HSP70-IN-27c

SKU: orb1226635

Description

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.

Images & Validation

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Key Properties

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CAS Number	1268273-90-0
MW	464.5831
Purity	>98% (HPLC)
Formula	C₂₄H₂₈N₆O₂S
SMILES	CN1CCN(CC1)C2=NC=C(C(=N2)OCC3=CC=CC=C3)SC4=CC=CC(=C4)NC(=O)CN
Target	HSP
Solubility	10 mM in DMSO

Bioactivity

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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.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

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HSP

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HSP70-IN-27c (orb1226635)

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HSP70-IN-27c

Description

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Key Properties

Bioactivity

Storage & Handling

Quality Guarantee

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HSP70-IN-27c (orb1226635)

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