MZ1 | PROTAC BRD4 Degrader | AmBeed-信号通路专用抑制剂

MZ1 {[allProObj[0].p_purity_real_show]}

货号：A732871

MZ1是一种高效、选择性的PROTAC分子，能够靶向BRD4和VHL E3泛素连接酶，将BRD4蛋白降解。MZ1通过诱导BRD4降解，在癌症等表观遗传疾病的研究中显示出潜力。

MZ1 化学结构
CAS号：1797406-69-9

MZ1 3D分子结构
CAS号：1797406-69-9

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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	+++ 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 BD1, Kd: 90 nM BRD4 BD2, Kd: 28 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	++++ 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	++++ 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	++++ BRD4-BD1, IC50: 119 nM BRD3-BD1, IC50: 9 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-BD1, IC50: 5 nM BRD4-BD2, IC50: 41 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	+++ BRD4_BD2, IC50: 214 nM BRD3_BD2, IC50: 98 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		++ 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			++ BRPF1B, Kd: 100 nM BRPF2, Kd: 500 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					++ 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					+ 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,Nrf2,NF-κB	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。

MZ1 生物活性

靶点

BET

Brd2(BD2), Kd:62 nM

Brd3(BD2), Kd:13 nM

描述

体内研究

MZ1 给药导致异种移植模型中的肿瘤大小显着减小，毒性降低。具体来说，从肿瘤接种后第3日开始，药物治疗组每2日腹腔注射MZ1，剂量为12.5mg/kg。MZ1处理显着降低了BRD4的蛋白质水平，并且还降低了肿瘤组织中增殖标志物PCNA的蛋白质水平，这表明MZ1在体内能显著抑制GBM的发生和发展。

体外研究

MZ1通过有效降解BRD4，大大减少了GBM细胞的增殖（IC50=0.47-3.68nM）。具体来说，MZ1在相对较低的浓度下能有效抑制GBM细胞系，对U87的IC50值为3.68 μM，对LN229的IC50值为0.89 μM，对A172的IC50值为0.80 μM，对U251的IC50值为0.47 μM。此外，MZ1在诱导GBM细胞中显着的细胞周期停滞和凋亡方面表现出显着的能力。

MZ1 细胞实验

Cell Line HeLa cells MDA-MB-231 MDA-MB-231R HeLa cells LS174t cells MM.1S cells LS174t cells HeLa cells BT549 SKOV3 OVCAR3 SSM2c cells A375 cells MeWo cells KYSE180 22RV1 cells	Concentration	Treated Time	Description	References
HeLa cells	1-3 µM	24 hours	To test the selective degradation of Brd4 by MZ1	Nat Chem Biol. 2017 May;13(5):514-521.
MDA-MB-231	0.4 µM	12, 24, or 48 hours	MZ1 efficiently downregulated the protein expression levels of BRD4 and BRD2.	J Exp Clin Cancer Res. 2019 Aug 30;38(1):383.
MDA-MB-231R	0.4 µM	12, 24, or 48 hours	MZ1 efficiently downregulated the protein expression levels of BRD4 and BRD2.	J Exp Clin Cancer Res. 2019 Aug 30;38(1):383.
HeLa cells	0.1 µM	2 hours	MZ1 treatment resulted in complete loss of BRD4 and a significant stabilization of MYC protein	Proc Natl Acad Sci U S A. 2020 Jun 16;117(24):13457-13467.
LS174t cells	200 nM	2 hours	MZ1 significantly reduced BRD4 signal intensity within 2 hours and caused clustering in the cytoplasm	Neoplasia. 2019 Nov;21(11):1110-1120.
MM.1S cells	100 nM	24 hours	MZ-1 inhibited BMSC- and IL-6-induced MYC mRNA and protein levels but did not affect JUNB expression.	Blood Cancer J. 2024 Aug 19;14(1):138.
LS174t cells	1 µM	24 hours	MZ1 induced complete degradation of BRD4 protein, followed by a reduction in MYC protein expression	Neoplasia. 2019 Nov;21(11):1110-1120.
HeLa cells	25-125 nM	4 hours or 18 hours	To evaluate the degradation effect of macroPROTAC-1 on Brd4, the results showed that macroPROTAC-1 could rapidly and effectively degrade Brd4.	Angew Chem Int Ed Engl. 2020 Jan 20;59(4):1727-1734.
BT549	0.2, 0.4, 1 µM	48 or 96 hours	MZ1 showed significant antiproliferative activity in BT549 cells.	J Exp Clin Cancer Res. 2019 Aug 30;38(1):383.
SKOV3	0.2, 0.4, 1 µM	48 or 96 hours	MZ1 showed significant antiproliferative activity in SKOV3 cells.	J Exp Clin Cancer Res. 2019 Aug 30;38(1):383.
OVCAR3	0.2, 0.4, 1 µM	48 or 96 hours	MZ1 showed significant antiproliferative activity in OVCAR3 cells.	J Exp Clin Cancer Res. 2019 Aug 30;38(1):383.
SSM2c cells	125 nM	72 hours	Combination of MZ1 and MRT-92 significantly inhibited melanoma cell growth and completely abrogated GLI1 expression.	Oncogene. 2021 Jun;40(22):3799-3814.
A375 cells	250 nM	72 hours	Combination of MZ1 and MRT-92 significantly inhibited melanoma cell growth and completely abrogated GLI1 expression.	Oncogene. 2021 Jun;40(22):3799-3814.
MeWo cells	125 nM	72 hours	Combination of MZ1 and MRT-92 significantly inhibited melanoma cell growth and completely abrogated GLI1 expression.	Oncogene. 2021 Jun;40(22):3799-3814.
KYSE180	1 µM	8 hours	After MZ1 treatment, BRDT protein was completely degraded, BRD4 expression was significantly decreased, and BRD2 and BRD3 protein levels were relatively unaffected.	Cell Death Differ. 2021 Jul;28(7):2207-2220.
22RV1 cells	250 nM		To evaluate the degradation effect of macroPROTAC-1 on Brd4 and its impact on Myc levels, the results showed that macroPROTAC-1 could significantly degrade Brd4 and reduce Myc levels.	Angew Chem Int Ed Engl. 2020 Jan 20;59(4):1727-1734.

