EPZ6438 | Histone Methyltransferase | Epigenetic Reader Domain

Tazemetostat {[allProObj[0].p_purity_real_show]}

货号：A223202 同义名： EPZ-6438; E7438

EPZ6438（EPZ-6438）是一种高效且选择性的EZH2抑制剂，口服可用。它抑制含有野生型EZH2的人类多梳抑制复合体2（PRC2）的活性，Ki值为2.5 nM。在肽和核小体测定中，他泽司他（EPZ-6438）抑制EZH2的IC50值分别为11和16 nM。它还以4 nM的IC50抑制大鼠EZH2，并以392 nM的IC50抑制EZH1。

Tazemetostat 化学结构
CAS号：1403254-99-8

Tazemetostat 3D分子结构
CAS号：1403254-99-8

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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	+++ BRD2, IC50: 31 nM BRD4, IC50: 22 nM						99%+
PFI-1	++ BRD2, IC50: 98 nM BRD4, IC50: 0.22 μM						98%
Apabetalone	+ BD2, IC50: 0.51 μM						99%
(+)-JQ1	+++ BRD4 (2), IC50: 33 nM BRD4 (1), IC50: 77 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						97%
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	++++ BRD9, Kd: 5.9 nM BRD7, Kd: 73 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 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		+ L3MBTL3, IC50: 35 μM L3MBTL4, IC50: 6 μM					99%
PFI-3		+++ SMARCA2A, Kd: 72 nM SMARCA4, Kd: 55 nM					99%+
UNC1215		+++ L3MBTL3, IC50: 120 nM L3MBTL3- D274A, IC50: 3.5 μM					99%+
EED226		++ EED, Kd: 82 nM PRC2, Kd: 114 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			++ BRPF2, IC50: 7.9 μM BRPF1, IC50: 80 nM				99%+
OF-1			++ BRPF1B, Kd: 100 nM BRPF2, Kd: 500 nM				99%+
GSK-5959			++ BRPF3, pIC50: 7.1 BRPF2, pIC50: 5.2				99%
GSK6853			++++ BRPF1, pIC50: 8.1				99%+
NI-42			++++ BRPF3, IC50: 260 nM BRPF1, IC50: 48 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					++++ EP300, IC50: 38 nM CREBBP, IC50: 21 nM		99%+
Nordihydroguaiaretic acid					✔	IGF-1R,HER2	99%+
Curcumin					+ p300, IC50: ~25 μM	Ferroptosis,NF-κB,Nrf2	98%
CPI-637					+++ EP300, IC50: 0.051 μM CBP, IC50: 0.03 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	96%
SGC0946	++++ DOT1L, IC50: 0.3 nM	99%+
PFI-2 HCl	++++ SETD7, Ki: 0.33 nM SETD7, IC50: 2 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。

Tazemetostat 生物活性

靶点

Histone Methyltransferase

EZH2, IC50:11 nM

EZH2, Ki:2.5 nM

描述

Tazemetostat (EPZ-6438) is a potent, selective, and orally available EZH2 inhibitor. It inhibits human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM and inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat also inhibits rat EZH2 with an IC50 of 4 nM and inhibits EZH1 with an IC50 of 392 nM. It induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells ^[1].

体内研究

Tazemetostat (EPZ-6438; 250 or 500 mg/kg twice daily for 21-28 days) effectively eradicates fast-growing G401 tumors ^[1].

体外研究

Tazemetostat (EPZ-6438) inhibits proliferation of multiple wild-type and mutant lymphoma cell lines with IC50s ranging from 0.49 nM to 7.6 μM ^[1].

作用机制

EPZ-6438 inhibits EZH2 in a manner competitive with the substrate S-adenosylmethionine (SAM) binding to EZH2.

