Molibresib | I-BET-762 | BET Inhibitor | AmBeed-信号通路专用抑制剂

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Molibresib {[allProObj[0].p_purity_real_show]}

货号：A222643 同义名： I-BET-762; GSK525762

Molibresib（I-BET762；GSK525762）是一种BET溴结构域抑制剂，其IC50在32.5-42.5 nM之间。

Molibresib 化学结构
CAS号：1260907-17-2

Molibresib 3D分子结构
CAS号：1260907-17-2

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Molibresib 纯度/质量文件产品仅供科研

货号：A222643 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	+++ 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 (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	+++ BRD9, pIC50: 7.3 BRD4, pIC50: 5.3						99%+
BI-7273	++++ BRD9, IC50: 19 nM BRD7, IC50: 117 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	++ 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	++++ 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 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		+ L3MBTL4, IC50: 6 μM L3MBTL3, IC50: 35 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		++ PRC2, Kd: 114 nM EED, Kd: 82 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			++++ 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					+ 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,NF-κB,Nrf2	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。

Molibresib 生物活性

靶点	BET BET proteins, IC50:35 nM
描述	The Bromodomain and Extra-Terminal Domain BET (Bromodomain and Extra-Terminal Domain) family is characterized by the presence of two tandem bromodomains and an extra-terminal domain. BET proteins can govern the assembly of histone acetylation-dependent chromatin complexes, thus regulating gene expression. I-BET-762 is a highly selective BET protein inhibitor with IC50 values of 32.5–42.5nM (measured by FRET analysis). I-BET-762 can suppress the inflammatory gene expression, including LPS-inducible Il6, Ifnb1, Il1b, Il12a, Cxcl9, Ccl12 and IL-1b processing enzyme Mefv, as well as diminish expression of transcription factors Rel, Irf4 and Irf8 in BMDMs. In contrast, I-BET762 only has a marginal effect on general gene transcription in macrophages without LPS-stimulation. Injection of I-BET-762, 30mg/kg, i.v., 1h before or 1.5 h after LPS administration can attenuate death of mice. Twice-daily injections of I-BET-762, 30mg/kg, i.v., for 2 days protected mice against death caused by sepsis^[1]. A phase 1 study of I-BET762 in combination with androgen deprivation therapy treatment for castrate-resistant prostate cancer and a phase 2 study of I-BET762 in combination with Fulvestrant treatment for ER+ breast cancer is recruiting (see https://clinicaltrials.gov/).
作用机制	I-BET-762 can interact with the BRD pocket in the manner of competition with acetylated peptide binding and displace BET proteins from acetylated chromatin in cells.

Molibresib 细胞研究

细胞系	浓度	检测类型	检测时间	活性说明	数据源
Rosetta2 DE3 cells		Function assay	30 mins	Displacement of FAM-labeled ZBA248 from BRD3 BD2 (306 to 417 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki=30.3 nM	26080064

Molibresib 动物研究

Dose

Mice: 8 mg/kg - 25 mg/kg^[3] (p.o.), 10 mg/kg^[4] (i.p.)

Administration

p.o., i.p.

Pharmacokinetics

Animal	Mice^[5]
Dose	1 mg/kg
Administration	i.v.
PAMPA	High
T_1/2	1.22 h
CL	12.57 ml/min/kg
AUC_0→last	1299 ng·h/ml
Vd_ss	1.11 L/kg

Molibresib 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03702036	-		-	-	-
NCT02706535	Drug Interactions	Phase 1	Completed	-	United States, Maryland ... 展开 >> GSK Investigational Site Baltimore, Maryland, United States, 21225 收起 <<
NCT03266159	Solid Tumours	Phase 2	Withdrawn(Study withdrawn befo... 展开 >>re active to fully evaluate impact of changing practice in target population.) 收起 <<	August 19, 2020	-

Molibresib 参考文献

[1]Wyce A, Degenhardt Y, et al. Inhibition of BET bromodomain proteins as a therapeutic approach in prostate cancer. Oncotarget. 2013 Dec;4(12):2419-29.

[2]Chan CH, Fang C, et al. BET bromodomain inhibition suppresses transcriptional responses to cytokine-Jak-STAT signaling in a gene-specific manner in human monocytes. Eur J Immunol. 2015 Jan;45(1):287-297.

