥1162	In-stock
50 mg	￥2900	In-stock
100 mg	￥4000	In-stock
200 mg	现货	询价
500 mg		询价
1 g		询价

or 大包装询价

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Customer Review

MCE 顾客使用本产品发表的 64 篇科研文献

: GSK126 purchased from MCE. Usage Cited in: Cell. 2018 Sep 20;175(1):186-199.e19. [Abstract]; Cells are treated with EPZ-6438 (1 μM) or GSK126 (1 μM) for 6 days. Protein levels are analyzed by immunoblotting. Cells are treated with EPZ-6438 (1 μM), JQ1 (0.25 μM) alone or combination for 6 days. Protein levels are analyzed by immunoblotting.

: GSK126 purchased from MCE. Usage Cited in: J Exp Med. 2018 May 7;215(5):1365-1382. [Abstract]; Immunoblot analysis of Ezh2, H3K27me3, H3, and Hsp60 (loading control) in whole-cell lysates of the indicated proinflammatory genes of macrophages or microglia that are pretreated with DMSO or GSK126 (4 μM) for 3 d and then left nontreated (NT) or stimulated for 6 h with the ligands of different TLRs.

: GSK126 purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129. [Abstract]; The effects of treatment with the indicated epigenetic inhibitors on cleaved PARP (Clv-PARP) expression in both PC9/ER and HCC827/ER cells. β-actin is used as a loading control.

: GSK126 purchased from MCE. Usage Cited in: Oncotarget. 2015 Sep 29;6(29):27023-36. [Abstract]; This includes ATF3 (Activating Transcription Factor 3) and metastasis suppressor NDRG1 (N-Myc Downstream Regulated Gene 1) that also shows an upregulation in protein expression (phosphorylated at threonine 346) with GSK126 in two EZH2 mutant cell lines by western blot.

GSK126 相关产品

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•同靶点蛋白产品:

查看 Histone Methyltransferase 亚型特异性产品:

查看所有亚型

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

GSK126 (GSK2816126A) is a potent, highly selective inhibitor of EZH2 methyltransferase with an IC₅₀ of 9.9 nM^[1].

IC₅₀ & Target^[1]

EZH2

9.9 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	GI₅₀	18.7 μM Compound: GSK-126	Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by WST-1 assay Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by WST-1 assay	[PMID: 24767850]
BT-549	IC₅₀	16.27 μM Compound: GSK126	Antiproliferative activity against human BT-549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human BT-549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
Daudi	GI₅₀	11.2 μM Compound: GSK-126	Cytotoxicity against human Daudi cells assessed as growth inhibition after 72 hrs by WST-1 assay Cytotoxicity against human Daudi cells assessed as growth inhibition after 72 hrs by WST-1 assay	[PMID: 24767850]
HeLa	IC₅₀	0.28 μM Compound: GSK-126	Inhibition of EZH2 in human HeLa cells assessed as reduction in H3K27me3 levels incubated for 72 hrs by ELISA method Inhibition of EZH2 in human HeLa cells assessed as reduction in H3K27me3 levels incubated for 72 hrs by ELISA method	[PMID: 26189078]
HK-2	IC₅₀	> 40 μM Compound: GSK126	Antiproliferative activity against human HK-2 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human HK-2 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
HL-60	IC₅₀	14.05 μM Compound: GSK126	Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
L02	IC₅₀	> 40 μM Compound: GSK126	Antiproliferative activity against human L02 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human L02 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
MCF-10A	IC₅₀	> 40 μM Compound: GSK126	Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
MCF7	IC₅₀	21.38 μM Compound: GSK126	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
MDA-MB-231	IC₅₀	12.82 μM Compound: GSK126	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
MDA-MB-468	IC₅₀	11.92 μM Compound: GSK126	Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
MV4-11	IC₅₀	7.34 μM Compound: GSK126	Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
PC-3	IC₅₀	10.04 μM Compound: 8; GSK126	Antiproliferative activity against human PC-3 cells assessed as inhibition of cell proliferation incubated for 3 to 7 days followed by replacement of medium containing compound every 3 days by CCK8 assay Antiproliferative activity against human PC-3 cells assessed as inhibition of cell proliferation incubated for 3 to 7 days followed by replacement of medium containing compound every 3 days by CCK8 assay	[PMID: 35569264]
PC-3	GI₅₀	9.4 μM Compound: GSK-126	Cytotoxicity against human PC3 cells assessed as growth inhibition after 72 hrs by WST-1 assay Cytotoxicity against human PC3 cells assessed as growth inhibition after 72 hrs by WST-1 assay	[PMID: 24767850]
Pfeiffer	GI₅₀	0.18 μM Compound: GSK-126	Cytotoxicity against human Pfeiffer cells expressing EZH2 A667G mutant assessed as growth inhibition after 72 hrs by WST-1 assay Cytotoxicity against human Pfeiffer cells expressing EZH2 A667G mutant assessed as growth inhibition after 72 hrs by WST-1 assay	[PMID: 24767850]
SK-OV-3	IC₅₀	10.49 μM Compound: 8; GSK126	Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell proliferation incubated for 3 to 7 days followed by replacement of medium containing compound every 3 days by CCK8 assay Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell proliferation incubated for 3 to 7 days followed by replacement of medium containing compound every 3 days by CCK8 assay	[PMID: 35569264]
T98G	GI₅₀	12.6 μM Compound: GSK-126	Cytotoxicity against human T98G cells assessed as growth inhibition after 72 hrs by WST-1 assay Cytotoxicity against human T98G cells assessed as growth inhibition after 72 hrs by WST-1 assay	[PMID: 24767850]
U2932	GI₅₀	6.7 μM Compound: GSK-126	Cytotoxicity against human U2932 cells assessed as growth inhibition after 72 hrs by WST-1 assay Cytotoxicity against human U2932 cells assessed as growth inhibition after 72 hrs by WST-1 assay	[PMID: 24767850]
U-87MG ATCC	GI₅₀	28.5 μM Compound: GSK-126	Cytotoxicity against human U87MG cells assessed as growth inhibition after 72 hrs by WST-1 assay Cytotoxicity against human U87MG cells assessed as growth inhibition after 72 hrs by WST-1 assay	[PMID: 24767850]

