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. 2015 Jul 20;6(28):24733–24749. doi: 10.18632/oncotarget.4619

Table 1. Proteasome inhibitors.

Compound/Origin (if natural) Activity, IC50, nM Type of assay Ref.
CT-L T-L C-L
Peptide aldehydes
Felutamide B (Penicillium fellutanum) 9.4 2000 1200 20S [65]
TP-110 27 20S [66]
MG132 68 4500 1400 20S [66]
Tyropeptin A (Kitasabospora sp.) 40 20S [65]
1400 5000 68 000 20S [66]
Dose-dependent PC12 cells [67]
Syrbactins
Glidobactin A (Burkholderiales) 15 >15 20S [68]
Syringolin A (Pseudomona syringae) 1300 >1300 >1300 20S [68]
Epoxyketones
Epoxomicin (Actinomycetes) 5.7 20S [65]
NC-022 300 20S [69]
NC-001 500 MM1.R, NCI-H929 [70]
YU-102 + 20S [71]
Vinyl esters
HMB-LLL-VE 41 4210 >10 000 20S [72]
Peptide Vinyl Sulfones
MB1 + 20S [73]
Natural polyphenols
Epigallocatechin gallate / EGCG (tea polyphenols) 86–194 20S [74]
1000–10000 Living Jurkat T cells [75]
Curcumin / diferuloylmethane (Curcuma longa) 1850 6230 3680 20S [76]
20000 HCT-116 and SW480 cells [76]
Natural cationic porphyrins
H2T4 750 530 460 20S and 26S [77]
β-lactones
Omuralide / clasto-lactacystin-β-lactone (Salinospora tropica) 29 690 8300 20S [78]
600 Living Jurkat T cells [75]
Hydronaphthoquinones
PI-083 1000 4500 4500 20S [79]
> 1000 > 4500 > 4500 Nude mice [79]
Isothiocyanates
BITC 4700 ~10000 ~10000 A549 cells [80]
Triterpenoids
Pristimerin (Celastrus Maytenus) <100 20S [81]
50 000 H929 and U266 U266 cells [81]
Celastrol (Tripterygium Wilfordi, Celastrus Regelii) 2500 A6 Xenopus cells, mammalian cells, human prostate cancer cells [82]
1000–5000 Nude mice PC-3 or LNCaP cells [83]
Chalcones
AM114 1000 20S [84]
1490 HCT116 p53 +/+ cells [84]
Imidazoline derivatives
TCH-013 2800 1600 20S [85]
Carbamides and carbamates
Hydroxyurea 1000 20S [86]
DSF / disulfiram 2000 MDA-MB-231 cells [87]
DSF Cu (II) 7500 20S [88]
>7500 26S [88]
DSF Cd 3500 20S [88]
3200 hMCF 10 DCIS cells and PC-3 cells [87]
Inorganics
CuCl2 5100 20S [89]

A summary of proteasome inhibitors known to-date grouped by: their origin (synthetic or natural), targeting specificity and IC50 against the proteasomal enzymatic activities (CT-L stands for ChymoTrypsin-Like, T-L stands for Trypsin-Like and C-L stands for Caspase-Like activity), and type of assay used for measuring the inhibitory effect. The compounds are also divided into classes according to their chemical structures (aldehydes, syrbactins, epoxyketones, etc.).