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Chimeric Human IgE anti NP antibody clone JW8/1 (MCA333S) used for stimulation of LAD2 cells-in vitro followed by evaluation of β-hexosaminidase activity.
FcR-dependent functional activity in primary human immune cells is inhibited by CC-509. When stimulated through the indicated FcR, CC-509 inhibits functional activity in (A) primary human macrophage, (B) primary human B-cells and (C) the LAD2 human mast cell line. (D) Left panel: CC-509 inhibits CD63 upregulation on basophils stimulated through indicated FcR in human whole blood. Right panel: Representative flow-cytometry plot showing the number of events and CD63 mean fluorescence intensity (MFI) on unstimulated (brown trace) or stimulated basophils in the presence of 0.1 µM (blue trace), 1.0 μM (green trace), or 10.0 μM (red trace) CC-509. IC50 values (μM) are indicated in upper-right portion of each panel. All data expressed as percent of DMSO-treated control, mean ± SD.
From: Ferguson GD, Delgado M, Plantevin-Krenitsky V, Jensen-Pergakes K, Bates RJ, Torres S, et al. (2016)
A Novel Triazolopyridine-Based Spleen Tyrosine Kinase Inhibitor That Arrests Joint Inflammation.
PLoS ONE 11(1): e0145705.