A cell-permeable indandione compound that inhibits the Bmi1-Ring1A E3 complex ubiquitin ligase activity both in cell-free assays (by 100% against self- and Top2α ubiquitination at 25 and 50 µM, respectively) and in HeLa cells (by 100% against Bmi1 ubiquitination at 50 µM). Shown to greatly potentiate Teniposide (VM26) cancer cytotoxicity (by 10-fold in A375 and A549 cultures at 5.5 and 33 µM, respectively) by preventing Top2α degradation following VM26 treatment (100% inhibition at 50 µM in HeLa cells).
Following reconstitution, aliquot and freeze (-207deg;C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas
Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Documentation
Bmi1-Ring1A E3 Ligase Inhibitor, PRT4165 - CAS 31083-55-3 - Calbiochem Certificates of Analysis
Title
Lot Number
203630
References
Reference overview
Alcganati, I., et al. 2009. PLosOne4, e8104.
Data Sheet
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
06-September-2013 JSW
Synonyms
2-(Pyridin-3-ylmethylene)-1H-indene-1,3(2H)-dione
Description
A cell-permeable indandione compound that inhibits the activity of the E3 ubiquitin ligase complex Bmi1-Ring1A both in cell-free assays (complete inhibition of self- and Top2α ubiquitination with 25 and 50 µM PRT4165, respectively) and in HeLa cells (complete inhibition of Bmi1 ubiquitination by 50 µM PRT4165; 5 h incubation). Modifies the cellular localization of Bmi1 without affecting its expression levels. Shown to greatly potentiate Teniposide (VM26) cancer cytotoxicity (by 10-fold in A375 melanoma and A549 lung cancer cultures with 5.5 and 33 µM PRT4165, respectively) by preventing Top2α degradation following VM26 treatment (100% inhibition with 50 µM PRT4165 after 4 h 100 µM VM26 treatment in HeLa cells).
Form
Yellow powder
Intert gas (Yes/No)
Packaged under inert gas
CAS number
31083-55-3
Chemical formula
C₁₅H₉NO₂
Structure formula
Purity
≥99% by HPLC
Solubility
DMSO (50 mg/ml). Use only fresh DMSO for reconstitution.
Storage
Protect from light +2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-207deg;C). Stock solutions are stable for up to 3 months at -20°C.
