GSK126 | GSK2816126A | EZH2 Inhibitor | AmBeed-信号通路专用抑制剂

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GSK126 {[allProObj[0].p_purity_real_show]}

货号：A114568 同义名： GSK2816126A;GSK2816126

GSK126是一种强效、高选择性的 EZH2 甲基转移酶抑制剂，IC50 为 9.9 nM，且对 EZH2 的选择性是其他 20 种人类甲基转移酶的 1000 倍以上。

GSK126 化学结构
CAS号：1346574-57-9

GSK126 3D分子结构
CAS号：1346574-57-9

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GSK126 纯度/质量文件产品仅供科研

货号：A114568 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Neuron, 2025. Ambeed. [ A1440350 ]; • Nature Communications, 2025, 16, 996. Ambeed. [ A111960 , A505336 ]; • JACS, 2025. Ambeed. [ A349578 , A2270125 ]; • PLoS Biol., 2025, 23(2): e3002961. Ambeed. [ A181909 ]; • Redox Rep., 2025, 30(1): 2454887. Ambeed. [ A1155014 ]; 更多 >

表观遗传阅读框亚型比较
组蛋白甲基转移酶亚型比较

产品名称	BET ↓ ↑	bromodomain ↓ ↑	BRPF ↓ ↑	CBP/beta-catenin ↓ ↑	p300/CBP ↓ ↑	其他靶点	纯度
MS436	++ BRD4 (1), Ki: <0.085 μM BRD4 (2), Ki: 0.34 μM						99%+
CPI-203	+++ BRD4, IC50: 37 nM						98+%
GSK1324726A	+++ BRD4, IC50: 22 nM BRD2, IC50: 31 nM						99%+
PFI-1	++ BRD4, IC50: 0.22 μM BRD2, IC50: 98 nM						98%
Apabetalone	+ BD2, IC50: 0.51 μM						99%
(+)-JQ1	+++ BRD4 (1), IC50: 77 nM BRD4 (2), IC50: 33 nM						98%
I-BET151	+ BRD3, IC50: 0.25 μM BRD4, IC50: 0.5 μM						98%
Molibresib	+++ BET proteins, IC50: 35 nM						99%+
I-BRD9	+++ BRD4, pIC50: 5.3 BRD9, pIC50: 7.3						99%+
BI-7273	++++ BRD7, IC50: 117 nM BRD9, IC50: 19 nM						99+%
Pelabresib	+++ BRD4-BD1, IC50: 39 nM						98%
ARV-825	+++ BRD4 BD2, Kd: 28 nM BRD4 BD1, Kd: 90 nM						99%+
Birabresib							99%+
BI 2536	+++ BRD4, Kd: 37 nM					c-Myc	99%+
Bromosporine	++ BRD2, IC50: 0.29 μM BRD9, IC50: 0.122 μM	++++ CECR2, IC50: 17 nM					99%+
XMD8-92	++ BRD4 (1), Kd: 170 nM						99%+
Mivebresib	✔						99%+
BI-9564	++++ BRD7, Kd: 73 nM BRD9, Kd: 5.9 nM	++ CECR2, Kd: 77 nM					98%
AZD5153 6-Hydroxy-2-naphthoic acid	++++ FL-BRD4, IC50: 5 nM						99%+
PLX51107	++++ BRD4 BD2, Kd: 1.7 nM BRD3 BD1, Kd: 2.1 nM						99%+
FL-411	+ BRD4(1), IC50: 0.43 μM						99%+
ABBV-744	✔						99%+
dBET6	++++ BRD4, IC50: 14 nM						99%+
dBET1	++++ BRD4, IC50: 20 nM						99%+
MZ1	++++ Brd2(BD2), Kd: 62 nM Brd3(BD2), Kd: 13 nM						99%+
dBET57	+ BRD4_BD1, DC50: 500 nM						99%+
SF2523	+ BRD4, IC50: 241 nM					DNA-PK	99%+
INCB054329	++++ BRD3-BD1, IC50: 9 nM BRD4-BD1, IC50: 119 nM						99%
INCB-057643	✔						99%+
(E/Z)-ZL0420	+++ BRD4 BD1, IC50: 27 nM BRD4 BD2, IC50: 32 nM						99%+
BMS-986158	✔						99%+
BRD4 Inhibitor-10	++++ BRD4-BD2, IC50: 41 nM BRD4-BD1, IC50: 5 nM						97%
A1874	✔						99%+
Y06036	++ BRD4 (1), Kd: 82 nM						99%+
Alobresib	✔					NF-κB	98%
ODM-207	✔						99%
GSK778	+++ BRD2-BD1, IC50: 75nM BRD4-BD1, IC50: 143 nM						97%
SRX3207	+ BRD41, IC50: 3070 nM BRD42, IC50: 3070 nM					Syk	98%
