o-Phenanthroline is a selective inhibitor of 26S proteasome subunit Rpn11 with IC50 of 10±2 uM.
o-Phenanthroline shows no activity for other DUBs (USP1/USP2/USP4/USP5/USP7/USP8/USP20/UCH37, IC50>50 uM).
o-Phenanthroline blocks cellular proteasome function, induces apoptosis in MM cells and overcomes resistance to proteasome inhibitor bortezomib, activates caspase cascade and endoplasmic stress response signaling.
o-Phenanthroline reduces progression of tumor growth and prolongs survival in mice MM xenograft model.
Physicochemical Properties
M.Wt
180.21
Formula
C12H8N2
Appearance
Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
4,5-Diazaphenanthrene
References
1. Song Y, et al. Oncogene. 2017 Jun 5. doi: 10.1038/onc.2017.172.
2. Verma R, et al. Science. 2002 Oct 18;298(5593):611-5.
