AU-15330

A PROTAC that drives BRM and BRG1 degradation, induces degradation of BRM and BRG1 in HeLa cervical cancer cells at 1 µM but also induces degradation of PBRM1 at the same concentration, decreases proliferation in a panel of 14 cancer cell lines (IC50s = 0.392-28.85 nM), reduces protein levels of FOXA1, ERG, Myc, and prostate-specific antigen in VCaP cells at 1 µM for 24 hours, reduces tumor volume in a VCaP mouse xenograft model. Formulation: A solid. InChI: InChI=1S/C39H49N9O5S/c1-23(25-10-12-26(13-11-25)34-24(2)41-22-54-34)42-37(52)31-18-27(49)20-48(31)38(53)35(39(3,4)5)43-33(51)21-46-14-16-47(17-15-46)30-19-29(44-45-36(30)40)28-8-6-7-9-32(28)50/h6-13,19,22-23,27,31,35,49-50H,14-18,20-21H2,1-5H3,(H2,40,45)(H,42,52)(H,43,51)/t23-,27+,31-,35+/m0/s1. InChIKey: HDCCMCFIGHIDJR-TUDDPRDOSA-N. SMILES: O[C@H](C[C@H]1C(N[C@H](C2=CC=C(C3=C(C)N=CS3)C=C2)C)=O)CN1C([C@@H](NC(CN4CCN(C5=C(N)N=NC(C6=C(O)C=CC=C6)=C5)CC4)=O)C(C)(C)C)=O