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LifeSensors

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PC1002 dBET1 10mg

$235.00
  • Product Code: PC1002 dBET1 10mg
  • Availability: Contact us for lead time
Tags: PROTAC

dBET1 is a potent and selective BRD4 protein degrader. The molecule, dubbed “degronimid”, is harnessed by combining two specific high affinity protein ligands, (+)-JQ1 for BRD4 and Phthalimide for E3 ubiquitin ligase cereblon (CRBN), tethered by a linker. Fully exploiting the cells’ own protein-degrading machinery, the molecule drags the ubiquitin ligase complex into the tagged protein, leading to a fast, sustainable, CRBN-dependent and ligand-guided BRD4 degradation. It is so selective that only three proteins, BRD2, 3, 4, of >7000 within the cell, were affected. dBET1 demonstrated powerful anti-leukemia activities both in cell and in animal model, with few noticeable side effects.


Application


JQ1 based PROTAC that 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) Drug Development. Phthalimide conjugation as a strategy for in vivo target protein degradation. Science 348 1376 PMID: 25999370

2.    Wurz et al (2017) A "click chemistry platform" for the rapid synthesis of bispecific molecules for inducing protein degradation. J.Med.Chem. 10.1021 PMID: 28378579


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