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Table 1 Inhibition of the proteasome

From: Oral proteasome inhibitor with strong preclinical efficacy in myeloma models

Compound (route of administration)

Proteasome inhibition, IC50 (nM)

Binding kinetics

CT-L, β5

T-L, β2

C-L, β1

Bortezomib (IV/SC)

2 ~ 4

2400 ~ 3700

16 ~ 29

reversible

Carfilzomib (IV)

7 ~ 9

400 ~ 460

420 ~ 590

irreversible

Ixazomib (PO)

3 ~ 5

>10000

6 ~ 7

reversible

LC53-0110 (PO)

1 ~ 5

>20000

600 ~ 1300

reversible

  1. The in vitro inhibition of the 20S proteasome catalytic activities was determined in RPMI8226 cellular lysates with fluorogenic peptide substrates specific for each catalytic subunit. Three reference compounds were tested in the assays along with LC53-0110. Binding kinetics was determined by assessing CT-L activity in RPMI8226 cells at different time points after 1-h pulse treatment of cells with a compound.
  2. CT-L chymotrypsin-like, T-L trypsin-like, C-L caspase-like. IV intravenous, SC subcutaneous, PO per os, by mouth
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BMC Cancer

ISSN: 1471-2407

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