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.- UPC:
- 51131508
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 5083130001