HSP90α Inhibitor Screening Kit (Fluorometric)

MILPITAS, Calif. - Sept. 13, 2021 - PRLog -- Heat shock protein (HSP) 90 is an ATP-dependent molecular chaperone that assists other proteins to fold properly, stabilizes proteins against heat stress, and assists in protein degradation. It has two isoforms (HSP90α and HSP90β) and both are abundantly expressed in the cytoplasm. Heat stress can cause proteins to denature thereby resulting in the loss of protein function.

However, HSP90 can bind to the proteins during heat stress and protect them from misfolding and aggregation. Since HSP90 stabilizes various proteins including cancer-related proteins, cancer-associated protein kinases, transcription factors etc. that are required for the survival of cancer cells, HSP90 is considered as a potential target for cancer therapeutics. HSP90 inhibitors can target either the N-terminal ATP binding site or the C-terminal site of HSP90. Additionally, a number of HSP90 inhibitors are in clinical trials.

BioVision's HSP90α Inhibitor Screening Kit is a 96-well fluorometric assay that can be used to screen and characterize the potential inhibitors of HSP90α. The assay is based on measuring the HSP90-dependent refolding of thermally denatured Lactate Dehydrogenase (LDH) in the presence and absence of potential HSP90α inhibitors. In the presence of potential HSP90α inhibitors, refolding of thermally denatured LDH will be arrested resulting in reduced LDH activity, which is measured by fluorescence at Ex/Em = 535/587 nm. Geldanamycin is included in the kit as a positive control. The assay is simple, rapid and provides a reliable test for screening HSP90α inhibitors.

Figures. (A) HSP90 thermal protection activity in the presence or absence of Geldanamycin. (B) HSP90 thermal protection activity in the presence or absence of DMSO. (c) Inhibition of HSP90α thermal protection activity by Geldanamycin. IC50 of Geldanamycin was calculated as 3.2±0.6 μM. Assay was performed following the kit protocol.

Storage Conditions -80°C
USAGE For Research Use Only! Not For Use in Humans.
For more information on this Assay Kit Cat# K2106 https://bit.ly/3k6LwP5