Cell Line

Concentration

Treated Time

Description

References

HeLa cells

1-3 µM

24 hours

To test the selective degradation of Brd4 by MZ1

Nat Chem Biol. 2017 May;13(5):514-521.

MDA-MB-231

0.4 µM

12, 24, or 48 hours

MZ1 efficiently downregulated the protein expression levels of BRD4 and BRD2.

J Exp Clin Cancer Res. 2019 Aug 30;38(1):383.

MDA-MB-231R

0.4 µM

12, 24, or 48 hours

MZ1 efficiently downregulated the protein expression levels of BRD4 and BRD2.

J Exp Clin Cancer Res. 2019 Aug 30;38(1):383.

HeLa cells

0.1 µM

2 hours

MZ1 treatment resulted in complete loss of BRD4 and a significant stabilization of MYC protein

Proc Natl Acad Sci U S A. 2020 Jun 16;117(24):13457-13467.

LS174t cells

200 nM

2 hours

MZ1 significantly reduced BRD4 signal intensity within 2 hours and caused clustering in the cytoplasm

Neoplasia. 2019 Nov;21(11):1110-1120.

MM.1S cells

100 nM

24 hours

MZ-1 inhibited BMSC- and IL-6-induced MYC mRNA and protein levels but did not affect JUNB expression.

Blood Cancer J. 2024 Aug 19;14(1):138.

LS174t cells

1 µM

24 hours

MZ1 induced complete degradation of BRD4 protein, followed by a reduction in MYC protein expression

Neoplasia. 2019 Nov;21(11):1110-1120.

HeLa cells

25-125 nM

4 hours or 18 hours

To evaluate the degradation effect of macroPROTAC-1 on Brd4, the results showed that macroPROTAC-1 could rapidly and effectively degrade Brd4.

Angew Chem Int Ed Engl. 2020 Jan 20;59(4):1727-1734.

BT549

0.2, 0.4, 1 µM

48 or 96 hours

MZ1 showed significant antiproliferative activity in BT549 cells.

J Exp Clin Cancer Res. 2019 Aug 30;38(1):383.

SKOV3

0.2, 0.4, 1 µM

48 or 96 hours

MZ1 showed significant antiproliferative activity in SKOV3 cells.

J Exp Clin Cancer Res. 2019 Aug 30;38(1):383.

OVCAR3

0.2, 0.4, 1 µM

48 or 96 hours

MZ1 showed significant antiproliferative activity in OVCAR3 cells.

J Exp Clin Cancer Res. 2019 Aug 30;38(1):383.

SSM2c cells

125 nM

72 hours

Combination of MZ1 and MRT-92 significantly inhibited melanoma cell growth and completely abrogated GLI1 expression.

Oncogene. 2021 Jun;40(22):3799-3814.

A375 cells

250 nM

72 hours

Combination of MZ1 and MRT-92 significantly inhibited melanoma cell growth and completely abrogated GLI1 expression.

Oncogene. 2021 Jun;40(22):3799-3814.

MeWo cells

125 nM

72 hours

Combination of MZ1 and MRT-92 significantly inhibited melanoma cell growth and completely abrogated GLI1 expression.

Oncogene. 2021 Jun;40(22):3799-3814.

KYSE180

1 µM

8 hours

After MZ1 treatment, BRDT protein was completely degraded, BRD4 expression was significantly decreased, and BRD2 and BRD3 protein levels were relatively unaffected.

Cell Death Differ. 2021 Jul;28(7):2207-2220.

22RV1 cells

250 nM

To evaluate the degradation effect of macroPROTAC-1 on Brd4 and its impact on Myc levels, the results showed that macroPROTAC-1 could significantly degrade Brd4 and reduce Myc levels.

Angew Chem Int Ed Engl. 2020 Jan 20;59(4):1727-1734.

