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. 2021 Jun 14;10(6):e1295. doi: 10.1002/cti2.1295

Figure 1.

Figure 1

BIIB091 potently inhibits BTK enzymatic activity and downstream proximal signaling events. (a) Chemical structure of BIIB091. (b–d) Detection of phosphorylated BTK and phosphorylated BTK‐associated proteins in whole blood from individual healthy human donors (b, c) or pooled blood from 15 DBA1 mice (d) treated in vitro with dimethyl sulfoxide (DMSO) or titrating concentrations of BIIB091 and lysed in the presence or absence of phosphatase inhibitors (PPi). Representative curve from one individual (b) . Calculated IC50 values across 19 healthy donors (individual data points) are shown along with the mean (24 nm) (c). (e) Phosphorylation levels of PLCγ2 (Y1217) measured in Ramos B cells pre‐treated with titrating concentrations of BIIB091 and stimulated with F(ab′)2 anti‐human IgM (IC50 = 6.9 nm) (Data shown are from one experiment).