Bromosporine | BET Inhibitor | AmBeed-信号通路专用抑制剂

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Bromosporine {[allProObj[0].p_purity_real_show]}

货号：A104099

Bromosporine抑制多种溴结构域，包括BRD2、BRD4、BRD9和CECR2，IC50分别为0.41 μM、0.29 μM、0.122 μM和0.017 μM。

Bromosporine 化学结构
CAS号：1619994-69-2

Bromosporine 3D分子结构
CAS号：1619994-69-2

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Bromosporine 纯度/质量文件产品仅供科研

货号：A104099 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: • JMC, 2024. Ambeed. [ A919389 , A918471 , A995972 ]; • Anal. Chem., 2024, 96(50): 19947-19954. Ambeed. [ A261947 , A1165388 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A220462 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A165235 , A110205 ]; • Pharmaceutics, 2024, 16(12): 1546. Ambeed. [ A272538 , A187261 , A691302 , A506702 ]; 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	+++ 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 (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	++++ BRD9, IC50: 19 nM BRD7, IC50: 117 nM						99+%
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	++++ 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	++++ 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	++++ 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	98%
ODM-207	✔						99%
GSK778	+++ BRD2-BD1, IC50: 75nM BRD4-BD1, IC50: 143 nM						97%
SRX3207	+ BRD41, IC50: 3070 nM BRD42, IC50: 3070 nM					Syk	98%
GSK046	+++ BRD4_BD2, IC50: 214 nM BRD3_BD2, IC50: 98 nM						98%
GSK620	✔						97%
Thalidomide-NH-C4-NH-Boc	✔						98%
Trotabresib	✔						99%
NHWD-870	✔						98%
CFT8634	++++ BRD9, DC50: 3 nM						99%
GSK2801		++ BAZ2B, Kd: 136 nM BAZ2A, Kd: 257 nM					99%+
KG-501		✔					99%+
UNC 669		+ L3MBTL3, IC50: 35 μM L3MBTL4, IC50: 6 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			++ BRPF2, Kd: 500 nM BRPF1B, Kd: 100 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					++ 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					++++ EP300, IC50: 38 nM CREBBP, IC50: 21 nM		99%+
Nordihydroguaiaretic acid					✔	HER2,IGF-1R	99%+
Curcumin					+ p300, IC50: ~25 μM	Ferroptosis,Nrf2,NF-κB	98%
PF-CBP1 HCl					++ p300/CBP, IC50: 363nM CREBBP, IC50: 125nM		97%
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。

Bromosporine 生物活性

靶点

bromodomain

CECR2, IC50:17 nM
BET

BRD9, IC50:0.122 μM

BRD2, IC50:0.29 μM

描述

Bromodomains are protein interaction modules that play an important role in the targeting of chromatin-modifying enzymes to specific sites. Bromodomain-containing proteins are involved in a variety of biological processes, including cell proliferation, differentiation, energy homeostasis, and neurological function. Bromosporine is a broad spectrum inhibitor for bromodomains with IC50 values of 0.41, 0.29, and 0.122μM for BRD2, BRD4, and BRD9, respectively. It also exhibited inhibitory activities against BAZ2A, BRPF3, CECR2, FALZ, and TIF1α with IC50 values of 9.36, 48.11, 0.017, 5.655, and 12.38μM, respectively^[3]. Bromosporine at a concentration of 10μM resulted in a temperature shift of 4.4, 5.9, 5.3, 5.9, 6.9, 6.2, 7.3, 5.2, 8.3, 0.4, 1.3, 5.2, 0.9, 0.9, 1.2, 0.4, -0.2, 3.9, and 3.4°C for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), BRD4(2), BRDT(1), BRDT(2), CECR2, PB1(5), TAF1(1), TAF1(2), TAF1L(1), TAF1L(2), BAZ2A, TIF1α, ATAD2, BRD9, and CREBBP, respectively. Bromosporine also showed moderate cytotoxicity in HeLa cells at a concentration of 18µM^[4]. Bromosporine can potently reactivate latent HIV-1 replication in a dose- and time-dependent manner^[5].

Bromosporine 参考文献

[1]Roberts TC, Etxaniz U, et al. BRD3 and BRD4 BET Bromodomain Proteins Differentially Regulate Skeletal Myogenesis. Sci Rep. 2017 Jul 21;7(1):6153.

[2]Picaud S, Leonards K, et al. Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia. Sci Adv. 2016 Oct 12;2(10):e1600760.

[3]University of Oxford. Structural Genomics Consortium Nuffield Dept. of Clinical Medicine. 15th Hellenic Symposium of Medicinal Chemistry Athens, 30, May, 2012

[4]Bromosporine (BSP)

[5]Pan H, Lu P, Shen Y, et al. The bromodomain and extraterminal domain inhibitor bromosporine synergistically reactivates latent HIV-1 in latently infected cells. Oncotarget. 2017;8(55):94104-94116.

Bromosporine 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.47mL

0.49mL

0.25mL

12.36mL

2.47mL

1.24mL

24.73mL

4.95mL

2.47mL

Bromosporine 技术信息

CAS号	1619994-69-2
分子式	C₁₇H₂₀N₆O₄S
分子量	404.443

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 Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 50 mg/mL(123.63 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

动物实验配方

Bromosporine {[allProObj[0].p_purity_real_show]}

Bromosporine 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Bromosporine 质控信息

Bromosporine 生物活性

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Bromosporine 实验方案

Bromosporine 技术信息

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bromodomain	CECR2, IC50:17 nM
BET	BRD9, IC50:0.122 μM BRD2, IC50:0.29 μM

Bromosporine {[allProObj[0].p_purity_real_show]}

Bromosporine 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Bromosporine 质控信息

Bromosporine 生物活性

Bromosporine 参考文献

Bromosporine 实验方案

Bromosporine 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

工作液计算器

细胞研究

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Bromosporine 纯度/质量文件产品仅供科研