Sigma-Aldrich Jq1 Analog-1A

Cell-permeable (+)-JQ1 analog that functions as a potent and selective molecular glue degrader between BRD2/4 and DCAF16.
JQ1 analog-1a is a cell-permeable (+)-JQ1 analog with a rigid primary amine tail that functions as a potent and selective molecular glue degrader between BRD2/4 and DCAF16. JQ1 analog-1a occupies the (+)-JQ1 binding site and specifically drives BRD4-DCAF16 complex assembly. Analog 1a binds to BRD4 BDI-BDII, BDI and BDII with high-affinity (Kd = 3, 4 and 6 nM, respectively in a TR-FRET binding assay) and dose-dependently degrades BRD4 (DC50 ~ 4 nM in HEK293 BRD4-HiBiT cells, T1/2 of 2h at 100 nM) with no hook effect in a proteasomal-dependent manner.