Desmethyl-QCA276

• Description :

  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.

• CAS Number :

  [2126819-55-2]

• Product Name Alternative :

  PROTAC BRD4-binding moiety 4

• UNSPSC :

  12352005

• Target :

  Ligands for Target Protein for PROTAC

• Type :

  Reference compound

• Related Pathways :

  PROTAC

• Applications :

  Cancer-programmed cell death

• Field of Research :

  Cancer

• Assay Protocol :

  https://www.medchemexpress.com/protac-brd4-binding-moiety-4-1.html

• Solubility :

  10 mM in DMSO

• Smiles :

  CC1=NN=C2COCC(C(CC3=CC=CC=C3)=C(C#CC4=CNN=C4)S5)=C5N21

• Molecular Formula :

  C21H17N5OS

• Molecular Weight :

  387.46

• References & Citations :

  [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.

• Shipping Conditions :

  Room temperature

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported