| Identification | Back Directory | [Name]
PROTAC BRD4-binding moiety 4 | [CAS]
2126819-55-2 | [Synonyms]
Desmethyl-QCA276
PROTAC BRD4-binding moiety 4
4H,6H-Thieno[2,3-e][1,2,4]triazolo[3,4-c][1,4]oxazepine, 9-methyl-3-(phenylmethyl)-2-[2-(1H-pyrazol-4-yl)ethynyl]- | [Molecular Formula]
C21H17N5OS | [MDL Number]
MFCD32200886 | [MOL File]
2126819-55-2.mol | [Molecular Weight]
387.46 |
| Hazard Information | Back Directory | [Uses]
Desmethyl-QCA276 (PROTAC BRD4-binding moiety 4), the QCA276-based moiety, binds to cereblon ligand via a linker to form PROTAC to degrade BET. QCA276 is a BET inhibitor with an IC50 of 10 nM, and with a Ki of 2.3 nM[1]. Desmethyl-QCA276 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. | [References]
[1] Qin C, et al. Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression. J Med Chem. 2018 Aug 9;61(15):6685-6704. DOI:10.1021/acs.jmedchem.8b00506 |
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