BSJ-03-123 is a potent, CDK6-selective small-molecule degrader.

BSJ-03-123 快速引发与 CDK6 和 CRBN 形成剂量依赖的三元复合体，但与 CDK4 和 CRBN 无法形成此类复合体。通过用 palbo 或 lenalidomide 预处理阻断 CDK6 或 CRBN 的结合位点可阻止三元复合体的形成。

4x10^6 MV4-11 CRBN-/- cells were treated for 3 h with 20 μM palbociclib, BSJ-03-123 or vehicle. 1x10^6 cells were spun down at 500 x g for 5 min, and the supernatant removed. Pellets were incubated at 46, 49, 52 or 55°C for 3 min followed by 3 min incubation at room temperature. 30 μl of lysis buffer (20 mM Tris-HCl pH 8.0, 120 mM NaCl, 0.5% NP-40, protease inhibitors) were added and cells lysed by 3 rounds of snap freezing and thawing. Denatured proteins were removed by 20 min centrifugation at 14.000 x g at 4°C and supernatants analyzed by Western Blotting.