pu-h71

PU-H71 is an effective selective HSP90 inhibitor with an IC50 of 51 nM.

PU-H71 HCl (Zelavespib HCl) is a novel Hsp90 inhibitor, a novel purine-based analog, and a radiosensitizer that may be a promising agent for CIRT. PU-H71 HCL shows antitumor activity in many preclinical models of malignancy. PU-H71 HCL has an inhibitory effect on the protein expression levels of Rad51 and Ku70, which may be associated with the double chain break repair in the homologous recombination pathway and non-homologous end-joining pathway.

PU-H71 hydrate is a potent inhibitor of heat shock protein 90 (Hsp90).

PU-H71 is an experimental inhibitor of Hsp90.

SMTIN-P01 is a mitochondria-targeted Hsp90 inhibitor. It is made from the isopropyl amine of the Hsp90 inhibitor PU-H71 being replaced with the mitochondria-targeting moiety triphenylphosphonium.

Icapamespib, also known as PU-HZ 151, is a heat shock protein 90 (HSP90) inhibitor. PU-HZ151 showed EC50 of 5 nM in the FP assay as compared to 11 nM for PU-H71 and a logD of 2.37 as compared to 1.21 for PU-H71. PU-HZ151 and radiolabeled PU-HZ151 showed selectivity for epichaperomes over the individual chaperome members. Icapamespib demonstrated the ability to productively engage the target in cells, mice, and humans.

ARRY-502 is a CRTH2 antagonist. Regulation of cytokine activity is important in molecularly targeted therapies for asthma.

Zelavespib (PU-H71) hydrochloride is a potent Hsp90 inhibitor with an IC50 of 51 nM in MDA-MB-468 cells.