A cell-permeable, orally available quinoline derivative with anti-malarial properties. Increases intralysosomal pH and thereby impairs autophagic degradation process. Reduces metabolic activity and suppresses proliferation of human dermal fibroblasts (IC50 = 30 µM). Shown to inhibit ERK1/2 phosphorylation (Thr202/Try204), but does not affect Akt and mTOR phosphorylation. Shown to directly block the binding of CXCL12 to CXCR4 and inhibit downstream effects in pancreatic cancer cells (EC50 = 9.8 µM). Effectively antagonizes CXCR4-mediated cell proliferation in PANC-1, Hs-766T, and MIAPaCa-2 cells. Suppresses Toll-like receptor 9 (TLR-9)-mediated dendritic cell activation and displays anti-inflammatory properties.
A cell-permeable, orally available quinoline derivative with anti-malarial properties. Increases intralysosomal pH and thereby impairs autophagic degradation process. Reduces metabolic activity and suppresses proliferation of human dermal fibroblasts (IC50 = 30 µM). Shown to inhibit ERK1/2 phosphorylation (Thr202/Try204), but does not affect Akt and mTOR phosphorylation. Shown to directly block the binding of CXCL12 to CXCR4 and inhibit downstream effects in pancreatic cancer cells (EC50 = 9.8 µM). Effectively antagonizes CXCR4-mediated cell proliferation in PANC-1, Hs-766T, and MIAPaCa-2 cells. Suppresses Toll-like receptor 9 (TLR-9)-mediated dendritic cell activation and displays anti-inflammatory properties.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Packaging
Packaged under inert gas
Warning
Toxicity: Harmful (C)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Kim, J., et al. 2012. PLoS ONE.7, e31004. Ramser, B., et al. 2009. J. Invest. Dermatol.129, 2419. Boya., P., et al. 2005. Mol. Cell. Biol.22, 1025. Oikarinen, A., et al. 2009. J. Invest. Dermatol.129, 2333. Kuznik, A., et al. 2011. J. Immunol.186, 4794.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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