HSP90A INHIBITOR PU-29F (C15-1304-466)

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
HSP90a

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Molecular Weight: 419.45. Empirical Formula: C₂₀H₂₆FN₅O₄. Assay: ≥. 98% (HPLC). Quality Level: 100. form: powder. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: off-white. solubility: DMSO: 100 . mg/mL. storage temp.: 2-8°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.