GSK046	+++ BRD3_BD2, IC50: 98 nM BRD4_BD2, IC50: 214 nM						98%
GSK620	✔						97%
Thalidomide-NH-C4-NH-Boc	✔						98%
Trotabresib	✔						99%
NHWD-870	✔						98%
CFT8634	++++ BRD9, DC50: 3 nM						99%
GSK2801		++ BAZ2B, Kd: 136 nM BAZ2A, Kd: 257 nM					99%+
KG-501		✔					99%+
UNC 669		+ L3MBTL4, IC50: 6 μM L3MBTL3, IC50: 35 μM					99%
PFI-3		+++ SMARCA4, Kd: 55 nM SMARCA2A, Kd: 72 nM					99%+
UNC1215		+++ L3MBTL3- D274A, IC50: 3.5 μM L3MBTL3, IC50: 120 nM					99%+
EED226		++ PRC2, Kd: 114 nM EED, Kd: 82 nM					99%+
BRD9539		✔					98%
UNC926		+ L3MBTL1, Kd: 3.9 μM					99%
666-15		++ CREB, IC50: 81 nM					99%+
UNC6852		+ EED, IC50: 247 nM					98%
BAZ1A-IN-1		+ BAZ1A, Kd: 0.52 μM					99%+
PFI-4			++ BRPF1, IC50: 80 nM BRPF2, IC50: 7.9 μM				99%+
OF-1			++ BRPF2, Kd: 500 nM BRPF1B, Kd: 100 nM				99%+
GSK-5959			++ BRPF3, pIC50: 7.1 BRPF2, pIC50: 5.2				99%
GSK6853			++++ BRPF1, pIC50: 8.1				99%+
NI-42			++++ BRPF1, IC50: 48 nM BRPF3, IC50: 260 nM				99%+
E-7386				+++ CBP/beta-catenin, IC50: 0.0484 μM			99%
I-CBP112					++ p300, Kd: 167 nM CBP, Kd: 151 nM		98+%
Histone Acetyltransferase Inhibitor II					+ p300, IC50: 5 μM		98%
C646					+ p300/CBP, Ki: 400 nM		99%+
Anacardic Acid					+ PCAF, IC50: 5 μM p300/CBP, IC50: 8.5 μM		99%+
SGC-CBP30					++++ CREBBP, IC50: 21 nM EP300, IC50: 38 nM		99%+
Nordihydroguaiaretic acid					✔	IGF-1R,HER2	99%+
Curcumin					+ p300, IC50: ~25 μM	NF-κB,Nrf2,Ferroptosis	98%
PF-CBP1 HCl					++ CREBBP, IC50: 125nM p300/CBP, IC50: 363nM		97%
CPI-637					+++ CBP, IC50: 0.03 μM EP300, IC50: 0.051 μM		99%+
Foscenvivint					✔	β-catenin	99%+
A-485					++ p300 HAT, IC50: 0.06 μM		99%+
GNE-781	+ BRD4(1), IC50: 5100 nM				++++ CBP, IC50: 0.94 nM		99%
NEO2734	+++ BET, IC50: <30 nM				+++ p300/CBP, IC50: <30 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	Histone Methyltransferase ↓ ↑	纯度
BRD4770	✔	99%+
UNC1999	+++ EZH2, IC50: 2 nM EZH1, IC50: 45 nM	99%+
EPZ005687	++ EZH2, Ki: 24 nM	98+%
EPZ015666	+++ PRMT5, Ki: 5 nM	99%+
3-Deazaneplanocin A HCl	++++ S-adenosylhomocysteine hydrolase, Ki: 50 pM	99%+
Tazemetostat	+++ EZH2, IC50: 11 nM EZH2, Ki: 2.5 nM	98%
GSK126	++ EZH2, IC50: 9.9 nM	99%+
MI-3	+ Menin-MLL, IC50: 648 nM	98%
MM-102	++ MLL1, IC50: 0.4 μM	99%
EI1	++ EZH2 (Y641F), IC50: 13 nM Ezh2 (wild-type), IC50: 15 nM	99% (HPLC)
SGC0946	++++ DOT1L, IC50: 0.3 nM	99%+
PFI-2 HCl	++++ SETD7, IC50: 2 nM SETD7, Ki: 0.33 nM	99%+
Pinometostat	++++ DOT1L, Ki: 80 pM	99%+
EPZ004777	+++ DOT1L, IC50: 0.4 nM	99%+
Entacapone	++ COMT, IC50: 151 nM	95%
UNC0379	+ SETD8, IC50: 7.9 μM	99%+
Menin-MLL inhibitor MI-2	+ Menin-MLL, IC50: 446 nM	98%
GSK343	+++ EZH2, IC50: 4 nM EZH1, IC50: 240 nM	99%+
BIX-01294 3HCl	+ G9a, IC50: 2.7 μM	99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

