EED226 | MAK683 | PRC2 Inhibitor | AmBeed-信号通路专用抑制剂

EED226 {[allProObj[0].p_purity_real_show]}

货号：A256458 同义名： MAK683

EED226是一种有效且选择性的 PRC2 抑制剂，直接与 EED 的 H3K27me3 结合口袋结合。

EED226 化学结构
CAS号：2083627-02-3

EED226 3D分子结构
CAS号：2083627-02-3

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表观遗传阅读框亚型比较

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	+++ BRD9, pIC50: 7.3 BRD4, pIC50: 5.3						99%+
BI-7273	++++ BRD9, IC50: 19 nM BRD7, IC50: 117 nM						97%
Pelabresib	+++ BRD4-BD1, IC50: 39 nM						98%
ARV-825	+++ BRD4 BD1, Kd: 90 nM BRD4 BD2, Kd: 28 nM						99%+
Birabresib							99%+
BI 2536	+++ BRD4, Kd: 37 nM					c-Myc	99%+
Bromosporine	++ BRD9, IC50: 0.122 μM BRD2, IC50: 0.29 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	++++ BRD3 BD1, Kd: 2.1 nM BRD4 BD2, Kd: 1.7 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	++++ Brd3(BD2), Kd: 13 nM Brd2(BD2), Kd: 62 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 BD2, IC50: 32 nM BRD4 BD1, IC50: 27 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	95%
ODM-207	✔						98%
GSK778	+++ BRD2-BD1, IC50: 75nM BRD4-BD1, IC50: 143 nM						97%
SRX3207	+ BRD42, IC50: 3070 nM BRD41, IC50: 3070 nM					Syk	98%
GSK046	+++ BRD3_BD2, IC50: 98 nM BRD4_BD2, IC50: 214 nM						98%
GSK620	✔						97%
Trotabresib	✔						99%
NHWD-870	✔						98%
CFT8634	++++ BRD9, DC50: 3 nM						98%
GSK2801		++ BAZ2A, Kd: 257 nM BAZ2B, Kd: 136 nM					99%+
KG-501		✔					99%+
UNC 669		+ L3MBTL4, IC50: 6 μM L3MBTL3, IC50: 35 μM					99%
PFI-3		+++ SMARCA2A, Kd: 72 nM SMARCA4, Kd: 55 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			++ BRPF2, pIC50: 5.2 BRPF3, pIC50: 7.1				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					++ CBP, Kd: 151 nM p300, Kd: 167 nM		98+%
Histone Acetyltransferase Inhibitor II					+ p300, IC50: 5 μM		98%
C646					+ p300/CBP, Ki: 400 nM		99%+
Anacardic Acid					+ p300/CBP, IC50: 8.5 μM PCAF, IC50: 5 μM		99%+
SGC-CBP30					++++ CREBBP, IC50: 21 nM EP300, IC50: 38 nM		99%+
Nordihydroguaiaretic acid					✔	HER2,IGF-1R	99%+
Curcumin					+ p300, IC50: ~25 μM	Ferroptosis,NF-κB,Nrf2	98%
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。

EED226 生物活性

靶点

bromodomain

PRC2, Kd:114 nM

EED, Kd:82 nM

描述

EED226 functions as an inhibitor of the PRC2, targeting the K27me3-pocket of the EED protein. It has demonstrated significant antitumor efficacy in a xenograft mouse model^[1]. EED226 stands out as a highly potent, efficient, and selective inhibitor of both EZH2 and EZH1, having been tested against a wide spectrum of epigenetic and non-epigenetic targets. It effectively diminishes the global H3K27Me3 mark in cells and exhibits selective cytotoxicity in cells with a heterozygous Y641N mutation. The permeability of EED226 is moderate, with measurements in Caco-2 cells showing an A→B permeability of 3.0x10^-6 cm/s, and an efflux ratio of 7.6^[2]. In vitro enzymatic assays reveal that EED226 is an inhibitor of PRC2, with an IC50 of 23.4 nM when using the H3K27me0 peptide as a substrate. Additionally, when the assay is conducted with mononucleosomes as the substrate and the stimulatory H3K27me3 present at 1× Kact (1.0 μM), EED226 exhibits an IC50 of 53.5 nM^[3].

