ACBI1

ACBI1 è un potente degradatore PROTAC delle subunità ATPasiche BAF SMARCA2 e SMARCA4, che degrada anche il membro del complesso BAF (PBAF) associato al polibromo PBRM1, con DC50 di 6 nM, 11 nM e 32 nM per SMARCA2, SMARCA4 e PBRM1 nelle cellule MV-4-11, rispettivamente. Questo composto può indurre effetti antiproliferativi e apoptosi.^{<a class="sref" href="#s_ref">[1]</a>}

• Linee cellulari

  MV-4-11 cells

• Concentrazioni

  0.1-1000 nM

• Tempo di incubazione

  18 h

• Metodo

  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 this compound 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 this chemical 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.