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GSK343 {[allProObj[0].p_purity_real_show]}

货号：A135977 Ambeed 开学季，买赠积分，赢豪礼

GSK343是一种极其强效和选择性的 EZH2 抑制剂，IC50 为 4 nM。

GSK343 化学结构 CAS号：1346704-33-3
GSK343 化学结构
CAS号：1346704-33-3
GSK343 3D分子结构
CAS号：1346704-33-3
GSK343 化学结构 CAS号：1346704-33-3
GSK343 3D分子结构 CAS号：1346704-33-3
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GSK343 纯度/质量文件 产品仅供科研

货号：A135977 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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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

 		{[allProObj[0].p_purity_real_show]}
CPI-203 +++

BRD4, IC50: 37 nM

 		{[allProObj[0].p_purity_real_show]}
GSK1324726A +++

BRD4, IC50: 22 nM

BRD2, IC50: 31 nM

 		{[allProObj[0].p_purity_real_show]}
PFI-1 ++

BRD4, IC50: 0.22 μM

BRD2, IC50: 98 nM

 		{[allProObj[0].p_purity_real_show]}
Apabetalone +

BD2, IC50: 0.51 μM

 		{[allProObj[0].p_purity_real_show]}
(+)-JQ1 +++

BRD4 (2), IC50: 33 nM

BRD4 (1), IC50: 77 nM

 		{[allProObj[0].p_purity_real_show]}
I-BET151 +

BRD4, IC50: 0.5 μM

BRD3, IC50: 0.25 μM

 		{[allProObj[0].p_purity_real_show]}
Molibresib +++

BET proteins, IC50: 35 nM

 		{[allProObj[0].p_purity_real_show]}
I-BRD9 +++

BRD9, pIC50: 7.3

BRD4, pIC50: 5.3

 		{[allProObj[0].p_purity_real_show]}
BI-7273 ++++

BRD7, IC50: 117 nM

BRD9, IC50: 19 nM

 		{[allProObj[0].p_purity_real_show]}
Pelabresib +++

BRD4-BD1, IC50: 39 nM

 		{[allProObj[0].p_purity_real_show]}
ARV-825 +++

BRD4 BD2, Kd: 28 nM

BRD4 BD1, Kd: 90 nM

 		{[allProObj[0].p_purity_real_show]}
Birabresib {[allProObj[0].p_purity_real_show]}
BI 2536 +++

BRD4, Kd: 37 nM

 		c-Myc {[allProObj[0].p_purity_real_show]}
Bromosporine ++

BRD2, IC50: 0.29 μM

BRD9, IC50: 0.122 μM

 		++++

CECR2, IC50: 17 nM

 		{[allProObj[0].p_purity_real_show]}
XMD8-92 ++

BRD4 (1), Kd: 170 nM

 		{[allProObj[0].p_purity_real_show]}
Mivebresib ✔ {[allProObj[0].p_purity_real_show]}
BI-9564 ++++

BRD9, Kd: 5.9 nM

BRD7, Kd: 73 nM

 		++

CECR2, Kd: 77 nM

 		{[allProObj[0].p_purity_real_show]}
AZD5153 6-Hydroxy-2-naphthoic acid ++++

FL-BRD4, IC50: 5 nM

 		{[allProObj[0].p_purity_real_show]}
PLX51107 ++++

BRD4 BD2, Kd: 1.7 nM

BRD3 BD1, Kd: 2.1 nM

 		{[allProObj[0].p_purity_real_show]}
FL-411 +

BRD4(1), IC50: 0.43 μM

 		{[allProObj[0].p_purity_real_show]}
ABBV-744 ✔ {[allProObj[0].p_purity_real_show]}
dBET6 ++++

BRD4, IC50: 14 nM

 		{[allProObj[0].p_purity_real_show]}
dBET1 ++++

BRD4, IC50: 20 nM

 		{[allProObj[0].p_purity_real_show]}
MZ1 ++++

Brd3(BD2), Kd: 13 nM

Brd2(BD2), Kd: 62 nM

 		{[allProObj[0].p_purity_real_show]}
dBET57 +

BRD4BD1, DC50: 500 nM

 		{[allProObj[0].p_purity_real_show]}
SF2523 +

BRD4, IC50: 241 nM

 		DNA-PK {[allProObj[0].p_purity_real_show]}
INCB054329 ++++

BRD3-BD1, IC50: 9 nM

BRD4-BD1, IC50: 119 nM

 		{[allProObj[0].p_purity_real_show]}
INCB-057643 ✔ {[allProObj[0].p_purity_real_show]}
(E/Z)-ZL0420 +++