EED226 细胞实验

Cell Line HeLa cells DB cells Female Germline Stem Cells (FGSCs) Murine renal tubular epithelial cells (mRTECs) KARPAS422 SK-HEP-1 cells PLC/PRF/5 cells	Concentration	Treated Time	Description	References
HeLa cells	5 µM	24 hours	To evaluate the degradation effect of UNC6852 on PRC2 components, results showed that UNC6852 significantly degraded EED and EZH2.	Cell Chem Biol. 2020 Jan 16;27(1):47-56.e15.
DB cells	10 µM	24 hours	To evaluate the degradation effect of UNC6852 on PRC2 components, results showed that UNC6852 significantly degraded EED, EZH2, and SUZ12.	Cell Chem Biol. 2020 Jan 16;27(1):47-56.e15.
Female Germline Stem Cells (FGSCs)	1, 5, 10 µM	24 hours and 48 hours	EED226 significantly increased the survival rate of FGSCs by decreasing the enrichment of H3K27me3 on the Oct4 promoter and exon, enhancing OCT4 expression, and inhibiting P53 and P63 expression.	Open Biol. 2023 Jan;13(1):220211.
Murine renal tubular epithelial cells (mRTECs)	10 µM	48 hours	To investigate the effect of EED226 on cisplatin-induced apoptosis in mRTECs, the results showed that EED226 significantly inhibited cisplatin-induced apoptosis.	J Cell Mol Med. 2022 Jul;26(14):4061-4075.
KARPAS422	0.18 µM	7 days	To evaluate the effect of EED inhibitors on cell growth; EED226 has an IC50 value of 0.18 μM in inhibition of KARPAS422 cell growth	J Med Chem. 2020 Jul 9;63(13):7252-7267.
SK-HEP-1 cells	5 µM	72 hours	EED226 treatment increases CXCL10 expression	Proc Natl Acad Sci U S A. 2021 Jul 27;118(30):e2102718118.
PLC/PRF/5 cells	5 µM	72 hours	EED226 treatment increases CXCL10 expression	Proc Natl Acad Sci U S A. 2021 Jul 27;118(30):e2102718118.

Cell Line

HeLa cells DB cells Female Germline Stem Cells (FGSCs) Murine renal tubular epithelial cells (mRTECs) KARPAS422 SK-HEP-1 cells PLC/PRF/5 cells

Concentration

Treated Time

Description

References

HeLa cells

5 µM

24 hours

To evaluate the degradation effect of UNC6852 on PRC2 components, results showed that UNC6852 significantly degraded EED and EZH2.

Cell Chem Biol. 2020 Jan 16;27(1):47-56.e15.

DB cells

10 µM

24 hours

To evaluate the degradation effect of UNC6852 on PRC2 components, results showed that UNC6852 significantly degraded EED, EZH2, and SUZ12.

Cell Chem Biol. 2020 Jan 16;27(1):47-56.e15.

Female Germline Stem Cells (FGSCs)

1, 5, 10 µM

24 hours and 48 hours

EED226 significantly increased the survival rate of FGSCs by decreasing the enrichment of H3K27me3 on the Oct4 promoter and exon, enhancing OCT4 expression, and inhibiting P53 and P63 expression.

Open Biol. 2023 Jan;13(1):220211.

Murine renal tubular epithelial cells (mRTECs)

10 µM

48 hours

To investigate the effect of EED226 on cisplatin-induced apoptosis in mRTECs, the results showed that EED226 significantly inhibited cisplatin-induced apoptosis.

J Cell Mol Med. 2022 Jul;26(14):4061-4075.

KARPAS422

0.18 µM

7 days

To evaluate the effect of EED inhibitors on cell growth; EED226 has an IC50 value of 0.18 μM in inhibition of KARPAS422 cell growth

J Med Chem. 2020 Jul 9;63(13):7252-7267.

SK-HEP-1 cells

5 µM

72 hours

EED226 treatment increases CXCL10 expression

Proc Natl Acad Sci U S A. 2021 Jul 27;118(30):e2102718118.

PLC/PRF/5 cells

5 µM

72 hours

EED226 treatment increases CXCL10 expression

Proc Natl Acad Sci U S A. 2021 Jul 27;118(30):e2102718118.

