GSK6853 | BRPF1 Bromodomain Inhibitor | AmBeed-信号通路专用抑制剂

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GSK6853 {[allProObj[0].p_purity_real_show]}

货号：A181180

GSK6853是一种有效而选择性的RPF1乙酰赖氨酸（pKd=9.5）抑制剂，与其他乙酰赖氨酸相比，选择性高达1600倍。

GSK6853 化学结构
CAS号：1910124-24-1

GSK6853 3D分子结构
CAS号：1910124-24-1

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GSK6853 纯度/质量文件产品仅供科研

货号：A181180 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 (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	++++ 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	++++ BRD3-BD1, IC50: 9 nM BRD4-BD1, IC50: 119 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	+++ 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					++ 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					✔	IGF-1R,HER2	99%+
Curcumin					+ p300, IC50: ~25 μM	Nrf2,Ferroptosis,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。

GSK6853 生物活性

靶点

BRPF

BRPF1, pIC50:8.1

描述

The bromodomain and PHD finger-containing (BRPF) family of BRPF1 is essential for the assembly of MYST histone acetyltransferase complexes. GSK6853 is a potent, selective, soluble, and cell-active inhibitor of the BRPF1 bromodomain (TR-FRET pIC50=8.1; NanoFRET pIC50=7.7). In the BROMOscan panel of bromodomain binding assay, GSK6853 exhibited potent inhibition towards BRPF1 with a pK_d value of 9.5 and >1600-fold selectivity over other bromodomains. In male CD1 mice, GSK6853 showed a high blood clearance (107mL/min/kg), a moderate volume of distribution (5.5L/kg) and a moderate terminal half-life (1.7h) following intravenous injection (1mg/kg). Via oral administration (3 mg/kg), GSK6853 demonstrated a moderate systemic exposure (Cmax=42ng/mL; Tmax=1.5h) and a bioavailability of 22%. Intraperitoneal administration (3 mg/kg) achieved a Cmax of 469ng/mL, Tmax of 0.25h, and a bioavailability of 85%^[2].

GSK6853 细胞实验

Cell Line Huh7 cells OVCAR-3 PEO4	Concentration	Treated Time	Description	References
Huh7 cells	32.9 ± 3.5 μM	72 h	Induces cellular death without affecting cellular shape	Protein Sci. 2024 Nov;33(11):e5191.
OVCAR-3	10 µM and 20 µM	12 days	To evaluate the effect of GSK6853 on ovarian cancer cell proliferation, results showed that GSK6853 significantly inhibited the proliferation of OVCAR-3 cells.	Sci Rep. 2025 Mar 4;15(1):7602.
PEO4	10 µM and 20 µM	12 days	To evaluate the effect of GSK6853 on ovarian cancer cell proliferation, results showed that GSK6853 significantly inhibited the proliferation of PEO4 cells.	Sci Rep. 2025 Mar 4;15(1):7602.

GSK6853 动物实验

Species Male CD1 mice	Animal Model Male CD1 mice	Administration	Dosage	Frequency	Description	References
Male CD1 mice	Male CD1 mice	Intraperitoneal (ip)	3 mg/kg		Evaluated the suitability of GSK6853 for potential PK/PD models, showing that the ip route is suitable for dosing.	ACS Med Chem Lett. 2016 May 9;7(6):552-7

GSK6853 参考文献

[1]Bamborough P, Barnett HA, et al. GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain. ACS Med Chem Lett. 2016 May 9;7(6):552-7.

[2]Bamborough P, Barnett HA, Becher I, et al. GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain. ACS Med Chem Lett. 2016;7(6):552-557.

GSK6853 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.44mL

0.49mL

0.24mL

12.21mL

2.44mL

1.22mL

24.42mL

4.88mL

2.44mL

GSK6853 技术信息

CAS号	1910124-24-1
分子式	C₂₂H₂₇N₅O₃
分子量	409.48
SMILES Code	O=C(NC1=C(N2[C@H](C)CNCC2)C=C(C(N3C)=C1)N(C)C3=O)C4=CC=CC=C4OC
MDL No.	MFCD30489734

别名
运输	蓝冰
InChI Key	FQWDVNSBYDXPIO-CQSZACIVSA-N
Pubchem ID	121232405

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: 25 mg/mL(61.05 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

GSK6853 {[allProObj[0].p_purity_real_show]}

GSK6853 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

GSK6853 质控信息

GSK6853 生物活性

GSK6853 细胞实验

GSK6853 动物实验

GSK6853 参考文献

GSK6853 实验方案

GSK6853 技术信息

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GSK6853 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

GSK6853 质控信息

GSK6853 生物活性

GSK6853 细胞实验

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GSK6853 参考文献

GSK6853 实验方案

GSK6853 技术信息

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摩尔计算器

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