BI-9564 | BRD9/BRD7 Bromodomains Inhibitor | AmBeed-信号通路专用抑制剂

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BI-9564 {[allProObj[0].p_purity_real_show]}

货号：A429986

BI-9564 is an inhibitor of BRD9 (IC50 = 75 nM) and BRD7 (IC50 = 3.4 µM).

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BI-9564 化学结构
CAS号：1883429-22-8

BI-9564 3D分子结构
CAS号：1883429-22-8

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BI-9564 纯度/质量文件产品仅供科研

货号：A429986 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	+ 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。

BI-9564 生物活性

靶点

bromodomain

CECR2, Kd:77 nM
BET

BRD9, Kd:5.9 nM

BRD7, Kd:73 nM

描述

Recurrent mutations in the subunits of the mammalian switch/sucrose nonfermentable complex have been observed in different types of tumors. Bromodomains are protein-binding domains with an affinity to lysine-acetylated target proteins. BI-9564 is a potent, selective inhibitor of BRD9 and BRD7 bromodomains with IC50 values of 75nM and 3.41μM, respectively. The IC50 values of BI-9564 for BRD4-BD1, BRD4-BD2, and BRD2-BD1 were above 100μM. BI-9564 binds to BRD9 and BRD7 with K_D values of 14nM and 239nM, respectively. In U2OS cells, BI-9564 inhibited BRD9 at a concentration of 100nM. No toxicity was observed in U2OS cells after 24-h exposure of BI-9564. BI-9564 inhibited proliferation of human acute myeloid eosinophilic leukemia cell line EOL-1 with an EC50 value of 800nM. In a xenograft model of human acute myeloid leukemia, daily oral treatment with BI-9564 (180mg/kg) for 12 days significantly reduced tumor growth with a tumor growth inhibition value of 52% as compared to the vehicle-treated group^[3].

BI-9564 细胞实验

Cell Line Chla266 BT12 KD G401 BT16	Concentration	Treated Time	Description	References
Chla266	33.7 µM	144 h	Evaluate the effect of BI-9564 on Chla266 cell proliferation, showing an IC50 of 33.7 µM	Int J Mol Sci. 2017 Jul 16;18(7):1537.
BT12	17.2 µM	144 h	Evaluate the effect of BI-9564 on BT12 cell proliferation, showing an IC50 of 17.2 µM	Int J Mol Sci. 2017 Jul 16;18(7):1537.
KD	22.3 µM	72 h	Evaluate the effect of BI-9564 on KD cell proliferation, showing an IC50 of 22.3 µM	Int J Mol Sci. 2017 Jul 16;18(7):1537.
G401	12.5 µM	72 h	Evaluate the effect of BI-9564 on G401 cell proliferation, showing an IC50 of 12.5 µM	Int J Mol Sci. 2017 Jul 16;18(7):1537.
BT16	15.9 µM	72 h	Evaluate the effect of BI-9564 on BT16 cell proliferation, showing an IC50 of 15.9 µM	Int J Mol Sci. 2017 Jul 16;18(7):1537.

BI-9564 动物实验

Species CIEA-NOG mice	Animal Model AML xenograft model	Administration	Dosage	Frequency	Description	References
CIEA-NOG mice	AML xenograft model	Oral	180 mg/kg	Once daily for 18 days	Evaluate the antitumor efficacy of BI-9564 in an AML model	J Med Chem. 2016 May 26;59(10):4462-75

BI-9564 参考文献

[1]Laetitia J M, Manfred K, et al. Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. J Med Chem. 2016 May 26; 59(10): 4462–4475.

[2]Karim RM, Schonbrunn E. An Advanced Tool To Interrogate BRD9. J Med Chem. 2016 May 26;59(10):4459-61.

[3]Martin LJ, Koegl M, Bader G, et al. Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. J Med Chem. 2016;59(10):4462-4475. doi:10.1021/acs.jmedchem.5b01865

BI-9564 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.83mL

0.57mL

0.28mL

14.15mL

2.83mL

1.41mL

28.30mL

5.66mL

2.83mL

BI-9564 技术信息

CAS号	1883429-22-8
分子式	C₂₀H₂₃N₃O₃
分子量	353.41
SMILES Code	O=C1N(C)C=C(C2=CC(OC)=C(CN(C)C)C=C2OC)C3=CC=NC=C13
MDL No.	MFCD30182324

别名
运输	蓝冰
InChI Key	BJFSUDWKXGMUKA-UHFFFAOYSA-N
Pubchem ID	117072549

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

细胞实验：

DMSO: 7 mg/mL(19.81 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

BI-9564 {[allProObj[0].p_purity_real_show]}

BI-9564 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

BI-9564 质控信息

BI-9564 生物活性

BI-9564 细胞实验

BI-9564 动物实验

BI-9564 参考文献

BI-9564 实验方案

BI-9564 技术信息

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BI-9564 {[allProObj[0].p_purity_real_show]}

BI-9564 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

BI-9564 质控信息

BI-9564 生物活性

BI-9564 细胞实验

BI-9564 动物实验

BI-9564 参考文献

BI-9564 实验方案

BI-9564 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

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细胞研究

临床研究

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