Description
General description
A cell-permeable, potent, selective, competitive, and reversible inhibitor of CD45 (IC₅₀ = 200 nM using pNPP as the substrate, 3.8 µM for CD45 lck, >30 µM for PTP1B lck) that displays anti-proliferative properties. Also reported to potently block T-cell receptor-mediated proliferation (IC₅₀ = 100 nM). Shown to be less cytotoxic (CC₅₀ = 3.5 µM) than other 1,2-naphthalenedione analogs. The phenanthrenedione group does not function as a thiol oxidizing agent. One of the most potent inhibitor of phosphatase tensin homolog deleted on chromosome 10 (PTEN) that enhances PIP3 signaling in a variety of cells and improves the efficacy of granulocyte transfusion in murine models of neutropenia-related pneumonia.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
CD45 using pNPP as a substrate
Product does not compete with ATP.
Reversible: yes
Target IC₅₀: 200 nM or 3.8 µM against CD45 using pNPP or phosphorylated Ick505 peptide as a substrate, respectively
Packaging
Packaged under inert gas
Other Notes
Li, Y., et al. 2011. Blood117, 6702.
Urbanek, R.A., et al. 2001. J. Med. Chem.44, 1777.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Harmful (C)
