GSK1324726A | I-BET726 | Epigenetic Reader Domain Inhibitor

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GSK1324726A {[allProObj[0].p_purity_real_show]}

货号：A186354 同义名： I-BET726

GSK1324726A是 BET 蛋白 BRD2、BRD3 和 BRD4 的抑制剂，其 IC50 分别为 41 nM、31 nM 和 22 nM。

GSK1324726A 化学结构
CAS号：1300031-52-0

GSK1324726A 3D分子结构
CAS号：1300031-52-0

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GSK1324726A 纯度/质量文件产品仅供科研

货号：A186354 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	+++ 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	++++ 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	+ BRD41, IC50: 3070 nM BRD42, 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		+ L3MBTL3, IC50: 35 μM L3MBTL4, IC50: 6 μM					99%
PFI-3		+++ SMARCA2A, Kd: 72 nM SMARCA4, Kd: 55 nM					99%+
UNC1215		+++ L3MBTL3- D274A, IC50: 3.5 μM L3MBTL3, IC50: 120 nM					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			++ BRPF2, pIC50: 5.2 BRPF3, pIC50: 7.1				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					++++ 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。

GSK1324726A 生物活性

靶点	BET BRD2, IC50:31 nM BRD4, IC50:22 nM
描述	GSK1324726A works as both a selective BET Bromodomain inhibitor with pIC50 values of 7.4, 7.1, 7 and 7.3 for BRD2, BRD3, BRD4 and BRDT, respectively, and a potent tetrahydroquinoline ApoA1 up-regulator. It inhibited the production of LPS-stimulated IL6 with pIC50 values of 7.3 and 6.4 in PBMC and HWB cells, respectively. Oral administration of GSK1324726A at doses of 3mg/kg and 10mg/kg significantly reduced expression of PAI-1 mRNA in a murine acute LPS challenge model. Intravenous injection with GSK1324726A at dose of 10mg/kg increased the ratio of survival of a murine septic shock model^[3].
作用机制	GSK1324726A binds to the acetyl-lysine pocket.^[3]

GSK1324726A 细胞实验

Cell Line SK–N–SH and CHP-212 cells CHP-212 cells Neuroblastoma cell lines	Concentration	Treated Time	Description	References
SK–N–SH and CHP-212 cells	100 nM or 1 µM	16 hours	To analyze the transcriptional changes induced by GSK1324726A in neuroblastoma cell lines using Illumina microarrays. Results showed that GSK1324726A treatment led to significant changes in gene expression, involving apoptosis, signaling, and N-Myc-driven pathways.	PLoS One. 2013 Aug 23;8(8):e72967.
CHP-212 cells	250 nM or 1 µM	48 hours	To assess the effect of GSK1324726A on the cell cycle of CHP-212 cells. Results showed that GSK1324726A treatment induced G1 phase arrest and increased the sub-G1 fraction at higher concentrations.	PLoS One. 2013 Aug 23;8(8):e72967.
Neuroblastoma cell lines	75 nM (gIC50)	6 days	To evaluate the growth inhibition and cytotoxic effects of GSK1324726A on neuroblastoma cell lines. Results showed that all tested neuroblastoma cell lines exhibited significant growth inhibition, with most cell lines showing net cell death.	PLoS One. 2013 Aug 23;8(8):e72967.

GSK1324726A 动物实验

Species Nude mice	Animal Model Human neuroblastoma xenograft models	Administration	Dosage	Frequency	Description	References
Nude mice	Human neuroblastoma xenograft models	Oral	5 mg/kg or 15 mg/kg	Once daily for 14 days (SK–N-AS model) or 42 days (CHP-212 model)	To evaluate the inhibitory effect of GSK1324726A on neuroblastoma tumor growth in vivo. Results showed that GSK1324726A treatment significantly inhibited tumor growth and downregulated MYCN and BCL2 expression.	PLoS One. 2013 Aug 23;8(8):e72967.

