dBET57

  Cat. No.:  DC21893   Featured
Chemical Structure
1883863-52-2
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Field of application
dBET57 is a novel BRD4 heterobifunctional small-molecule ligand (PROTAC), exhibits significant and selective degradation of BRD4 BD1 (DC50/5h=500 nM), but is inactive on BRD4 BD2..
Cas No.: 1883863-52-2
Chemical Name: 2-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-N-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethyl)acetamide
Synonyms: dBET57,dBET 57,dBET-57
SMILES: CC1=C(SC2=C1C(=N[C@H](C3=NN=C(N32)C)CC(=O)NCCNC4=CC=CC5=C4C(=O)N(C5=O)C6CCC(=O)NC6=O)C7=CC=C(C=C7)Cl)C
Formula: C34H31ClN8O5S
M.Wt: 699.183
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: dBET57 is a potent and selective heterobifunctional degrader of BRD4 based on the PROTAC technology, with a DC50/5h of 500 nM for BRD4BD1, and is inactive on BRD4BD2[1].
Target: DC50/5h: 500 nM (BRD4BD1)[1]
References: [1]. Nowak RP, et al. Plasticity in binding confers selectivity in ligand-induced protein degradation. Nat Chem Biol. 2018 Jul;14(7):706-714.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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