JQ-1

化学名:JQ-1

英語名:(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

CBNumberCB72572988

MFC23H25ClN4O2S

MW456.99

MOL File1268524-70-4.mol

别名

(6S)-2,3,9-トリメチル-4-(4-クロロフェニル)-1-チア-5,7,8,9a-テトラアザ-6H-シクロペンタ[e]アズレン-6β-酢酸tert-ブチル

(6S)-4-(4-クロロフェニル)-2,3,9-トリメチル-6H-チエノ[3,2-f][1,2,4]トリアゾロ[4,3-a][1,4]ジアゼピン-6-酢酸tert-ブチル

(6S)-6,9a-ジヒドロ-2,3,9-トリメチル-4-(4-クロロフェニル)-5,7,8,9a-テトラアザアズレノ[4,5-b]チオフェン-6-酢酸tert-ブチル

JQ-1物理性質

融点	>205°C (dec.)
沸点	610.4±65.0 °C(Predicted)
比重(密度)	1.33
貯蔵温度	2-8°C
溶解性	DMSO：可溶20mg/mL、透明
外見	粉
酸解離定数(Pka)	2.05±0.60(Predicted)
色	白からベージュ
安定性：	-20°C の DMSO またはエタノール溶液で最大 2 か月間保存できます。
InChIKey	DNVXATUJJDPFDM-KRWDZBQOSA-N

危険有害性情報のコード(GHS)

JQ-1 価格

製品番号	包装	価格	製品説明	購入
富士フイルム和光純薬株式会社(wako) W01COBQH-8485	250mg	￥52500		購入
富士フイルム和光純薬株式会社(wako) W01COBQH-8485	100mg	￥63000		購入
Sigma-Aldrich Japan SML1524	5mg	￥39200	≥98% (HPLC)	購入
Sigma-Aldrich Japan SML1524	25mg	￥119000	≥98% (HPLC)	購入
富士フイルム和光純薬株式会社(wako) W01TRCT117580	5mg	￥18300		購入

JQ-1 化学特性,用途語,生産方法

使用
BET bromodomain inhibitor JQ1 activates HIV latency through antagonizing Brd4 inhibition of Tat-transactivation.
一般的な説明
JQ1 is a member of the triazolo-diazepine compound family, which functions as a pan-BET (bromodomain and extra-terminal motif) family inhibitor. JQ1 is known to suppress cell proliferation and therefore, can be used as a therapeutic drug for a number of cancers including multiple myeloma and acute myeloid leukemia.
Biochem/physiol Actions
(+)-JQ1 is a high affinity, potent and selective inhibitor of BET bromodomain proteins, including BRD2, BRD3, BRD4 and BRDT. (+)-JQ1 (also known as SGCBD01), the active enantiomer of (+/-)-JQ1, inhibits Brd4 (bromodomain-containing 4), which forms complexes with chromatin via two tandem bromodomains (BD1 and BD2) that bind to acetylated lysine residues in histones and Brd4 association with acetylated chromatin is believed to regulate the recruitment of elongation factor b and additional transcription factors to specific promoter regions. The nuclear protein in testis (NUT) gene is known to form fusions with Brd4 that create a potent oncogene, leading to rare, but highly lethal tumors referred to as NUT midline carcinomas (NMC). (+)-JQ1 inhibits recruitment and binding of Brd4 to TNFa and E-selectin promoter elements, and accelerates recovery time in FRAP (fluorescence recovery after photobleaching) assays using GFP-Brd4. Thus (+)-JQ1 is a useful tool to study the role of Brd4 in transcriptional initiation.For characterization details of (+)-JQ1, please visit the JQ-1 probe summary on the Structural Genomics Consortium (SGC) website.(-)-JQ1 is the negative control for the active enantiomer, (+)-JQ1. (-)-JQ1 is available from Sigma. To learn more about and purchase (-)-JQ1, click here.To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc

JQ-1 上流と下流の製品情報

JQ-1 生産企業

JQ-1 スペクトルデータ(¹HNMR)

1268524-70-4, JQ-1 キーワード

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