BRD4 BD1, IC50: 27 nM

BRD4 BD2, IC50: 32 nM

 		{[allProObj[0].p_purity_real_show]}
BMS-986158 ✔ {[allProObj[0].p_purity_real_show]}
BRD4 Inhibitor-10 ++++

BRD4-BD2, IC50: 41 nM

BRD4-BD1, IC50: 5 nM

 		{[allProObj[0].p_purity_real_show]}
A1874 ✔ {[allProObj[0].p_purity_real_show]}
Y06036 ++

BRD4 (1), Kd: 82 nM

 		{[allProObj[0].p_purity_real_show]}
Alobresib ✔ NF-κB {[allProObj[0].p_purity_real_show]}
ODM-207 ✔ {[allProObj[0].p_purity_real_show]}
GSK778 +++

BRD2-BD1, IC50: 75nM

BRD4-BD1, IC50: 143 nM

 		{[allProObj[0].p_purity_real_show]}
SRX3207 +

BRD41, IC50: 3070 nM

BRD42, IC50: 3070 nM

 		Syk {[allProObj[0].p_purity_real_show]}
GSK046 +++

BRD4BD2, IC50: 214 nM

BRD3BD2, IC50: 98 nM

 		{[allProObj[0].p_purity_real_show]}
GSK620 ✔ {[allProObj[0].p_purity_real_show]}
Thalidomide-NH-C4-NH-Boc ✔ {[allProObj[0].p_purity_real_show]}
Trotabresib ✔ {[allProObj[0].p_purity_real_show]}
NHWD-870 ✔ {[allProObj[0].p_purity_real_show]}
CFT8634 ++++

BRD9, DC50: 3 nM

 		{[allProObj[0].p_purity_real_show]}
GSK2801 ++

BAZ2B, Kd: 136 nM

BAZ2A, Kd: 257 nM

 		{[allProObj[0].p_purity_real_show]}
KG-501 ✔ {[allProObj[0].p_purity_real_show]}
UNC 669 +

L3MBTL4, IC50: 6 μM

L3MBTL3, IC50: 35 μM

 		{[allProObj[0].p_purity_real_show]}
PFI-3 +++

SMARCA4, Kd: 55 nM

SMARCA2A, Kd: 72 nM

 		{[allProObj[0].p_purity_real_show]}
UNC1215 +++

L3MBTL3, IC50: 120 nM

L3MBTL3- D274A, IC50: 3.5 μM

 		{[allProObj[0].p_purity_real_show]}
EED226 ++

EED, Kd: 82 nM

PRC2, Kd: 114 nM

 		{[allProObj[0].p_purity_real_show]}
BRD9539 ✔ {[allProObj[0].p_purity_real_show]}
UNC926 +