EED226 动物实验

Species Mice Mice C57BL/6J mice Balb/c nude mice	Animal Model Hepatic tumor model KARPAS422 human B cell lymphoma xenograft model Cisplatin-induced acute kidney injury model G401 xenograft tumor model	Administration	Dosage	Frequency	Description	References
Mice	Hepatic tumor model	Intraperitoneal injection	20 mg/kg	5 days a week for 28 days	EZH2 inhibitor GSK343 induces tumor suppression through reexpression of CXCL10	Proc Natl Acad Sci U S A. 2021 Jul 27;118(30):e2102718118.
Mice	KARPAS422 human B cell lymphoma xenograft model	Oral gavage	300 mg/kg	Twice a day	To determine the efficacy of EED226 in tumor regression; achieved complete KARPAS422 cell tumor regression.	J Med Chem. 2020 Jul 9;63(13):7252-7267.
C57BL/6J mice	Cisplatin-induced acute kidney injury model	Intragastric administration	40 mg/kg	Twice a day for 48 hours	To investigate the protective effect of EED226 on cisplatin-induced acute kidney injury, the results showed that EED226 significantly improved renal function, attenuated renal tubular cell apoptosis and inflammatory response.	J Cell Mol Med. 2022 Jul;26(14):4061-4075.
Balb/c nude mice	G401 xenograft tumor model	Oral	100 mg/kg	Once daily for 21 days	Evaluate the antitumor effect of MAK683 in vivo, results showed MAK683 significantly inhibited tumor growth and induced adipocyte differentiation	J Biol Chem. 2024 Oct;300(10):107765

Species

Mice Mice C57BL/6J mice Balb/c nude mice

Animal Model

Hepatic tumor model KARPAS422 human B cell lymphoma xenograft model Cisplatin-induced acute kidney injury model G401 xenograft tumor model

Administration

Dosage

Frequency

Description

References

Mice

Hepatic tumor model

Intraperitoneal injection

20 mg/kg

5 days a week for 28 days

EZH2 inhibitor GSK343 induces tumor suppression through reexpression of CXCL10

Proc Natl Acad Sci U S A. 2021 Jul 27;118(30):e2102718118.

Mice

KARPAS422 human B cell lymphoma xenograft model

Oral gavage

300 mg/kg

Twice a day

To determine the efficacy of EED226 in tumor regression; achieved complete KARPAS422 cell tumor regression.

J Med Chem. 2020 Jul 9;63(13):7252-7267.

C57BL/6J mice

Cisplatin-induced acute kidney injury model

Intragastric administration

40 mg/kg

Twice a day for 48 hours

To investigate the protective effect of EED226 on cisplatin-induced acute kidney injury, the results showed that EED226 significantly improved renal function, attenuated renal tubular cell apoptosis and inflammatory response.

J Cell Mol Med. 2022 Jul;26(14):4061-4075.

Balb/c nude mice

G401 xenograft tumor model

Oral

100 mg/kg

Once daily for 21 days

Evaluate the antitumor effect of MAK683 in vivo, results showed MAK683 significantly inhibited tumor growth and induced adipocyte differentiation

J Biol Chem. 2024 Oct;300(10):107765

EED226 动物研究

Animal study

EED226 prompts significant and lasting tumor regression in the EZH2MUT preclinical DLBCL model. In CD-1 mice, a 14-day regimen of EED226 at a dose of 300 mg/kg twice daily is well-tolerated without noticeable side effects. EED226 exhibits minimal in vivo clearance and near-complete oral bioavailability. Additionally, EED226 is characterized by a low distribution volume (0.8 L/kg), a reasonable terminal half-life of 2.2 hours, and moderate binding to plasma proteins^[2].

EED226 参考文献

EED226 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.71mL

0.54mL

0.27mL

13.54mL

2.71mL

1.35mL

27.07mL

5.41mL

2.71mL

EED226 技术信息

CAS号	2083627-02-3
分子式	C₁₇H₁₅N₅O₃S
分子量	369.4
SMILES Code	O=S(C1=CC=C(C2=CN=C(NCC3=CC=CO3)N4C2=NN=C4)C=C1)(C)=O
MDL No.	MFCD30738018

别名	MAK683
运输	蓝冰
InChI Key	DYIRSNMPIZZNBK-UHFFFAOYSA-N
Pubchem ID	123132228

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, store in freezer, under -20°C

溶解方案

细胞实验：

DMSO: 120 mg/mL(324.85 mM)，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

方案三

配制的工作液建议现用现配，短期内尽快用完。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

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