[3]Small molecule inhibitors of the BET family: Selective inhibition of the N-terminal bromodomain

Molibresib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.36mL

0.47mL

0.24mL

11.80mL

2.36mL

1.18mL

23.59mL

4.72mL

2.36mL

Molibresib 技术信息

CAS号	1260907-17-2
分子式	C₂₂H₂₂ClN₅O₂
分子量	423.9
SMILES Code	O=C(NCC)C[C@H]1C2=NN=C(C)N2C3=CC=C(OC)C=C3C(C4=CC=C(Cl)C=C4)=N1
MDL No.	MFCD22417091

别名	I-BET-762; GSK525762; GSK525762A; I-BET762
运输	蓝冰
InChI Key	AAAQFGUYHFJNHI-SFHVURJKSA-N
Pubchem ID	46943432

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: 190 mg/mL(448.22 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

1M HCl: 100 mg/mL(235.91 mM)，配合低频超声，并调节pH至1

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

方案四

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT03702036	-		-	-	-
NCT02706535	Drug Interactions	Phase 1	Completed	-	United States, Maryland ... 展开 >> GSK Investigational Site Baltimore, Maryland, United States, 21225 收起 <<
NCT03266159	Solid Tumours	Phase 2	Withdrawn(Study withdrawn befo... 展开 >>re active to fully evaluate impact of changing practice in target population.) 收起 <<	August 19, 2020	-
NCT03150056	Solid Tumours	Phase 1	Recruiting	July 29, 2019	-
NCT02964507	Neoplasms	Phase 2	Recruiting	June 1, 2020	-
NCT01587703	Carcinoma, Midline	Phase 1	Active, not recruiting	December 14, 2018	United States, Maryland ... 展开 >> GSK Investigational Site Baltimore, Maryland, United States, 21231-2410 United States, Massachusetts GSK Investigational Site Boston, Massachusetts, United States, 02215 United States, Pennsylvania GSK Investigational Site Philadelphia, Pennsylvania, United States, 19104 United States, Tennessee GSK Investigational Site Nashville, Tennessee, United States, 37232 United States, Texas GSK Investigational Site Houston, Texas, United States, 77030 Australia, Victoria GSK Investigational Site Clayton, Victoria, Australia, 3168 Canada, Alberta GSK Investigational Site Edmonton, Alberta, Canada, T6G 1Z2 France GSK Investigational Site Bordeaux Cedex, France, 33076 GSK Investigational Site Lyon Cedex 08, France, 69373 GSK Investigational Site Paris Cedex 5, France, 75248 Korea, Republic of GSK Investigational Site Seoul, Korea, Republic of, 03080 GSK Investigational Site Seoul, Korea, Republic of, 03722 Netherlands GSK Investigational Site Amsterdam, Netherlands, 1066 CX Spain GSK Investigational Site Barcelona, Spain, 08035 GSK Investigational Site Madrid, Spain, 28040 GSK Investigational Site Málaga, Spain, 29010 United Kingdom GSK Investigational Site Sutton, Surrey, United Kingdom, SM2 5PT GSK Investigational Site Newcastle upon Tyne, United Kingdom, NE7 7DN 收起 <<
NCT01943851	Cancer	Phase 1	Recruiting	September 26, 2022	United States, Arkansas ... 展开 >> GSK Investigational Site Recruiting Little Rock, Arkansas, United States, 72205 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com United States, Colorado GSK Investigational Site Recruiting Aurora, Colorado, United States, 80045 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com United States, New York GSK Investigational Site Recruiting New York, New York, United States, 10065 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com United States, Pennsylvania GSK Investigational Site Completed Philadelphia, Pennsylvania, United States, 19104 United States, Texas GSK Investigational Site Recruiting Houston, Texas, United States, 77030 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com Australia, Victoria GSK Investigational Site Recruiting East Melbourne, Victoria, Australia, 3002 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com Korea, Republic of GSK Investigational Site Not yet recruiting Seoul, Korea, Republic of, 03722 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com GSK Investigational Site Recruiting Seoul, Korea, Republic of, 06351 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com Spain GSK Investigational Site Recruiting Barcelona, Spain, 08036 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com GSK Investigational Site Recruiting Madrid, Spain, 28006 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com GSK Investigational Site Recruiting Madrid, Spain, 28040 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com GSK Investigational Site Recruiting Málaga, Spain, 29010 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com GSK Investigational Site Recruiting Salamanca, Spain, 37007 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com United Kingdom GSK Investigational Site Recruiting Cambridge, United Kingdom, CB2 0QQ Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com GSK Investigational Site Completed London, United Kingdom, W12 0NN 收起 <<

Molibresib {[allProObj[0].p_purity_real_show]}

Molibresib 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Molibresib 质控信息

Molibresib 生物活性

Molibresib 细胞研究

Molibresib 动物研究

Molibresib 临床研究

Molibresib 参考文献

Molibresib 实验方案

Molibresib 技术信息

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Molibresib {[allProObj[0].p_purity_real_show]}

Molibresib 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Molibresib 质控信息

Molibresib 生物活性

Molibresib 细胞研究

Molibresib 动物研究

Molibresib 临床研究

Molibresib 参考文献

Molibresib 实验方案

Molibresib 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

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