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LifeSensors/PC1002 dBET1 5mg/PC1002 dBET1 5mg

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PC1002dBET15mg

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dBET1 is a potent andselective BRD4 protein degrader. The molecule, dubbed “degronimid”, isharnessed by combining two specific high affinity protein ligands, (+)-JQ1 forBRD4 and Phthalimide for E3 ubiquitin ligase cereblon (CRBN), tethered by alinker. Fully exploiting the cells’ own protein-degrading machinery, themolecule drags the ubiquitin ligase complex into the tagged protein, leading toa fast, sustainable, CRBN-dependent and ligand-guided BRD4 degradation. It isso selective that only three proteins, BRD2, 3, 4, of >7000 within the cell,were affected. dBET1 demonstrated powerful anti-leukemia activities both incell and in animal model, with few noticeable side effects.ApplicationJQ1 based PROTACthat selectively degrades BRD4 in cellsProduct InformationPurity: >99.5% MW: 799.7Formula: C38H37ClN8O7S∙0.8H2OCAS No. 1799711-21-9Physical State: Lyophilized white powderQuantity: 5mg; 10mg; 25 mgSolubility: 40 mg/mL in DMSOStorage: Store desiccated as supplied at -20°C for up to 3 years. Store solutions at -80°C for up to 6 months or -20°C for up to 1 month.DocumentsDatasheetReferences1. Winter et al (2015) DrugDevelopment. Phthalimide conjugation as a strategy for in vivo target proteindegradation. Science 3481376 PMID: 25999370 2. Wurz et al (2017) A "clickchemistry platform" for the rapid synthesis of bispecific molecules forinducing protein degradation. J.Med.Chem. 10.1021 PMID: 28378579

LifeSensors公司目前主要的产品有400多种，其产品主要覆盖泛素和泛素蛋白酶体通路等科学应用领域，并且产品线在不断的扩大中。公司开创了两大独家技术平台：用于细胞信号和药物发现的泛素蛋白酶体系统(UPS)，以及增强目的蛋白在大肠杆菌、酵母、昆虫和哺乳动物细胞中表达与纯化的SUMO融合表达系统。

泛素蛋白酶体系统正在成为继激酶之后，药物发现的下一个机遇，必将成为未来许多新型药物的创新来源。作为泛素蛋白领域的先驱公司，药物的发现、分析化合物以及去泛素酶和泛素化酶的高通量筛选正是LifeSensors创新技术的真正亮点。此外，LifeSensors还为泛素的蛋白质组学提供众多定制技术服务，并且已经开发了各种各样的测定细胞中的生理底物或生物标志物的方法。