A-1210477

• Background:

  Induced myeloid leukemia cell differentiation protein (MCL-1) is part of the BCL-2 family of proteins that regulates apoptosis. The intrinsic (mitochondrial) apoptotic pathway is activated by intracellular signals strictly controlled by the BCL-2 family of proteins and are grouped into the antiapoptotic, activator, and sensitizer subsets. All function through complex interactions to regulate the integrity of the mitochondrial membrane. As part of the antiapoptotic subset, MCL-1 inhibits mitochondrial outer membranepermeabilization (MOMP) and the release of cytochrome C from mitochondria. MCL-1 is essential for the survival of various cell types that include the nervous system, cardiomyocytes and lymphocytes. Overexpression of MCL-1 is frequently observed inmany tumor types and is closely associated with tumorigenesis and drug resistance. Because of its ability to strictly regulate cell fate, MCL-1 is a target of interest for many drug therapies.

• Description:

  A-1210477 is a potent and selective inhibitor of MCL-1 with a Kiof 0.45 nM1. A-1210477 specifically binds MCL-1 and promotes apoptosis of cancer cells in an MCL-1-dependent manner.2

• Purity:

  ≥ 90%

• Format:

  Solid.

• Solubility:

  Soluble in DMSO up to 10 mg/mL.

• Molecular Formula:

  C46H55N7O7S

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  Powder-20°C3 years4°C2 yearsIn solvent-80°C2 years-20°C1 year

• Calculated Molecular Weight:

  850.04 Da

• CAS Number:

  1668553-26-1