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Molibresib 99%+

货号:A222643 同义名: I-BET-762;GSK525762 Ambeed 开学季,买赠积分,赢豪礼

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: 99%+
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 (1), Ki: <0.085 μM

BRD4 (2), Ki: 0.34 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 +

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 ++++

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 ++

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 ++++

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 +

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 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 98%
ODM-207 99%
GSK778 +++

BRD4-BD1, IC50: 143 nM

BRD2-BD1, IC50: 75nM

97%
SRX3207 +

BRD42, IC50: 3070 nM

BRD41, IC50: 3070 nM

Syk 98%
GSK046 +++

BRD4BD2, IC50: 214 nM

BRD3BD2, IC50: 98 nM

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

98%
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 ++++

BRPF1, IC50: 48 nM

BRPF3, IC50: 260 nM

99%+
E-7386 +++

CBP/beta-catenin, IC50: 0.0484 μM

97%
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 +

PCAF, IC50: 5 μM

p300/CBP, IC50: 8.5 μM

99%+
SGC-CBP30 ++++

CREBBP, IC50: 21 nM

EP300, IC50: 38 nM

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

p300, IC50: ~25 μM

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

CREBBP, IC50: 125nM

p300/CBP, IC50: 363nM

97%
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

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

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

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

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