Tazemetostat 细胞实验

Cell Line LNCaP-EnzR cells LNCaP cells C4-2B cells LNCaP cells C4-2B cells LNCaP cells C4-2B cells TNBC cell lines G401 cells DB pancreatic ductal epithelial cells IDH1R132H and IDH1 wild-type mouse glioma cells DLBCL cell lines (SUDHL-4, DB, SUDHL-6, WSU-DLCL2, SUDHL-10, Karpas 422) EZH2 wild-type DLBCL cell lines (RI-1, U9-293) SUDHL-4 SUDHL-6 WaGa	Concentration	Treated Time	Description	References
LNCaP-EnzR cells	1 μM	5 days	To evaluate the effect of EPZ-6438 on enzalutamide-resistant cells, results showed that EPZ-6438 could enhance the sensitivity to enzalutamide	Cancer Res. 2018 Oct 15;78(20):5731-5740.
LNCaP cells	1 μM	5 days	To evaluate the synergistic effect of EPZ-6438 combined with enzalutamide, results showed that combination treatment significantly inhibited cell proliferation	Cancer Res. 2018 Oct 15;78(20):5731-5740.
C4-2B cells	1 μM	5 days	To evaluate the effect of EZH2 inhibitors on enzalutamide sensitivity, results showed that EZH2 inhibitors significantly enhanced the inhibitory effect of enzalutamide on cell proliferation	Cancer Res. 2018 Oct 15;78(20):5731-5740.
LNCaP cells	1 μM	5 days	Validating the synergistic antiproliferative effect of EPZ-6438 and enzalutamide	Cancer Res. 2018 Oct 15;78(20):5731-5740.
C4-2B cells	1 μM	5 days	Screening EZH2 inhibitors to enhance the inhibitory effect of enzalutamide on cell proliferation	Cancer Res. 2018 Oct 15;78(20):5731-5740.
LNCaP cells	1 μM	5 days	Validate the synergistic antiproliferative effects of EPZ-6438 and enzalutamide co-treatment.	Cancer Res. 2018 Oct 15;78(20):5731-5740.
C4-2B cells	1 μM	5 days	Screening epigenetic inhibitors, EZH2 inhibitors significantly enhanced the inhibitory effect of enzalutamide on cell proliferation.	Cancer Res. 2018 Oct 15;78(20):5731-5740.
TNBC cell lines	5 μM	5 days pretreatment followed by 4 days of combination treatment	To evaluate the cytotoxic effects of MAK683 in combination with AKT inhibitors on TNBC cells, showing that 60% of cell lines were highly sensitive to this combination, resulting in substantial cell depletion	Nature. 2024 Nov;635(8039):755-763.
G401 cells	10 μM	11 days	Evaluate the effect of RB1 loss on TAZ resistance	Cancer Discov. 2024 Jun 3;14(6):965-981.
DB	312.5-5000 nM	48 h	Tazemetostat upregulated HLA I and HLA-A*02 cell surface expression.	Blood Adv. 2022 Jul 26;6(14):4107-4121.
pancreatic ductal epithelial cells	1 μM	48 h	To evaluate the regenerative capacity of Tazemetostat on pancreatic ductal epithelial cells, results showed that Tazemetostat restored the expression of β-cell-related genes and promoted insulin secretion.	Signal Transduct Target Ther. 2024 Jan 1;9(1):2.
IDH1R132H and IDH1 wild-type mouse glioma cells	5 µM	48 h	Tazemetostat significantly reduced H3K27me3 levels in both IDH1R132H and wild-type cells and significantly increased H3K27ac levels.	Cells. 2024 Jan 25;13(3):219.
DLBCL cell lines (SUDHL-4, DB, SUDHL-6, WSU-DLCL2, SUDHL-10, Karpas 422)	1 μM	48 h	To evaluate the effect of Tazemetostat on HLA I and HLA-A*02 expression in DLBCL cell lines, results showed that Tazemetostat alone or in combination with Decitabine significantly upregulated HLA expression.	Blood Adv. 2022 Jul 26;6(14):4107-4121.
EZH2 wild-type DLBCL cell lines (RI-1, U9-293)	1 μM	48 h	To evaluate the effect of Tazemetostat on HLA expression in EZH2 wild-type DLBCL cell lines, results showed that Tazemetostat had little to no effect on HLA expression in EZH2 wild-type cell lines.	Blood Adv. 2022 Jul 26;6(14):4107-4121.
SUDHL-4	312.5-5000 nM	48 h	Tazemetostat decreases global H3K27me3 with 96 h of drug treatment.	Blood Adv. 2022 Jul 26;6(14):4107-4121.
SUDHL-6	312.5-5000 nM	48 h	Tazemetostat upregulated HLA I and HLA-A*02 cell surface expression.	Blood Adv. 2022 Jul 26;6(14):4107-4121.
WaGa	0.5 μM	12 days	To assess the impact of Tazemetostat on WaGa cell viability, observing significant reduction in cell viability	J Invest Dermatol. 2022 Oct;142(10):2783-2792.e15.

Cell Line

Concentration

Treated Time

Description

References

LNCaP-EnzR cells

1 μM

5 days

To evaluate the effect of EPZ-6438 on enzalutamide-resistant cells, results showed that EPZ-6438 could enhance the sensitivity to enzalutamide