HSP90a Inhibitor; PU-29F

Biochem/physiol Actions

Primary TargetHSP90a

Cell permeable: yes

General description

A cell-permeable 6-amino-purine based compound that selectively binds to HSP90a (EC₅₀ = 5.4 µM) and inhibits its activity in SKBr3 and MCF-7 breast cancer cells. Exhibits much reduced activity towards other paralogs (EC₅₀ = 22.85, 71, and 173 5.4 µM for HSP90b, GRP94 AND Trap-1, respectively). Selectively depletes cytosolic HER2 and induces its redistribution towards lysosomes and early endosomes (~20 5.4 µM) without affecting membrane associated HER2. Does not appear to be toxic towards nonmalignant cells.

A cell-permeable 6-amino-purine based compound that selectively binds to HSP90a (EC₅₀ = 5.4 µM) and inhibits its activity in SKBr3 and MCF-7 breast cancer cells. Exhibits much reduced activity towards other paralogs (EC₅₀ = 22.85, 71, and 173 5.4 µM for HSP90b, GRP94 AND Trap-1, respectively). Selectively depletes cytosolic HER2 and induces its redistribution towards lysosomes and early endosomes (~20 5.4 µM) without affecting membrane associated HER2. Does not appear to be toxic towards nonmalignant cells.Please note that the molecular weight for this compound is batch-specific due to variable water content.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Patel, P.D., et al. 2013. Nat. Chem. Biol.9, 677.

Packaging

5 mg in Glass bottle

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)