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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 化学结构
CAS号：1260907-17-2
Molibresib 3D分子结构
CAS号：1260907-17-2
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]}
批次查询： 批次纯度:

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产品名称 BET ↓ bromodomain ↓ BRPF ↓ CBP/beta-catenin ↓ p300/CBP ↓ 其他靶点 纯度
MS436 ++

BRD4 (2), Ki: 0.34 μM

BRD4 (1), Ki: <0.085 μM

 		99%+
CPI-203 +++

BRD4, IC50: 37 nM

 		99+%
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 +

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 ++++

BRD7, IC50: 117 nM

BRD9, IC50: 19 nM

 		99+%
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 ++++

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 +

BRD4BD1, 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-BD2, IC50: 41 nM

BRD4-BD1, IC50: 5 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 +++

BRD3BD2, IC50: 98 nM

BRD4BD2, IC50: 214 nM

 		98%
GSK620 ✔ 97%
Thalidomide-NH-C4-NH-Boc ✔ 98%
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 +

L3MBTL4, IC50: 6 μM

L3MBTL3, IC50: 35 μM

 		98%
PFI-3 +++

SMARCA4, Kd: 55 nM

SMARCA2A, Kd: 72 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

 		97%
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 +

PCAF, IC50: 5 μM

p300/CBP, IC50: 8.5 μM

 		99%+
SGC-CBP30 ++++

EP300, IC50: 38 nM

CREBBP, IC50: 21 nM

 		99%+
Nordihydroguaiaretic acid ✔ HER2,IGF-1R 99%+
Curcumin +

p300, IC50: ~25 μM

 		Nrf2,Ferroptosis,NF-κB 98%
PF-CBP1 HCl ++

CREBBP, IC50: 125nM

p300/CBP, IC50: 363nM

 		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

 		98%
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 活动说明 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
T1/2 1.22 h
CL 12.57 ml/min/kg
AUC0→last 1299 ng·h/ml
Vdss 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 423.895
别名 I-BET-762;GSK525762;GSK525762A
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
溶解度

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
动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 13 mg/mL clear

PO 0.5% CMC-Na 30 mg/mL suspension

Tags: Molibresib | 1260907-17-2 | I-BET762 | GSK525762 | GSK525762A | GSK525762 | GSK 525762 | GSK-525762 | BET Inhibitor | Epigenetics | Epigenetic Reader Domain | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Molibresib 纯度/质量文件 | Molibresib 亚型比较 | Molibresib 生物活性 | Molibresib 细胞研究 | Molibresib 动物研究 | Molibresib 临床数据 | Molibresib 参考文献 | Molibresib 实验方案 | Molibresib 技术信息

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