HSP Modulators: MAL3-101

MAL3-101 Chemical Structure HSP70 Inhibitors and ModulatorsMAL3-101

Heat Shock Protein 70/HSP70 Inhibitor

CAS Number: 912361-26-3

Molecular Formula: C54H66N4O10

Molecular Weight: 931.14 g/mol

Research Areas: Cancer Research, Heat Shock, Apoptosis

 

Alternative Names: Benzyl 4-([1,1′-biphenyl]-4-yl)-1-(6-((2-(butylamino)-1-(4-(2-methoxy-2-oxoethoxy)-3-(methoxycarbonyl)phenyl)-2-oxoethyl)(hexyl)amino)-6-oxohexyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate

 

Biological Description

MAL3-101 is an allosteric Heat shock protein 70 (Hsp70) modulator. It inhibits Hsp70 ATPase activity. MAL3-101 binds within the interface between Hsp70 and Hsp40. It has anti-proliferative activity against multiple myeloma cells. MAL3-101 treatment has been shown to also cause apoptosis in Merkel Cell Carcinomas. It also showed in vivo antitumor activity in an Merkel Cell Carcinomas xenograft model.

 

References:

  1. Fewell SW, et al. Small molecule modulators of endogenous and co-chaperone-stimulated Hsp70 ATPase activity. J Biol Chem. 2004;279(49):51131-40. 
  2. Wisen S, et al. Binding of a small molecule at a protein-protein interface regulates the chaperone activity of hsp70-hsp40. ACS Chem Biol. 2010;5(6):611-22.
  3. Braunstein MJ, et al. Antimyeloma Effects of the Heat Shock Protein 70 Molecular Chaperone Inhibitor MAL3-101. J Oncol. 2011;2011:232037.
  4. Adam C, et al. The HSP70 Modulator MAL3-101 Inhibits Merkel Cell Carcinoma. PLoS One. 2014;9(4):e92041.