BIX 02565 is a potent inhibitor of ribosomal S6 kinase 2 (RSK2, IC50: 1.1 nM).

PRKD1:35 nM (cell free), RSK2:1.1 nM (cell free), LRRK2:16 nM (cell free)

BIX 02565 对RSK2的抑制作用达到了IC50值为1.1 nM。同时，它对LRRK2和PRKD1也显示出抑制作用，其IC50值分别为16 nM和35 nM [1]。此外，BIX 02565在肾上腺素α1A-、α1B-、α1D-、α2A-、β2-及咪唑啉I2受体上产生了超过50%的抑制作用（IC50s范围为0.052-1.820 μM）[2]。

在大鼠CV筛选中，BIX 02565（1、3、10 mg/kg）的灌注导致平均动脉压（MAP；降至基线以下-65 ± 6 mm Hg）和心率（降低至-93 ± 13次/分钟）的急剧下降。在装配了遥测仪的大鼠中，BIX 02565（30、100、300 mg/kg p.o. QD，连续4天）引起了依赖浓度的MAP下降（第4天时至-39 ± 4 mm Hg于T(max)）；通过Demming回归分析显示，无论给药途径和麻醉的影响如何，均呈现出强相关性[2]。

A monolayer of exponentially growing HLR-CREB cells was prepared and transfected using Effectene with RSK2. Cells were plated into 96-well culture plates, and compounds were added 20 to 24 h after transfection. Luciferase expression (48 h) and activity (5 min) were determined using Steady-Glo per manufacturer's instructions, and results were represented as the percentage luciferase activity relative to the control measured in the absence of inhibitors (percentage of control); the IC50 was fitted to a standard four-parameter logistic equation. Each data point represents an average of triplicate observations [2].

Mean arterial pressure was assessed in conscious, freely moving male Sprague-Dawley rats (n = 6/group) instrumented with telemetry transmitters similar to that described previously. BIX 02565 (30, 100, and 300 mg/kg p.o. QD) was administered as a solution (10 ml/kg) in a 20% hydroxy-propyl-β-cyclodextran vehicle as described previously. Mean arterial pressure was reported from 2 h before (baseline) and 90 h after the first dose; compound was administered at 0, 24, 48, and 72 h. A blood sample was collected from satellite rats (n = 3/group) at 1-h after dose (Tmax) on days 1 and 4 for analysis of plasma drug concentrations by mass spectrometry [2].