SMILES string
CC1=C(SC2=C1C(C3=CC=C(C#CCN)C=C3)=N[C@H](C4=NN=C(N24)C)CC(OC(C)(C)C)=O)C
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Quality Level
Biochem/physiol Actions
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.
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.
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Andrea G Shergalis et al.
ACS chemical biology, 18(2), 331-339 (2023-01-20)
Molecular glues (MGs) are monovalent small molecules that induce an interaction between proteins (native or non-native partners) by altering the protein-protein interaction (PPI) interface toward a higher-affinity state. Enhancing the PPI between a protein and E3 ubiquitin ligase can lead
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