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. 2020 Nov 6;11(5):1300–1314. doi: 10.1016/j.apsb.2020.11.001

Table 1.

HMGCR-targeted PROTACs derived from lovastatin with pomalidomide or VH032.

Compd. Linker E3 ligase HMGCR inhibition IC50 (μmol/L)a Remaining HMGCR at 1 μmol/L (%)b
16a CH2(CH2CH2O)3(CH2)3 CRBN 1.25 73 ± 6
16b (CH2CH2O)2(CH2)2 CRBN 1.88 56 ± 4
16c (CH2)3 CRBN 2.49 89 ± 7
21a (CH2)7 VHL 1.56 63 ± 5
21b (CH2)10 VHL 1.32 42 ± 5
Lovastatin – – 0.74 266 ± 29

2.1.

a

IC50 values for HMGCR inhibition were obtained from triplicate experiments.

b

Percentage HMGCR level remaining relative to the control of each compound at 1 μmol/L. The data are the means ± SD from three independent experiments. − Not applicable.