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1268273-90-0

1268273-90-0 structure
1268273-90-0 structure
  • Name: HSP70-IN-1
  • Chemical Name: HSP70-IN-1
  • CAS Number: 1268273-90-0
  • Molecular Formula: C24H28N6O2S
  • Molecular Weight: 464.583
  • Catalog: Research Areas Cancer
  • Create Date: 2018-06-10 05:10:02
  • Modify Date: 2024-01-14 18:47:10
  • HSP70-IN-1 is a heat shock protein (HSP) inhibitor; inhibits the growth of Kasumi-1 cells with an IC50 of 2.3 μM.

Name HSP70-IN-1
Synonyms N-(3-{[4-(Benzyloxy)-2-(4-methyl-1-piperazinyl)-5-pyrimidinyl]sulfanyl}phenyl)glycinamide
Acetamide, 2-amino-N-[3-[[2-(4-methyl-1-piperazinyl)-4-(phenylmethoxy)-5-pyrimidinyl]thio]phenyl]-
Description HSP70-IN-1 is a heat shock protein (HSP) inhibitor; inhibits the growth of Kasumi-1 cells with an IC50 of 2.3 μM.
Related Catalog
Target

HSP70

Caspase-3/7:1.9 μM (IC50, MOLM13 cells)

In Vitro The heat shock protein 70 (Hsp70) is a molecular chaperone which plays an important function in protein homeostasis as well as in cell signaling and survival. Hsp70 is frequently overexpressed in cancer, where the elevated expression is furthermore believed to be a cause of or to lead to resistance to chemotherapy and other treatments. HSP70-IN-1 interferes with the formation of functional Hsp70-HOP-Hsp90 machinery by its ability to dose-dependently alter the megacomplex components and to destabilize an Hsp70-Hsp90 machinery client, Raf-1. In cells, the refolding of heat-denatured luciferase by endogenous as well as transfected Hsp70 is inhibited by HSP70-IN-1. HSP70-IN-1 also results in induction of apoptosis in cancer cells. Addition of HSP70-IN-1to cancer cells dose-dependently alters the formation of the Hsp70-HOP complex, a phenomenon associated with their destabilization and reduction in half-life[1].
References

[1]. Taldone T, et al. Heat shock protein 70 inhibitors. 2. 2,5'-thiodipyrimidines, 5-(phenylthio)pyrimidines, 2-(pyridin-3-ylthio)pyrimidines, and 3-(phenylthio)pyridines as reversible binders to an allosteric site on heat shock protein 70. J Med Chem. 2014 Feb 27;57(4):1208-24.

Density 1.3±0.1 g/cm3
Molecular Formula C24H28N6O2S
Molecular Weight 464.583
Exact Mass 464.199432
LogP 3.27
Index of Refraction 1.686
Storage condition 2-8℃