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.
Application
JQ1 based PROTACthat selectively degrades BRD4 in cells
Product Information
Purity: >99.5%
MW: 799.7
Formula: C38H37ClN8O7S∙0.8H2O
CAS No. 1799711-21-9
Physical State: Lyophilized white powder
Quantity: 5mg; 10mg; 25 mg
Solubility: 40 mg/mL in DMSO
Storage: 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.
Documents
References
1. 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
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那糖酵解中依赖NAD的酶不是要在线粒体内反应？
蛋白酶分布广泛,主要存在于人和动物消化道中，而消化道通过口与肛门与外界相通，属于外环境或外界环境
（溶菌酶、凝血酶原等）分布在内环境
（消化）酶分布在消化道