L3MBTL1, Kd: 3.9 μM

 		{[allProObj[0].p_purity_real_show]}
666-15 ++

CREB, IC50: 81 nM

 		{[allProObj[0].p_purity_real_show]}
UNC6852 +

EED, IC50: 247 nM

 		{[allProObj[0].p_purity_real_show]}
BAZ1A-IN-1 +

BAZ1A, Kd: 0.52 μM

 		{[allProObj[0].p_purity_real_show]}
PFI-4 ++

BRPF1, IC50: 80 nM

BRPF2, IC50: 7.9 μM

 		{[allProObj[0].p_purity_real_show]}
OF-1 ++

BRPF2, Kd: 500 nM

BRPF1B, Kd: 100 nM

 		{[allProObj[0].p_purity_real_show]}
GSK-5959 ++

BRPF3, pIC50: 7.1

BRPF2, pIC50: 5.2

 		{[allProObj[0].p_purity_real_show]}
GSK6853 ++++

BRPF1, pIC50: 8.1

 		{[allProObj[0].p_purity_real_show]}
NI-42 ++++

BRPF1, IC50: 48 nM

BRPF3, IC50: 260 nM

 		{[allProObj[0].p_purity_real_show]}
E-7386 +++

CBP/beta-catenin, IC50: 0.0484 μM

 		{[allProObj[0].p_purity_real_show]}
I-CBP112 ++

p300, Kd: 167 nM

CBP, Kd: 151 nM

 		{[allProObj[0].p_purity_real_show]}
Histone Acetyltransferase Inhibitor II +

p300, IC50: 5 μM

 		{[allProObj[0].p_purity_real_show]}
C646 +

p300/CBP, Ki: 400 nM

 		{[allProObj[0].p_purity_real_show]}
Anacardic Acid +

p300/CBP, IC50: 8.5 μM

PCAF, IC50: 5 μM

 		{[allProObj[0].p_purity_real_show]}
SGC-CBP30 ++++

CREBBP, IC50: 21 nM

EP300, IC50: 38 nM

 		{[allProObj[0].p_purity_real_show]}
Nordihydroguaiaretic acid ✔ HER2,IGF-1R {[allProObj[0].p_purity_real_show]}
Curcumin +

p300, IC50: ~25 μM

 		Nrf2,Ferroptosis,NF-κB {[allProObj[0].p_purity_real_show]}
PF-CBP1 HCl ++

CREBBP, IC50: 125nM

p300/CBP, IC50: 363nM

 		{[allProObj[0].p_purity_real_show]}
CPI-637 +++

CBP, IC50: 0.03 μM

EP300, IC50: 0.051 μM

 		{[allProObj[0].p_purity_real_show]}
Foscenvivint ✔ β-catenin {[allProObj[0].p_purity_real_show]}
A-485 ++

p300 HAT, IC50: 0.06 μM

 		{[allProObj[0].p_purity_real_show]}
GNE-781 +

BRD4(1), IC50: 5100 nM

 		++++

CBP, IC50: 0.94 nM

 		{[allProObj[0].p_purity_real_show]}
NEO2734 +++

BET, IC50: <30 nM

 		+++

p300/CBP, IC50: <30 nM

 		{[allProObj[0].p_purity_real_show]}
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 ↓ 其他靶点 纯度
BRD4770 ✔ {[allProObj[0].p_purity_real_show]}
UNC1999 +++

EZH1, IC50: 45 nM

EZH2, IC50: 2 nM

 		{[allProObj[0].p_purity_real_show]}
EPZ005687 ++

EZH2, Ki: 24 nM

 		{[allProObj[0].p_purity_real_show]}
EPZ015666 +++

PRMT5, Ki: 5 nM

 		{[allProObj[0].p_purity_real_show]}
3-Deazaneplanocin A HCl ++++

S-adenosylhomocysteine hydrolase, Ki: 50 pM

 		{[allProObj[0].p_purity_real_show]}
EPZ6438 +++

EZH2, Ki: 2.5 nM

EZH2, IC50: 11 nM

 		{[allProObj[0].p_purity_real_show]}
GSK126 ++

EZH2, IC50: 9.9 nM

 		{[allProObj[0].p_purity_real_show]}
MI-3 +

Menin-MLL, IC50: 648 nM

 		{[allProObj[0].p_purity_real_show]}
MM-102 ++

MLL1, IC50: 0.4 μM

 		{[allProObj[0].p_purity_real_show]}
EI1 ++

Ezh2 (wild-type), IC50: 15 nM

EZH2 (Y641F), IC50: 13 nM

 		{[allProObj[0].p_purity_real_show]}
SGC0946 ++++

DOT1L, IC50: 0.3 nM

 		{[allProObj[0].p_purity_real_show]}
PFI-2 HCl ++++

SETD7, Ki: 0.33 nM

SETD7, IC50: 2 nM

 		{[allProObj[0].p_purity_real_show]}
Pinometostat ++++

DOT1L, Ki: 80 pM

 		{[allProObj[0].p_purity_real_show]}
EPZ004777 +++

DOT1L, IC50: 0.4 nM

 		{[allProObj[0].p_purity_real_show]}
Entacapone ++

COMT, IC50: 151 nM

 		{[allProObj[0].p_purity_real_show]}
UNC0379 +

SETD8, IC50: 7.9 μM

 		{[allProObj[0].p_purity_real_show]}
Menin-MLL inhibitor MI-2 +

Menin-MLL, IC50: 446 nM

 		{[allProObj[0].p_purity_real_show]}
GSK343 +++

EZH1, IC50: 240 nM

EZH2, IC50: 4 nM

 		{[allProObj[0].p_purity_real_show]}
BIX-01294 3HCl +

G9a, IC50: 2.7 μM

 		{[allProObj[0].p_purity_real_show]}
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。

