(+)-JQ-1

产品编号: T2110 别名:

JQ1

(+)-JQ-1 是一种有效特异性的可逆 BET 溴结构域抑制剂，可激活自噬，抑制BRD4(1/2)的IC50分别为 77 nM 和 33 nM。

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CAS：1268524-70-4

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生物活性化学信息储存和溶解度信息参考文献引用文献

产品描述

(+)-JQ1 is a BET bromodomain inhibitor (IC50: 77 nM/33 nM for BRD4 (1/2)).

体外活性

Binding of a tetra-acetylated Histone H4 peptide to BRD4 was strongly inhibited by (+)-JQ1, with IC50 values of 77 nM and 33 nM for the first and second bromodomain, respectively. Compared to vehicle control, JQ1 (500 nM) markedly accelerated time to half fluorescence recovery in photobleached regions of cells transfected with GFP-BRD4-NUT. Treatment of the patient-derived 797 NMC cell line for 48 hours with JQ1 (500 nM) effaces nuclear foci, producing diffuse nuclear NUT staining by IHC [1]. MM cell proliferation was uniformly inhibited by JQ1, including several MM cell lines selected for resistance to FDA-approved agents (dexamethasone-resistant MM.1R and melaphalan-resistant LR5) [2].

体内活性

A marked reduction in 18F-fluorodeoxyglucose (FDG) uptake was observed with JQ1 treatment (50 mg/kg), whereas vehicle-treated animals demonstrated progressive disease. A reduction in tumor growth with JQ1 treatment [1]. Treatment of mice with JQ1 reduced seminiferous tubule area, testis size, and spermatozoa number and motility without affecting hormone levels. Although JQ1-treated males mate normally, inhibitory effects of JQ1 evident at the spermatocyte and round spermatid stages cause a complete and reversible contraceptive effect [3]. Raji BL tumors grew significantly slower in (+)-JQ1-treated (twice a day at 30 mg/kg or once a day at 50 mg/kg, i.p.) mice compared with vehicle-treated controls. In this model, the average tumor volume was 45% smaller in the compound-treated group at day 14 [4].

细胞实验

Cells were plated at 5,000 cells per well of 96-well plates containing titrations of the compounds as indicated. After incubation, the cells were washed once with PBS and resuspended in 175 μL of ice-cold 70% ethanol and fixed for a minimum of 16 h at 4 °C. The cells were pelleted and washed 1× with PBS and stained for 30 min at room temperature (RT) with 120 μL of staining solution [propidium iodide (20 μg/mL), RNase A (25 μg/mL), 0.1% Triton X-100 in PBS]. Cell number and cell cycle data were obtained by using a flow cytometer using the Express Pro module. DNA content histograms were analyzed by using ModFit LT 3.2 Software. To calculate the number of viable cells in each well, the concentration of events measured using the Guava was multiplied by the volume of cells in the well, then by the fraction of cells in G1+S+G2/M. GI50 values for each cell line were calculated as the concentration of compound giving a 50% reduction in cell number relative to the DMSO control [4].

动物实验

(Harlan) inoculated s.c. with 3 × 10^6 cells per mouse resuspended in 10% Matrigel. Two weeks later (average tumor volume 150 mm3), mice were assigned into two groups: 15 mice were treated with vehicle control (5:95 DMSO:10% 2-Hydroxypropyl-β-cyclodextrin), and 15 mice were treated with 30 mg/kg (+)-JQ1 by i.p. injection twice a day for 28 d. Body weight and tumor volume were measured daily. Tumor volume was calculated from caliper measurements by using the following formula: W × H × L × 0.52. Mice were killed when tumor volume reached 2,000 mm3, when body weight decreased >20% of initial weight, or when the mice were in poor health as established in the IACUC protocol. Survival was plotted and analyzed in GraphPad Prism software, and statistical significance was calculated by using log-rank (Mantel-Cox) and Gehan–Breslow–Wilcoxon tests. MV4-11 xenografts were established in nude mice injected with 10 × 10^6 cells per mouse. JQ1 was dosed i.p. and formulated as described above. Mice were divided into 4 groups of 10 animals: vehicle control once a day; 50 mg/kg (+)-JQ1 once a day; 30 mg/kg (+)-JQ1 twice a day; and cytarabine 100 mg/kg daily (5 d on, 2 d off). Treatment of mice with cytarabine at 100 mg/kg resulted in significant weight loss at day 8 and, therefore, the dose needed to be decreased to 75 mg/kg [4].

Cas No.

1268524-70-4

分子式

C23H25ClN4O2S

分子量

456.99

别名

JQ1;(+)-JQ-1

参考文献

[1]Filippakopoulos P, et al. Selective inhibition of BET bromodomains. Nature. 2010 Dec 23;468(7327):1067-73.[2]Delmore JE, et al. BET bromodomain inhibition as a therapeutic strategy to target c-Myc. Cell. 2011 Sep 16;146(6):904-17.[3]Mertz JA, et al. Targeting MYC dependence in cancer by inhibiting BET bromodomains. Proc Natl Acad Sci U S A. 2011 Oct 4;108(40):16669-74.[4]Matzuk MM, et al. Small-molecule inhibition of BRDT for male contraception. Cell. 2012 Aug 17;150(4):673-84.[5]Wang M, Zhao L, Tong D, et al. BET bromodomain inhibitor JQ1 promotes immunogenic cell death in tongue squamous cell carcinoma[J]. International Immunopharmacology. 2019, 76: 105921.

引用文献

[1]Ding D, Zheng R, Tian Y, et al. Retinoblastoma protein as an intrinsic BRD4 inhibitor modulates small molecule BET inhibitor sensitivity in cancer. Nature Communications. 2022, 13(1): 1-15.[2]Zhang G M, Huang S S, Ye L X, et al. Reciprocal positive regulation between BRD4 and YAP in GNAQ-mutant uveal melanoma cells confers sensitivity to BET inhibitors. Pharmacological Research. 2022: 106464.[3]Wang M, Zhao L, Tong D, et al. BET bromodomain inhibitor JQ1 promotes immunogenic cell death in tongue squamous cell carcinoma. International Immunopharmacology. 2019, 76: 105921 [4]Zhao F, Huang Y, Zhang Y, et al. SQLE inhibition suppresses the development of pancreatic ductal adenocarcinoma and enhances its sensitivity to chemotherapeutic agents in vitro. Molecular Biology Reports. 2022: 1-9

储存和溶解度

Ethanol:45.7 mg/mL (100 mM)
DMSO:45.7 mg/mL (100 mM)
keep away from direct sunlight
Powder: -20°C for 3 years
In solvent: -80°C for 2 years

剂量换算 (+)-JQ-1 1268524-70-4

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剂量 mg/kg

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给药体积 ul

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% DMSO +

% +

% Tween 80 +

% ddH₂O

% DMSO +

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工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

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技术支持

在抑制剂处理说明中可以找到您可能遇到的问题的答案。主题包括如何准备储备溶液，如何存储产品以及基于细胞的测定和动物实验需要特别注意的问题。

Keywords

Inhibitor (+)JQ1 (+) JQ 1 JQ-1 Autophagy Epigenetic Reader Domain inhibit JQ 1 Target Protein-binding Moiety JQ1 Ligands for Target Protein for PROTAC 1268524-70-4

(+)-JQ-1 相关推荐

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注册成功

(+)-JQ-1

JQ1

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