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. Author manuscript; available in PMC: 2022 Mar 1.
Published in final edited form as: Biochem Pharmacol. 2021 Feb 3;185:114451. doi: 10.1016/j.bcp.2021.114451

Figure 2: Analog B2 substantially prolongs Fluo-Sec residence time on SNAP-SCTRs:

Figure 2:

Effects of DMSO, 12.5 μM of (A) 2-sulfonyl pyrimidines A1 (dark green), A2 (light green), (B) 2-mercapto pyrimidines B1 (light blue), B2 (dark blue), (C) 2-amino pyrimidines C4 (light red), C9 (dark red) or (B) 3.1 or 6.3 μM B2 (dotted lines in blue shades) on dissociation half-lives t1/2 of Fluo-Sec from SNAP-SCTR HEK-293 cell membranes induced by addition of an excess Sec-FL. LanthaScreen ratios normalized to Fluo-Sec bound at time 0; dissociation half-lives (t1/2) determined applying Dissociation – One phase exponential decay-equation in GraphPad Prism 8.4.0; experiments performed in triplicate in at least three independent experiments; data points shown as mean ± SD. Statistical significance of rate constant K changes compared to DMSO determined using GraphPad Prism’s unpaired t-test corrected with Holm-Sidak method, α = 0.01; (A) not significant; (B, C) significant (p < 0.01).