S63845, an MCL-1 Selective BH3 Mimetic: Another Arrow in Our Quiver

Cancer Cell. 2016 Dec 12;30(6):834-835. doi: 10.1016/j.ccell.2016.11.016.

Abstract

A recent study reports a novel small molecule inhibitor of MCL-1 with efficacy in killing MCL-1-dependent cancer cells in vitro and in vivo. With the advent of S63845, the targeting of BCL-2, BCL-XL, and MCL-1 is now possible in vivo, but optimal clinical use is yet to be determined.

MeSH terms

  • Animals
  • Apoptosis
  • Cell Survival / drug effects
  • Gene Expression Regulation, Neoplastic / drug effects
  • Humans
  • Molecular Targeted Therapy
  • Myeloid Cell Leukemia Sequence 1 Protein / metabolism*
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism
  • Pyrimidines / pharmacology*
  • Pyrimidines / therapeutic use
  • Thiophenes / pharmacology*
  • Thiophenes / therapeutic use

Substances

  • MCL1 protein, human
  • Myeloid Cell Leukemia Sequence 1 Protein
  • Pyrimidines
  • S63845
  • Thiophenes