GNE-781 | CBP Inhibitor | AmBeed-信号通路专用抑制剂

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

货号：A1176639

GNE-781 是一种有效、口服活性和选择性的 CBP 抑制剂，在 TR-FRET 测定中的 IC50 为 0.94 nM。GNE-781 还抑制 BRET 和 BRD4 (1)，IC50 值分别为 6.2 nM 和 5100 nM。

GNE-781 化学结构
CAS号：1936422-33-1

GNE-781 3D分子结构
CAS号：1936422-33-1

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GNE-781 纯度/质量文件产品仅供科研

货号：A1176639 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: • Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]; • Cell, 2025. Ambeed. [ A122167 ]; • Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]; • Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]; • Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]; 更多 >

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	+++ 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	+ BRD4, IC50: 0.5 μM BRD3, IC50: 0.25 μM						98%
Molibresib	+++ BET proteins, IC50: 35 nM						99%+
I-BRD9	+++ BRD9, pIC50: 7.3 BRD4, pIC50: 5.3						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	++ 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	++++ 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	++++ BRD4-BD1, IC50: 119 nM BRD3-BD1, IC50: 9 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-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	+++ BRD4-BD1, IC50: 143 nM BRD2-BD1, IC50: 75nM						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		++ 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, 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			++ BRPF1, IC50: 80 nM BRPF2, IC50: 7.9 μM				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			++++ 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					+ PCAF, IC50: 5 μM p300/CBP, IC50: 8.5 μM		99%+
SGC-CBP30					++++ EP300, IC50: 38 nM CREBBP, IC50: 21 nM		99%+
Nordihydroguaiaretic acid					✔	HER2,IGF-1R	99%+
Curcumin					+ p300, IC50: ~25 μM	Nrf2,NF-κB,Ferroptosis	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。

GNE-781 生物活性

靶点	p300/CBP CBP, IC50:0.94 nM BET BRD4(1), IC50:5100 nM

GNE-781 细胞实验

Cell Line JJN3 cells KMS11 cells human myeloma cell lines (HMCL) MCF10A-EGR2-Luc cells MCF10A-DUSP1-Luc cells	Concentration	Treated Time	Description	References
JJN3 cells	JJN3 cells		POM + G781 significantly reduced MYC and IRF4 protein levels	Blood Cancer Discov. 2024 Jan 8;5(1):34-55.
KMS11 cells	KMS11 cells		POM + G781 significantly reduced MYC and IRF4 protein levels	Blood Cancer Discov. 2024 Jan 8;5(1):34-55.
human myeloma cell lines (HMCL)	human myeloma cell lines (HMCL)		G781 downregulated IRF4 and MYC more consistently and to similar degrees	Blood Cancer Discov. 2024 Jan 8;5(1):34-55.
MCF10A-EGR2-Luc cells	MCF10A-EGR2-Luc cells		To study the effect of GNE-781 on EGF-induced EGR2 transcription. Results showed that GNE-781 enhanced EGR2 reporter activity.	Nucleic Acids Res. 2021 Dec 16;49(22):12744-12756.
MCF10A-DUSP1-Luc cells	MCF10A-DUSP1-Luc cells		To study the effect of GNE-781 on EGF-induced DUSP1 transcription. Results showed that GNE-781 dampened the early induction phase of DUSP1.	Nucleic Acids Res. 2021 Dec 16;49(22):12744-12756.

GNE-781 动物实验

Species Mice	Animal Model Vk*MYC mouse model	Administration	Dosage	Frequency	Description	References
Mice	Vk*MYC mouse model	Oral	3.75 mg/kg and 15 mg/kg	Twice daily for 2 weeks	High-dose G781 (15 mpk) was more effective than low-dose G781 in reducing M-spikes, but showed dose toxicity	Blood Cancer Discov. 2024 Jan 8;5(1):34-55.

GNE-781 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

9.51mL

1.90mL

0.95mL

19.03mL

3.81mL

1.90mL

GNE-781 技术信息

CAS号	1936422-33-1
分子式	C₂₇H₃₃F₂N₇O₂
分子量	525.59
SMILES Code	CN1N=CC(C2=C(C(F)F)C=C3N(CCCC3=C2)C4=NN(C5CCOCC5)C6=C4CN(CC6)C(NC)=O)=C1
MDL No.	MFCD31693834

别名
运输	蓝冰

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, store in freezer, under -20°C

溶解方案

细胞实验：

DMSO: 105 mg/mL(199.77 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

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

GNE-781 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

GNE-781 质控信息

GNE-781 生物活性

GNE-781 细胞实验

GNE-781 动物实验

GNE-781 实验方案

GNE-781 技术信息

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

GNE-781 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

GNE-781 质控信息

GNE-781 生物活性

GNE-781 细胞实验

GNE-781 动物实验

GNE-781 实验方案

GNE-781 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

工作液计算器

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GNE-781 纯度/质量文件产品仅供科研