ACBI1

ACBI1 es un potente PROTAC degradador de las subunidades ATPasa BAF SMARCA2 y SMARCA4, también degrada el miembro del complejo BAF (PBAF) asociado a polibromo PBRM1, con DC50s de 6 nM, 11 nM y 32 nM para SMARCA2, SMARCA4 y PBRM1 en células MV-4-11, respectivamente. Este compuesto puede inducir efectos antiproliferativos y apoptosis.^{<a class="sref" href="#s_ref">[1]</a>}

• Líneas celulares

  MV-4-11 cells

• Concentraciones

  0.1-1000 nM

• Tiempo de incubación

  18 h

• Método

  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.