Journal: Molecules
Article Title: Strategic Fluorination to Achieve a Potent, Selective, Metabolically Stable, and Orally Bioavailable Inhibitor of CSNK2
doi: 10.3390/molecules29174158
Figure Lengend Snippet: In vivo CSNK2 inhibition. ( A ) SARS-CoV-2 viral titer measured in mouse lungs 24 h post-inoculation when treated with vehicle or with compound 2 (30 mg/kg p.o. b.i.d.) (n = 5). ( B ) AKT (phospho-Ser129) levels normalized to total AKT levels in mouse lungs following treatment with compound 2 (30 mg/kg p.o. b.i.d.) for 3, 6, and 36 h (n = 3). ( C ) EIF2S2 (phospho-Ser2) levels normalized to total EIF2S2 levels in mouse lungs following treatment with compound 2 (30 mg/kg p.o. b.i.d.) for 3, 6, and 36 h (n = 3). **: p = 0.0028 using unpaired t -test with Welch’s correction.
Article Snippet: Blots were blocked in 5% Milk in 1X TBST (0.1% Tween 20) for 1 h at room temperature, washed with 1X TBST, and incubated with primary antibodies in 5% BSA in 1X TBST for 10 h at room temperature; 1:10,000 phospho-EIF2S2 P-S2 (from Laszlo Gyenis from the David Litchfield group), 1:200 EIF2S2 (Novus Biologicals, H00008894-M09, Centennial, CO, USA), 1:5000 GAPDH (Proteintech, 10494-1-AP, Rosemont, IL, USA).
Techniques: In Vivo, Inhibition