JQ1-JX5 

JQ1-JX5 is a DCAF16-based BRD4 PROTAC degrader. JQ1-JX5 covalently modifies Cys58 of DCAF16, promotes ternary complex formation with BRD4, enables BRD4 ubiquitination and proteasomal degradation. JQ1-JX5 induces time-dependent degradation of BRD4 long and short isoforms in AGS cells with DC₅₀ of 43.97 and 16.77 nM. JQ1-JX5 can be used for the research of cancer, such as acute myeloid leukemia^[1]. (Pink: BRD4 ligand (HY-78695); Blue: DCAF16 E3 ligase ligand; Black: linker).

JQ1-JX5 (1.0 μM; 3-36 h) induces time-dependent degradation of BRD4 long and short isoforms in AGS cells with DC₅₀ of 43.97 and 16.77 nM, and ~90% loss of both isoforms achieved by 24 hours^[1].
JQ1-JX5 (0.01-5 μM; 12 h) induces degradation of BRD4 long and short isoforms in AGS, MDA-MB-453, AsPC1, MV-4-11, MDA-MB-231, and HEK293T cells^[1].
JQ1-JX5 inhibits AGS cells proliferation with an IC₅₀ of 0.4993 μM^[1].
JQ1-JX5 mediates the degradation of BRD4 by covalent recruitment of DCAF16^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

602.13

C₂₉H₂₄ClN₇O₂S₂

CC1=NN=C2[C@@H](N=C(C3=C(N21)SC(C)=C3C)C4=CC=C(C=C4)Cl)CC(NCCOC5=CC=C6N=C(SC6=C5)C#N)=O

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• [1]. Zhang J, et al. New Reversible Covalent Warheads: Cyanobenzothiazoles Recruiting DCAF16 for Targeted Protein Degradation. J Med Chem. 2026;69(9):11620-11637.  [Content Brief]