LO-3-61

LO-3-61, a JQ-1 analog bearing a truncated fumaramide handle, is a PROTAC (proteolysis-targeting chimeras) -like BRD4 degrader. LO-3-61 degrades both the long and short isoforms of BRD4 CUL4DcAr16-dependently in cells. LO-3-61 shows selectivity for BRD3 and BRD4 degradation in MDA-MB-231 cells[1].

C32H30Cl2N8O3S

677.6

O=C(NC1=CC(Cl)=CN=C1)/C=C/C(N2CCN(C(C[C@H]3C4=NN=C(C)N4C5=C(C(C)=C(C)S5)C(C6=CC=C(Cl)C=C6)=N3)=O)CC2)=O

E1/E2/E3 Enzyme; Epigenetic Reader Domain

Room temperature