MZ1 动物实验

Species BALB/c nu/nu mice Athymic Nude mice NOD scid gamma (NSG) mice NOD scid gamma NSG™ mice	Animal Model MDA-MB-231R xenograft model A375 melanoma xenograft model Multiple myeloma xenograft model Multiple myeloma xenograft model	Administration	Dosage	Frequency	Description	References
BALB/c nu/nu mice	MDA-MB-231R xenograft model	Intraperitoneal injection	10 mg/kg	Once daily for two weeks	MZ1 prevented the growth of JQ1-resistant tumors and reduced BRD4 expression levels.	J Exp Clin Cancer Res. 2019 Aug 30;38(1):383.
Athymic Nude mice	A375 melanoma xenograft model	Intraperitoneal injection	100 mg/kg	Once daily for 10 days	Combination of MZ1 and MRT-92 significantly inhibited melanoma growth and completely abrogated GLI1 expression.	Oncogene. 2021 Jun;40(22):3799-3814.
NOD scid gamma (NSG) mice	Multiple myeloma xenograft model	Intraperitoneal injection	5 mg/kg	5 times per week until tumors reached a maximum diameter of 1.5 cm	MZ-1 alone or in combination with doxycycline significantly reduced tumor size and prolonged mouse survival.	Blood Cancer J. 2024 Aug 19;14(1):138.
NOD scid gamma NSG™ mice	Multiple myeloma xenograft model	Intraperitoneal injection	5 mg/kg	5 times per week until tumors reached a maximum diameter of 1.5 cm	MZ-1 significantly reduced tumor size and prolonged mouse survival, and its combination with doxycycline further enhanced the anti-tumor effect.	Blood Cancer J. 2024 Aug 19;14(1):138.

Species

BALB/c nu/nu mice Athymic Nude mice NOD scid gamma (NSG) mice NOD scid gamma NSG™ mice

Animal Model

MDA-MB-231R xenograft model A375 melanoma xenograft model Multiple myeloma xenograft model Multiple myeloma xenograft model

Administration

Dosage

Frequency

Description

References

BALB/c nu/nu mice

MDA-MB-231R xenograft model

Intraperitoneal injection

10 mg/kg

Once daily for two weeks

MZ1 prevented the growth of JQ1-resistant tumors and reduced BRD4 expression levels.

J Exp Clin Cancer Res. 2019 Aug 30;38(1):383.

Athymic Nude mice

A375 melanoma xenograft model

Intraperitoneal injection

100 mg/kg

Once daily for 10 days

Combination of MZ1 and MRT-92 significantly inhibited melanoma growth and completely abrogated GLI1 expression.

Oncogene. 2021 Jun;40(22):3799-3814.

NOD scid gamma (NSG) mice

Multiple myeloma xenograft model

Intraperitoneal injection

5 mg/kg

5 times per week until tumors reached a maximum diameter of 1.5 cm

MZ-1 alone or in combination with doxycycline significantly reduced tumor size and prolonged mouse survival.

Blood Cancer J. 2024 Aug 19;14(1):138.

NOD scid gamma NSG™ mice

Multiple myeloma xenograft model

Intraperitoneal injection

5 mg/kg

5 times per week until tumors reached a maximum diameter of 1.5 cm

MZ-1 significantly reduced tumor size and prolonged mouse survival, and its combination with doxycycline further enhanced the anti-tumor effect.

Blood Cancer J. 2024 Aug 19;14(1):138.

MZ1 动物研究

Dose

Mice: 10 mg/kg^[2] (i.p.)

Administration

i.p.

MZ1 参考文献

MZ1 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.00mL

0.20mL

0.10mL

4.99mL

1.00mL

0.50mL

9.97mL

1.99mL

1.00mL

MZ1 技术信息

CAS号	1797406-69-9
分子式	C₄₉H₆₀ClN₉O₈S₂
分子量	1002.64
SMILES Code	CC1=C(C)SC2=C1C(C3=CC=C(C=C3)Cl)=N[C@@H](CC(NCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@H](C4)O)C(NCC5=CC=C(C6=C(N=CS6)C)C=C5)=O)=O)=O)=O)C7=NN=C(C)N27
MDL No.	N/A

别名
运输	蓝冰
InChI Key	PTAMRJLIOCHJMQ-PYNGZGNASA-N
Pubchem ID	122201421

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C

溶解方案

细胞实验：

DMSO: 105 mg/mL(104.72 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

方案三

MZ1 {[allProObj[0].p_purity_real_show]}

MZ1 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

MZ1 质控信息

MZ1 生物活性

MZ1 细胞实验

MZ1 动物实验

MZ1 动物研究

MZ1 参考文献

MZ1 实验方案

MZ1 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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MZ1 {[allProObj[0].p_purity_real_show]}

MZ1 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

MZ1 质控信息

MZ1 生物活性

MZ1 细胞实验

MZ1 动物实验

MZ1 动物研究

MZ1 参考文献

MZ1 实验方案

MZ1 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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MZ1 纯度/质量文件产品仅供科研