体外研究
(In Vitro)

GSK126 可有效抑制野生型和突变型 EZH2 甲基转移酶活性，且效力相似 (K_i=0.5-3 nM)，与所用底物无关，并且与 S-腺苷甲硫氨酸 (SAM) 具有竞争性，与肽底物无竞争性。GSK126 对其他甲基转移酶和多种其他蛋白质类别 (EZH1，IC₅₀=680 nM) 具有高度选择性^[1]。用 GSK126 处理三种 SCLC 细胞系可诱导生长抑制。用 0.5、2 和 8 μM GSK126 处理 SCLC 细胞系 (Lu130、H209 和 DMS53)，并通过 WST-8 测定分析生长曲线。在所有三种细胞系中，8 μM 浓度的 GSK126 处理均会抑制细胞生长，而 Lu130 和 H209 对 GSK126 更敏感，即使在较低剂量下也是如此^[2]。

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

体内研究
(In Vivo)

GSK126 以每 20 克体重 0.2 毫升的剂量体积腹膜内注射给雌性米色 SCID 小鼠。GSK126 有效抑制 EZH2 突变 DLBCL 细胞系的增殖，并显著抑制小鼠 EZH2 突变 DLBCL 异种移植瘤的生长^[1]。

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

分子量

526.67

Formula

C₃₁H₃₈N₆O₂

CAS 号

1346574-57-9

性状

固体

颜色

White to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 12.5 mg/mL (23.73 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8987 mL	9.4936 mL	18.9872 mL
5 mM	0.3797 mL	1.8987 mL	3.7974 mL
10 mM	0.1899 mL	0.9494 mL	1.8987 mL

查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (2.37 mM); 澄清溶液

此方案可获得 ≥ 1.25 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 1.25 mg/mL (2.37 mM); 悬浊液; 超声助溶

此方案可获得 1.25 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 1.25 mg/mL (2.37 mM); 澄清溶液

此方案可获得 ≥ 1.25 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
方案四

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 0.82 mg/mL (1.56 mM); 澄清溶液
方案五

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.82 mg/mL (1.56 mM); 澄清溶液

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： 50% PEG300 50% Saline
Solubility: 10 mg/mL (18.99 mM); 悬浊液; 超声助溶
方案二

请依序添加每种溶剂： 20% SBE-β-CD in Saline adjusted to pH 4-4.5 with 1 N Acetic
Solubility: 20 mg/mL (37.97 mM); 澄清溶液; 超声加热助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.98%

选择批次：

Data Sheet (655 KB) SDS (537 KB)

COA (200 KB) HNMR (213 KB) RP-HPLC (148 KB) LCMS (122 KB)