GSK126 生物活性

靶点	Histone Methyltransferase EZH2, IC50:9.9 nM
描述	EZH2 is the enzymatic subunit of PRC2 (Polycomb repressive complex 2), a complex that can methylate lysine 27 of histone H3 (H3K27) to promote transcriptional silencing. GSK126 is a potent inhibitor of EZH2 and inhibits both wild-type and mutant EZH2 methyltransferase activity with similar potencies (Ki^app=0.5 - 3 nM, measure by enzymatic activity) and has more than 1,000-fold selectivity for EZH2 as compared with other methyltransferases and 150-fold as compared to EZH1 (Ki^app = 89 nM). GSK126 induced a 50% loss of H3K27me3 in both EZH2 wild-type and mutant DLBCL cell lines at concentrations ranging from 7 - 252 nM independent of EZH2 mutation status (treated with GSK126 for 48h). GSK126 most potently inhibited H3K27me3, followed by H3K27me2 and H3K27me1 were only weakly reduced at the highest inhibitor concentration, with no effect on total histone H3 and PRC2 components. Following 10 days of once-daily dosing of GSK126 in mice using subcutaneous xenografts of KARPAS-422 and Pfeiffer cells, on dose 15 - 150 mg/kg, global H3K27me3 decreased and EZH2 targeted genes (TXNIP and TNFRSF21) expression increased in a dose dependent fashion. With daily 50 mg/kg dosing, complete tumor growth inhibition can be observed in both KARPAS-422 and Pfeiffer cell models. Complete tumor eradication can be observed on dose of 150 mg/kg daily or 300 mg/kg twice a week^[1].
作用机制	GSK126 is the SAM-competitive inhibitor of PRC2^[1].

GSK126 细胞研究

细胞系	浓度	检测类型	检测时间	活性说明	数据源
human A549 cells		Cytotoxic assay	72 h	Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by WST-1 assay, GI50=18.7 μM.	24767850
human Daudi cells		Cytotoxic assay	72 h	Cytotoxicity against human Daudi cells assessed as growth inhibition after 72 hrs by WST-1 assay, GI50=11.2 μM.	24767850
human HeLa cells		Function assay	72 h	Inhibition of EZH2 in human HeLa cells assessed as reduction in H3K27me3 levels incubated for 72 hrs by ELISA method, IC50=0.28 μM.	26189078
human PC3 cells		Cytotoxic assay	72 h	Cytotoxicity against human PC3 cells assessed as growth inhibition after 72 hrs by WST-1 assay, GI50=9.4 μM.	24767850

GSK126 动物研究

Dose

Mice: 2.5 mg/kg^[2] (i.v.); min = 125 mg/kg, max = 1000 mg/kg^[3] (p.o.)

Administration

i.v., p.o.

Pharmacokinetics

Animal	Rats^[4]
Dose	50 mg/kg
Administration	p.o.
C_max	155.6 ± 42.4 ng/ml
T_max	0.25 h
AUC_0→∞	636.3 ± 82.0 h·ng/ml
T_β	10.7 ± 3.2 h

GSK126 参考文献

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

[2]Zhang P, de Gooijer MC, et al. ABCB1 and ABCG2 restrict the brain penetration of a panel of novel EZH2-Inhibitors. Int J Cancer. 2015 Oct 15;137(8):2007-18.

[3]Campbell JE, Kuntz KW, et al. EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity. ACS Med Chem Lett. 2015 Mar 4;6(5):491-5.

[4]EZH2 Inhibitor GSK126: Metabolism, drug transporter and rat pharmacokinetic studies

GSK126 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.90mL

0.38mL

0.19mL

9.49mL

1.90mL

0.95mL

18.99mL

3.80mL

1.90mL

GSK126 技术信息

CAS号	1346574-57-9
分子式	C₃₁H₃₈N₆O₂
分子量	526.672

别名	GSK2816126A;GSK2816126
运输	蓝冰

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place,Sealed in dry,2-8°C

溶解方案

细胞实验：

DMSO: 12 mg/mL(22.78 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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

方案二

动物实验配方

IP 5% DMSO+water 0.8 mg/mL clear

PO 0.5% CMC-Na 48 mg/mL suspension

GSK126 {[allProObj[0].p_purity_real_show]}

GSK126 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

GSK126 质控信息

GSK126 生物活性

GSK126 细胞研究

GSK126 动物研究

GSK126 参考文献

GSK126 实验方案

GSK126 技术信息

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GSK126 {[allProObj[0].p_purity_real_show]}

GSK126 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

GSK126 质控信息

GSK126 生物活性

GSK126 细胞研究

GSK126 动物研究

GSK126 参考文献

GSK126 实验方案

GSK126 技术信息

最近浏览的产品

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摩尔计算器

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总药量计算器

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GSK126 纯度/质量文件产品仅供科研