ACBI1

ACBI1 is a potent PROTAC degrader of BAF ATPase subunits SMARCA2 and SMARCA4, also degrades the polybromo-associated BAF (PBAF) complex member PBRM1, with DC50s of 6 nM, 11 nM and 32 nM for SMARCA2, SMARCA4 and PBRM1 in MV-4-11 cells, respectively. ACBI1 can induce anti-proliferative effects and apoptosis.^{<a class="sref" href="#s_ref">[1]</a>}

ACBI1 is diluted from a 10 mM DMSO stock solution to 20 μM in buffer consisting of 20 mM 1,3-bis[tris(hydroxymethyl)methylamino] propane (BIS-TRIS) propane, 150 mM NaCl, 1 mM TCEP, pH 7.4 and a final DMSO concentration of 0.2%. Two sets of sequential titrations aer performed; first, a titration of SMARCA2BD (200 μM, in the syringe) into the PROTAC solution (20 μM, in the cell), followed by a titration of VCB complex solution (168 μM in the syringe) into the PROTAC–SMARCA2BD complex solution retained in the cell. Binary experiments consisted of an analogous initial single injection of buffer (syringe) into the PROTAC solution (20 μM, in the cell), followed by a titration of VCB complex solution (168 μM in the syringe) into the diluted PROTAC solution retained in the cells.