产品使用指南 (1538 KB)

参考文献

[1]. McCabe MT, et al. EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations. Nature. 2012 Dec 6;492(7427):108-12. [Content Brief]

[2]. Sato T, et al. PRC2 overexpression and PRC2-target gene repression relating to poorer prognosis in small cell lung cancer. Sci Rep. 2013 May 29;3:1911. [Content Brief]

Kinase Assay ^[1]	The five-member PRC2 complex (Flag-EZH2, EED, SUZ12, AEBP2, RbAp48) containing either wild-type or mutant (A677G, Y641N, Y641C, Y641H, Y641S or Y641F) EZH2 is prepared. GSK126 is dissolved in DMSO and tested at concentrations of 0.6 nM to 300 nM with a final DMSO concentration of 2.5%. In contrast to wild-type EZH2 which prefers H3K27me0 as a substrate in vitro, EZH2 Y641 mutants prefer H3K27me2 and have little activity with H3K27me0 or H3K27me1. The A677G mutant is distinct from both the wild-type and Y641 mutant forms of EZH2 in that it efficiently methylates H3K27me0, H3K27me1, and H3K27me2; therefore, histone H3 peptides (residues 21-44; 10 μM final) with either K27me0 (wild type, A677G EZH2), K27me1 (A677G EZH2), or K27me2 (A677G, Y641N, Y641C, Y641H, Y641S and Y641F EZH2) are used as methyltransferase substrates. GSK126 is added to plates followed by addition of 6 nM EZH2 complex and peptide. As the potency of GSK126 is at or near the tight binding limit of an assay run at [SAM]=K_m, _IC50 values are measured at a high concentration of the competitive substrate SAM relative to its K_m (7.5 μM SAM where the SAM K_m is 0.3 μM)^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[2]	JUB- and PTRF-introduced DMS53 cells are seeded at density of 1×10³ cells/well in 96-well plate, and cellular growth is analyzed using WST-8 kit at 12, 36, 60, and 84 h. Cellular growth of Lu130, H209, and DMS53 with treatment by DZNep or GSK126 is also analyzed using WST-8 kit. DZNep is dissolved in PBS at 5 mM, and cells are cultured at the final concentration of 5 μM. GSK126 is dissolved in DMSO at 10 mM, and cells are cultured at 0.5, 2, and 8 μM^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] GSK126 or vehicle is administered intraperitoneally at a dose volume of 0.2 mL per 20 g body weight. Pfeiffer or KARPAS-422 cells (1×10⁷) in 100% Matrigel are implanted subcutaneously in female beige SCID mice. Tumors are measured with calipers, and block randomized according to tumour size into treatment groups. For efficacy studies, 10 mice are randomized in each treatment group before the initiation of dosing and GSK126 treatment is initiated once the tumour volumes are approximately 200 mm³ in the Pfeiffer and KARPAS-422 studies and 500 mm³ in the KARPAS-422 intermittent dosing study. Mice are weighed and tumors measured with calipers twice weekly. Two-tailed t-tests are conducted assuming two samples of equal variance. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. McCabe MT, et al. EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations. Nature. 2012 Dec 6;492(7427):108-12. [Content Brief] [2]. Sato T, et al. PRC2 overexpression and PRC2-target gene repression relating to poorer prognosis in small cell lung cancer. Sci Rep. 2013 May 29;3:1911. [Content Brief]

GSK126 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.8987 mL	9.4936 mL	18.9872 mL	47.4681 mL
	5 mM	0.3797 mL	1.8987 mL	3.7974 mL	9.4936 mL
	10 mM	0.1899 mL	0.9494 mL	1.8987 mL	4.7468 mL
	15 mM	0.1266 mL	0.6329 mL	1.2658 mL	3.1645 mL
	20 mM	0.0949 mL	0.4747 mL	0.9494 mL	2.3734 mL

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:

GSK1261346574-57-9GSK2816126AGSK 126GSK-126Histone MethyltransferaseInhibitorinhibitorinhibit

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GSK126 (Synonyms: GSK2816126A)

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实验参考方法

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

GSK126 相关分类

完整储备液配制表

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GSK126 (Synonyms: GSK2816126A)

Customer Review

GSK126 相关抗体

MCE 顾客使用本产品发表的 64 篇科研文献

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生物活性

实验参考方法

纯度 & 产品资料

参考文献

GSK126 相关抗体:

摩尔计算器

稀释计算器

GSK126 相关分类

完整储备液配制表

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