PROTAC SMARCA2/4-degrader-19

PROTAC SMARCA2/4-degrader-19 (Compound I-412) is a PROTAC degrader targeting the catalytic subunits SMARCA2 and SMARCA4 of the SWI/SNF complex. It degrades SMARCA2 in MV411 and A549 cell lines with a DC50 of less than 100 nM, and it degrades SMARCA4 in MV411 with a DC50 also under 100 nM.

CC1=NC(N2C3CN(CC2CC3)C=4C=C(N=NC4N)C5=C(O)C=CC=C5)=NC=C1[C@@H]6CC[C@@H](C(N[C@H](C(=O)N7[C@H](C(NCC8=CC=C(C=C8)C9=C(C)N=CS9)=O)C[C@@H](O)C7)C(C)(C)C)=O)CC6