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.

• 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

• CAS Number:

  [2126819-55-2]