Chemical Name: 7-[5-[[4-[4-[(Dimethylamino)sulfonyl]-1-piperazinyl]phenoxy]methyl]-1,3-dimethyl-1H-pyrazol-4-yl]-1-[2-(4-morpholinyl)ethyl]-3-[3-(1-naphthalenyloxy)propyl]-1H-indole-2-carboxylic acid
Biological ActivitySelective, high affinity Mcl-1 inhibitor (Ki = 454 pM). Disrupts Mcl-BIM complexes (IC50 in low μM range). Also inhibits Mcl-1NOXA interactions. Exhibits no effect on Bcl-XL-Bim or Bcl-X-BCL-Xs interactions. Induces apoptosis in multiple myeloma and non-small cell lung cancer cell lines and exhibits a synergistic effect with NavitoclaxTM to induce apoptosis in vitro. Cell permeable.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Structure-guided design of a series of MCL-1 inhibitors with high affinity and selectivity.
Bruncko et al.
Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax).
Leverson et al.
Cell Death Dis., 2015;6:e1590
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