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. Author manuscript; available in PMC: 2020 Aug 22.
Published in final edited form as: J Med Chem. 2019 Aug 2;62(16):7575–7582. doi: 10.1021/acs.jmedchem.9b00871

Figure 3.

Figure 3.

Screen and characterization of potent CDK6-degrading PROTACs. (A/B) CDK6 levels in U251 cells upon 24 h drug treatment. All drugs were administrated at 1 μM. PD (palbociclib) and PD.HCI (commercialized inhibitor, salt) were applied here as control. (C) CP-10 induced more significant degradation of CDK6 than CDK4. Relative expression levels of CDK4/6 normalized to β-Tubulin were labeled. Thus calculated DC50 of CDK6 was about 2.1 nM while DC50 of CDK4 was about 150~180 nM. (D) CP-10 induced specific degradation of CDK6. Immunoblots of representative proteins in samples from two groups of replicates. U2Sl cells were treated with 500 nM PD, CP-1 0 or vehicle control (DMSO) for 4 h. (E) Docking of CP-10 onto CDK4(PDB: 2w96) or CDK6(PDB: 2euf)via Maestro 11.3 (Schrödinger). Docking scores were presented.