HSP70-IN-27c

Research use only, not for human use.

HSP70-IN-27c is a potent, irreversible inhibitor of Hsp70 without Hsp 90 binding activity.

HSP70-IN-27c is a potent, irreversible inhibitor of Hsp70 without Hsp 90 binding activity, inhibits growth of Kasumi-1 AML cells with IC50 of 2.3 uM, and inhibits Caspase-3,7 activation in MOLM13 AML cells with IC50 of 1.9 uM; inhibits HER2 and Raf-1 steady-state levels, PARP cleavage in SKBr3 breast cancer cells with IC50 of about 1.5 uM, induces apoptosis in MDA-MB-468 cells.

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.

——

——

Cytoskeleton/Cell Adhesion Molecules

HSP

Kasumi-1

——

——

1268273-90-0

464.5831

C24H28N6O2S

>98% (HPLC)

10 mM in DMSO

CN1CCN(CC1)C2=NC=C(C(=N2)OCC3=CC=CC=C3)SC4=CC=CC(=C4)NC(=O)CN

Acetamide, 2-amino-N-[3-[[2-(4-methyl-1-piperazinyl)-4-(phenylmethoxy)-5-pyrimidinyl]thio]phenyl]-

(-20℃)

With Ice Pack

≥ 2 years