Chemical Structure : dBET1
CAS No.: 1799711-21-9
Catalog No.: PC-62321Not For Human Use, Lab Use Only.
dBET1 is a proteolysis-targeting chimera (PROTAC) molecule that appendes a competitive antagonist of BET bromodomain (JQ1) to a phthalimide moiety to hijack the cereblon E3 ubiquitin ligase complex.
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dBET1 is a proteolysis-targeting chimera (PROTAC) molecule that appendes a competitive antagonist of BET bromodomain (JQ1) to a phthalimide moiety to hijack the cereblon E3 ubiquitin ligase complex.
dBET1 induces highly selective cereblon-dependent BET protein degradation in vitro (EC50=430 nM) and in vivo and delayed leukemia progression in mice.
M.Wt | 785.273 | |
Formula | C38H37ClN8O7S | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
(6S)-4-(4-chlorophenyl)-N-[4-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]butyl]-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide |
1. Winter GE, et al. Science. 2015 Jun 19;348(6241):1376-81.
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