(-)-JQ1
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
(-)-JQ1是(+)-JQ1的立体异构体，不与任何bromodomain相互作用，可用于阴性对照实验。(+)-JQ1 是一个细胞通透性的BET bromodomain小分子抑制剂，竞争结合乙酰赖氨酸的识别基序。在BRD4依赖性细胞系和患者来源的异种移植模型中，(+)-JQ1竞争结合bromodomain，将BRD4融合癌蛋白从染色质中替换出来，从而诱导鳞状分化和特异性的抗增殖效应。然而，研究结果表明，(-)-JQ1与任何被检测的bromodomain没有显著的相互作用，抑制BRD4(1)时的IC50值为10,000 nM。
参考文献：
Filippakopoulos P, Qi J, Picaud S, Shen Y, Smith WB, Fedorov O, Morse EM, Keates T, Hickman TT, Felletar I, Philpott M, Munro S, McKeown MR, Wang Y, Christie AL, West N, Cameron MJ, Schwartz B, Heightman TD, La Thangue N, French CA, Wiest O, Kung AL, Knapp S, Bradner JE. Selective inhibition of BET bromodomains. Nature. 2010 Dec 23;468(7327):1067-73. doi: 10.1038/nature09504. Epub 2010 Sep 24.
- 1. Te Zhang, Wenjie Xia, et al. "Super-enhancer hijacking LINC01977 promotes malignancy of early-stage lung adenocarcinoma addicted to the canonical TGF-β/SMAD3 pathway." J Hematol Oncol. 2022 Aug 18;15(1):114. PMID: 35982471
- 2. Xiaofei Zhang, Tiebo Mao, et al. "Synergistic blocking of RAS downstream signaling and epigenetic pathway in KRAS mutant pancreatic cancer." Aging (Albany NY). 2022 Apr 25;14(8):3597-3606. PMID: 35468095
- 3. Nora-Guadalupe P Ramirez, Jeon Lee, et al. "ADAP1 promotes latent HIV-1 reactivation by selectively tuning KRAS–ERK–AP-1 T cell signaling-transcriptional axis." Nat Commun. 2022 Mar 1;13(1):1109. PMID: 35232997
- 4. Danhui Liu, Yuzhen Liu, et al. "Trichostatin A promotes esophageal squamous cell carcinoma cell migration and EMT through BRD4/ERK1/2-dependent pathway." Cancer Med. 2021 Aug;10(15):5235-5245. PMID: 34160902
- 5. Seung-Kyoon Kim, Xihui Liu, et al. "Functional coordination of BET family proteins underlies altered transcription associated with memory impairment in fragile X syndrome." Sci Adv. 2021 May 19;7(21):eabf7346. PMID: 34138732
- 6. Somayeh Layeghi-Ghalehsoukhteh, Shreoshi Pal Choudhuri, et al. "Concerted cell and in vivo screen for pancreatic ductal adenocarcinoma (PDA) chemotherapeutics." Sci Rep. 2020 Nov 26;10(1):20662. PMID: 33244070
- 7. Te Zhang, Xuming Song, et al. "Aberrant super-enhancer landscape reveals core transcriptional regulatory circuitry in lung adenocarcinoma." Oncogenesis. 2020 Oct 17;9(10):92. PMID: 33070167
- 8. Wu SY, Lee CF, et al. "Opposing Functions of BRD4 Isoforms in Breast Cancer." Mol Cell. 2020;78(6):1114-1132.e10. PMID: 32446320
- 9. Alfonso-Dunn R, Turner AW, et al. "Transcriptional Elongation of HSV Immediate Early Genes by the Super Elongation Complex Drives Lytic Infection and Reactivation from Latency." Cell Host Microbe. 2017 Apr 12;21(4):507-517.e5. PMID: 28407486
- 10. Alonso, Victoria Lucia, et al. "Overexpression of bromodomain factor 3 in Trypanosoma cruzi (TcBDF3) affects differentiation of the parasite and protects it against bromodomain inhibitors." FEBS Journal (2016). PMID: 27007774
- 11. Peeters, Janneke GC, et al. "Inhibition of Super-Enhancer Activity in Autoinflammatory Site-Derived T Cells Reduces Disease-Associated Gene Expression." Cell reports (2015). PMID: 26387944
- 12. Sengupta, Surojeet, et al. "Inhibition of BET proteins impairs estrogen-mediated growth and transcription in breast cancers by pausing RNA polymerase advancement." Breast cancer research and treatment (2015): 1-14. PMID: 25721606
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 456.99 |
| Cas No. | 1268524-71-5 |
| Formula | C23H25ClN4O2S |
| Synonyms | (-)-JQ1 |
| Solubility | ≥22.85 mg/mL in DMSO; insoluble in H2O; ≥46.9 mg/mL in EtOH with ultrasonic |
| Chemical Name | (R)-tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate |
| SDF | Download SDF |
| Canonical SMILES | CC1=C(C)SC2=C1C(C3=CC=C(Cl)C=C3)=N[C@H](CC(OC(C)(C)C)=O)C4=NN=C(C)N24 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验[1]： | |
|
细胞系 |
BRD4依赖性的NMC细胞 |
|
溶解方法 |
溶于DMSO。为了获得更高的浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
|
反应条件 |
细胞增殖抑制：250 nM，72小时；细胞周期停滞诱导：250 nM，48小时。 |
|
应用 |
在BRD4依赖性的NMC细胞中，分化通常伴随生长停滞，主要表现在Ki67染色减少，细胞增殖的持续抑制和G1细胞周期停滞。(-)-JQ1对映体是(+)-JQ1的无活性负对照。(+)-JQ1有效减少BRD4靶基因RAD21和RAN的表达，而(-)-JQ1没有该效果。 |
| 动物实验[1]： | |
|
动物模型 |
NMC 797异种移植雌性NCr裸鼠 |
|
剂量 |
50 mg/kg/天；腹腔注射 |
|
应用 |
在治疗后4天，用FDG-PET成像对小鼠进行评估。JQ1 ((+)/-)治疗显著减少FDG摄取，而对照组小鼠出现疾病的发展。肿瘤体积的测量证实了JQ1减少肿瘤生长。JQ1在该剂量和疗程下耐受性良好，没有明显的细胞毒性效应或体重减轻。 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。 |
|
References: [1] Filippakopoulos P, Qi J, Picaud S, et al. Selective inhibition of BET bromodomains. Nature, 2010, 468(7327): 1067-1073. |
|
| 描述 | (-)-JQ1是(+)-JQ1的立体异构体，不与任何bromodomain相互作用，可用于阴性对照实验。 | |||||
| 靶点 | ||||||
| IC50 | ||||||
质量控制和MSDS
- 批次：
化学结构
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