簡(jiǎn)介：JQ1 compound是一種 BET bromodomain 抑制劑，抑制 BRD4(1/2) 的 IC50 分別為 77 nM 和 33 nM。
JQ1 compound物理化學(xué)性質(zhì)：
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密度 |
1.3±0.1 g/cm3 |
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沸點(diǎn) |
610.4±65.0 °C at 760 mmHg |
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分子式 |
C23H25ClN4O2S |
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分子量 |
456.988 |
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閃點(diǎn) |
322.9±34.3 °C |
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精確質(zhì)量 |
456.138672 |
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PSA |
97.61 |
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LogP |
4.49 |
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外觀性狀 |
white to beige |
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蒸汽壓 |
0.0±1.7 mmHg at 25°C |
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折射率 |
1.657 |
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儲(chǔ)存條件 |
2-8°C |
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水溶解性 |
DMSO: soluble20mg/mL, clear |
JQ1 compound詳細(xì)介紹：
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中文名稱(chēng)： |
(S)-(+)-2-(4-(4-氯苯基)-2,3,9-三甲基-6H-噻吩并[3,2-F][1,2,4]三唑并[4,3-A][1,4]二氮雜卓-6-基)乙酸叔丁酯 |
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中文別名： |
（+）-JQ1 抑制劑;(S)-(＋)-2-(4-(4-氯苯基)-2,3,9-三甲基-6H-噻吩并[3,2-F][1,2,4];(S)-(+)-2-(4-(4-氯苯基)-2,3,9-三甲基-6H-噻吩并[3,2-f][1,2,4]三唑并[4,3-a][1,4]二氮雜卓-6-基)乙酸叔丁酯;(S)-(+)-叔丁基 2-(4-(4-氯苯基)-2,3,9-三甲基-6H-噻吩并[3,2-f][1,2,4]噻唑并[4,3-a][1,4]二氮雜革-6-基)乙酸酯;(S)-2-(4-(4-氯苯基)-2,3,9-三甲基-6H-噻吩并[3,2-F][1,2,4]三唑并[4,3-A][1,4]二氮雜卓-6-基)乙酸叔丁酯;2,4-二氯呋喃并[3,2-D]嘧啶 |
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英文名稱(chēng)： |
JQ1 compound |
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英文別名： |
(S)-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;(+)-JQ-1;(S)-(+)-Tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4];(+)?-?JQ-?1;(＋)-JQ1;(S)-(+)-Tert-butyl 2;(S)-(+)-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)aceta...;(S)-(+)-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;(S)-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;6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic acid,;JQ1;(6s)-6-(2-Tert-Butoxy-2-Oxoethyl)-4-(4-Chlorophenyl)-2,3,9-Trimethyl-6,7-Dihydrothieno[3,2-F][1,2,4]triazolo[4,3-A][1,4]diazepin-10-Ium;(S)-JQ1;3mxf;4flp;CHEMBL1957266;JQ-1;SureCN881227;UNII-1MRH0IMX0W;6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic acid, 4-(4-chlorophenyl)-2,3,9-trimethyl-, 1,1-dimethylethyl ester, (6S)-;JQ1 compound;Bromodomain Inhibitor, (+)-JQ1;1MRH0IMX0W;(S)-(+)-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;(S)-te |
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CAS號(hào)： |
1268524-70-4 |
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分子式： |
C23N4O2SCLH25 |
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分子量： |
456.99 |
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詳細(xì)描述： |
博飛美科提供1268524-70-4，Bromodomain Inhibitor, (+)-JQ1，Perfemiker，上?，F(xiàn)貨。 Perfemiker，致力于提供高品質(zhì)、高性價(jià)比小分子化合物的產(chǎn)品。 Perfemiker小分子化合物大量庫(kù)存，提供超過(guò)2萬(wàn)種的抑制劑、激動(dòng)劑、拮抗劑等產(chǎn)品，是藥物及疾病研究的重要原料供應(yīng)商。 (+)-JQ-1 是一種 BET bromodomain 抑制劑，抑制 BRD4(1/2)，IC50 分別為 77 nM/33 nM。 查詢關(guān)鍵詞:“1268524-70-4，Bromodomain Inhibitor, (+)-JQ1，Perfemiker，上?，F(xiàn)貨”。 |
JQ1 compound參考文獻(xiàn)：
[1]. Filippakopoulos P, et al. Selective inhibition of BET bromodomains. Nature. 2010 Dec 23;468(7327):1067-73.
[2]. Matzuk MM, et al. Small-molecule inhibition of BRDT for male contraception. Cell. 2012 Aug 17;150(4):673-84.
[3]. Peirs S, et al. Targeting BET proteins improves the therapeutic efficacy of BCL-2 inhibition in T-cell acute lymphoblastic leukemia. Leukemia. 2017 Feb 3.
[4]. T?gel L, et al. Dual Targeting of Bromodomain and Extraterminal Domain Proteins, and WNT or MAPK Signaling, Inhibits c-MYC Expression and Proliferation of Colorectal Cancer Cells. Mol Cancer Ther. 2016 Jun;15(6):1217-26.
[5]. Sahni JM, et al. Bromodomain and Extraterminal Protein Inhibition Blocks Growth of Triple-negative Breast Cancers through the Suppression of Aurora Kinases. J Biol Chem. 2016 Nov 4;291(45):23756-23768.
[6]. Nakamura Y, et al. Targeting of super-enhancers and mutant BRAF can suppress growth of BRAF-mutant colon cancer cells via repression of MAPK signaling pathway. Cancer Lett. 2017 Aug 28;402:100-109.
[7]. Bhattacharyya S, et al. Altered hydroxymethylation is seen at regulatory regions in pancreatic cancer and regulates oncogenic pathways. Genome Res. 2017 Nov;27(11):1830-1842.
[8]. Lv B, et al. Enhancement of adenovirus infection and adenoviral vector-mediated gene delivery by bromodomain inhibitor JQ1. Sci Rep. 2018 Aug 1;8(1):11554. doi: 10.1038/s41598-018-28421-x.
[9]. Huang X, et al. Targeting Epigenetic Crosstalk as a Therapeutic Strategy for EZH2-Aberrant Solid Tumors. Cell. 2018 Sep 20;175(1):186-199.e19. doi: 10.1016/j.cell.2018.08.058. Epub 2018 Sep 13.
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