For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
Description
Pimitespib (TAS-116) is a novel, small-molecule inhibitor which inhibits geldanamycin-FITC binding to HSP90 proteins with Ki values of 34.7 nmol/L, 21.3 nmol/L, >50,000 nmol/L, and >50,000 nmol/L for HSP90α, HSP90β, GRP94, and TRAP1, respectively. Furthermore, TAS-116 does not inhibit other ATPases such as HSP70 (IC50 >200 μmol/L).
In vitro
TAS-116 is a selective inhibitor of cytosolic HSP90α and β that does not inhibit HSP90 paralogs such as endoplasmic reticulum GRP94 or mitochondrial TRAP1. Treatment of HCT116 cells with 0.3 μmol/L TAS-116 for 8 hours results in reduced levels of DDR1, which interacts with HSP90α and induction of HSP70, which is a surrogate marker of cytosolic HSP90 inhibition.