GSK1324726A 动物研究

Dose

Mice: 5 mg/kg, 15 mg/kg^[2] (p.o.); 10 mg/kg^[1] (i.v.) Rat: 1 mg/kg^[1] (i.v.); 3 mg/kg^[1] (p.o.)

Administration

p.o., i.v.

Pharmacokinetics

Animal	Mice^[1]	Rats^[1]	Dogs^[1]	Monkeys^[1]
Dose	10 mg/kg (i.v.) 3 mg/kg (p.o.)	1 mg/kg (i.v.) 3 mg/kg (p.o.)	1 mg/kg (i.v.) 3 mg/kg (p.o.)	1 mg/kg (i.v.) 2 mg/kg (p.o.)
Administration	i.v. p.o.	i.v. p.o.	i.v. p.o.	i.v. p.o.
F	45% (p.o.)	28 ± 1% (p.o.)	80 ± 12% (p.o.)	103 ± 35% (p.o.)
CL_b	3.1 ± 0.4 ml/min/kg (i.v.)	26 ± 4 ml/min/kg (i.v.)	6.0 ± 1 ml/min/kg (i.v.)	3.0 ± 0.9 ml/min/kg (i.v.)
T_1/2	3.6 ± 0.2 h (i.v.)	> 8 h (i.v.)	1.8 ± 0.6 h (i.v.)	2.7 ± 0.1 h (i.v.)
Vss	0.48 ± 0.1 L/kg (i.v.)	2.0 ± 0.4 L/kg (i.v.)	0.8 ± 0.1 L/kg (i.v.)	1.0 ± 0.4 L/kg (i.v.)
AUC_0→t	6028 ng·h/ml (p.o.)	539 ± 96 ng·h/ml (p.o.)	5900 ± 968 ng·h/ml (p.o.)	10968 ± 3852 ng·h/ml (p.o.)

GSK1324726A 参考文献

[1]Gosmini R, Nguyen VL, et al. The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor. J Med Chem. 2014 Oct 9;57(19):8111-31.

[2]Wyce A, Ganji G, et al. BET inhibition silences expression of MYCN and BCL2 and induces cytotoxicity in neuroblastoma tumor models. PLoS One. 2013 Aug 23;8(8):e72967.

[3]Gosmini R, Nguyen VL, Toum J, Simon C, Brusq JM, Krysa G, Mirguet O, Riou-Eymard AM, Boursier EV, Trottet L, Bamborough P, Clark H, Chung CW, Cutler L, Demont EH, Kaur R, Lewis AJ, Schilling MB, Soden PE, Taylor S, Walker AL, Walker MD, Prinjha RK, Nicodème E. The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor. J Med Chem. 2014 Oct 9;57(19):8111-31. doi: 10.1021/jm5010539. Epub 2014 Sep 24. PMID: 25249180.

GSK1324726A 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.30mL

0.46mL

0.23mL

11.50mL

2.30mL

1.15mL

22.99mL

4.60mL

2.30mL

GSK1324726A 技术信息

CAS号	1300031-52-0
分子式	C₂₅H₂₃ClN₂O₃
分子量	434.91
SMILES Code	O=C(O)C1=CC=C(C2=CC3=C(N(C(C)=O)[C@@H](C)C[C@H]3NC4=CC=C(Cl)C=C4)C=C2)C=C1
MDL No.	MFCD28144683

别名	I-BET726
运输	蓝冰
InChI Key	FAWSUKOIROHXAP-NPMXOYFQSA-N
Pubchem ID	52912222

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

溶解方案

细胞实验：

DMSO: 45 mg/mL(103.47 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：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

GSK1324726A {[allProObj[0].p_purity_real_show]}

GSK1324726A 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

GSK1324726A 质控信息

GSK1324726A 生物活性

GSK1324726A 细胞实验

GSK1324726A 动物实验

GSK1324726A 动物研究

GSK1324726A 参考文献

GSK1324726A 实验方案

GSK1324726A 技术信息

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GSK1324726A 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

GSK1324726A 质控信息

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GSK1324726A 动物研究

GSK1324726A 参考文献

GSK1324726A 实验方案

GSK1324726A 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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临床研究

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