GSK343 生物活性

靶点

  • Histone Methyltransferase

    EZH1, IC50:240 nM

    EZH2, IC50:4 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. GSK343 is a highly selective EZH2 inhibitor with Kiapp value of 1.2 nM and IC50 value of 174 nM (measured by enzymatic activity in HCC1806 cells), 60-fold more selective to EZH1 and 1000-fold more selective to other methyltransferases tested. Incubation with GSK343 for 72 h led to reduction of H3K27me3 in a dose-dependent manner in HCC1806 breast cancer cells with IC50 value of 174 nM. Greater than 90% inhibition of global H3K27me3 was achieved at higher concentration>1000 nM. Inhibition of EZH2 by GSK343 affected the breast and prostate cancer cell lines tested in 6-day proliferation assay. Among these cells, the prostate cancer cell line LNCaP showed the most sensitive to EZH2 inhibition, with growth IC50 values of 2.9 μM, approximately 20-fold above the IC50 on H3K27me3[1]. GSK343 on concentration of 5 μM can suppress proliferation, migration and invasion and induces G0/G1 arrest in U87 and LN229 glioma cells. Treatment with GSK343 can lead to downregulation of H3K27me3 (5 μM, 4-24 h) in a time-dependent manner and cause a reduction in EZH2, EED and SUZ12 protein levels in U87 and LN229 cells (5 μM, for 48 h). Meanwhile, the expression of the classical EZH2 target genes, including E-cadherin, PTEN and p21, increase in U87 and LN229 cells (5 or 7.5 μM, for 48 h). GSK343 reverses mesenchymal transition in glioma cells and attenuates the stemness of glioma stem cells. Intraperitoneal injections of GSK343 (10 mg/kg) every other day for 28 days inhibited glioma tumorigenesis and invasiveness in nude mice intracranially xenotransplanted with luciferase-expressing U87 glioma cells. Prolonged survival period can be observed on day 45[2].
作用机制 GSK343 is the SAM-competitive inhibitor of PRC2.[1]

GSK343 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
2D10 0.25-2.0 μM Function Assay 96 h reduces total cellular trimethylated H3K27 in a time- and dose-dependent manner 26041287
A549 0-20 μM Growth Inhibition Assay 72 h shows cytotoxicity in a dose-dependent manner 25203626
A549 10 μM Function Assay 24 h induces autophagy 25203626
HepG2 0-20 μM Growth Inhibition Assay 72 h shows cytotoxicity in a dose-dependent manner 25203626

GSK343 动物研究

Dose Nude Mice (i.p.): 20 mg/kg[2], 5 mg/kg[3]
Administration i.p.

GSK343 参考文献

[1]Verma SK, Tian X, et al. Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2. ACS Med Chem Lett. 2012 Oct 19;3(12):1091-6.

[2]Yu T, Wang Y, et al. The EZH2 inhibitor GSK343 suppresses cancer stem-like phenotypes and reverses mesenchymal transition in glioma cells. Oncotarget. 2017 Sep 27;8(58):98348-98359.

GSK343 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.85mL

0.37mL

0.18mL

9.23mL

1.85mL

0.92mL

18.46mL

3.69mL

1.85mL

GSK343 技术信息

CAS号1346704-33-3
分子式C31H39N7O2
分子量 541.687
别名
运输蓝冰
存储条件

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度

DMSO: 15 mg/mL(27.69 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
动物实验配方

Tags: GSK343 | 1346704-33-3 | GSK 343 | GSK-343 | EZH2 Inhibitor | Epigenetics | Autophagy | Histone Methyltransferase | Autophagy | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | GSK343 纯度/质量文件 | GSK343 亚型比较 | GSK343 生物活性 | GSK343 细胞研究 | GSK343 动物研究 | GSK343 参考文献 | GSK343 实验方案 | GSK343 技术信息

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