ACBI1

ACBI1 ist ein potenter PROTAC-Degrader der BAF-ATPase-Untereinheiten SMARCA2 und SMARCA4, der auch das Polybromo-assoziierte BAF (PBAF)-Komplexmitglied PBRM1 abbaut, mit DC50-Werten von 6 nM, 11 nM und 32 nM für SMARCA2, SMARCA4 bzw. PBRM1 in MV-4-11-Zellen. Diese Verbindung kann antiproliferative Effekte und Apoptose induzieren.^{<a class="sref" href="#s_ref">[1]</a>}

• Zelllinien

  MV-4-11 cells

• Konzentrationen

  0.1-1000 nM

• Inkubationszeit

  18 h

• Methode

  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.