A 2-phenylpyridazin-3(2H)-one based non-copper chelater that selectively inhibits the activity of Superoxide dismutase 1 (Cu/Zn-SOD) (IC50 = 1.07 µM). Cells over-expressing SOD1 show reduced sensitivity to LCS-1. Shown to preferably inhibit the growth of a variety of human lung adenocarinoma cell lines with EGFR and KRAS mutations (IC50 = 200 nM). Prevents serum-induced activation of the ERK and PI 3-kinase/AKT signaling thereby affecting cell growth and survival. Apparent half-life of this compound is reported to be 6.6 min in human liver microsomes.
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
Somwar, R., et al. 2011, PNAS in press. Somwar, R., et al. 2009. J. Biomol. Screen14, 1176
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 2
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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Frontiers in oncology, 12, 937444-937444 (2022-08-19)
Gliomas are characterized by high morbidity and mortality, and have only slightly increased survival with recent considerable improvements for treatment. An innovative therapeutic strategy had been developed via inducing ROS-dependent cell death by targeting antioxidant proteins. In this study, we
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