Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S1013 Bortezomib (PS-341) <1 mg/mL 76 mg/mL <1 mg/mL
S2619 MG-132 <1 mg/mL 90 mg/mL 25 mg/mL
S2853 Carfilzomib (PR-171) <1 mg/mL 50 mg/mL <1 mg/mL
S2181 Ixazomib Citrate (MLN9708) <1 mg/mL 100 mg/mL <1 mg/mL
S2180 Ixazomib (MLN2238) <1 mg/mL 72 mg/mL 9 mg/mL
S7049 Oprozomib (ONX 0912) <1 mg/mL 100 mg/mL <1 mg/mL
S1157 Delanzomib (CEP-18770) <1 mg/mL 83 mg/mL 83 mg/mL
S1290 Celastrol <1 mg/mL 90 mg/mL <1 mg/mL
S7038 Epoxomicin <1 mg/mL 100 mg/mL 100 mg/mL
S7933 VR23 <1 mg/mL 31 mg/mL <1 mg/mL
S7462 PI-1840 <1 mg/mL 78 mg/mL 33 mg/mL

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations

Bortezomib (PS-341)

Bortezomib (PS-341) is a potent 20S proteasome inhibitor with Ki of 0.6 nM. It exhibits favorable selectivity towards tumor cells over normal cells.



MG132 is a potent cell-permeable proteasome and calpain inhibitor with IC50s of 0.1 and 1.2 μM for the inhibition of proteasome and calpain, respectively.


Carfilzomib (PR-171)

Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM in ANBL-6 cells, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities.


Ixazomib Citrate (MLN9708)

Ixazomib Citrate (MLN9708) immediately hydrolyzed to MLN2238, the biologically active form, on exposure to aqueous solutions or plasma. MLN2238 inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50/Ki of 3.4 nM/0.93 nM in cell-free assays, less potent to β1 and little activity to β2. Phase 3.


Ixazomib (MLN2238)

MLN2238 inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50 and Ki of 3.4 nM and 0.93 nM in cell-free assays, respectively, also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites, with IC50 of 31 and 3500 nM. Phase 3.


Oprozomib (ONX 0912)

Oprozomib (ONX 0912) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM. Phase 1/2.


Delanzomib (CEP-18770)

Delanzomib (CEP-18770) is an orally active inhibitor of the chymotrypsin-like activity of proteasome with IC50 of 3.8 nM, with only marginal inhibition of the tryptic and peptidylglutamyl activities of the proteosome. Phase 1/2.



Celastrol is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM.



Epoxomicin is a selective proteasome inhibitor with anti-inflammatory activity, inhibits primarily the CH-L activity of the 20S proteasome, while T-L and PGPH catalytic activities are also inhibited at 100- and 1000-fold reduced rate.



VR23 is a potent proteasome inhibitor with IC50 of 1 nM, 50-100 nM, and 3 μM for trypsin-like proteasomes, chymotrypsin-like proteasomes, and caspase-like proteasomes, respectively.



PI-1840 is a reversible and selective chymotrypsin-like (CT-L) inhibitor with IC50 of 27 nM with little effects on the other two major proteasome proteolytic activities, trypsin-like (T-L) and postglutamyl-peptide-hydrolysis-like (PGPH-L).

Tags: Proteasome inhibition | ubiquitin-Proteasome system | ubiquitin-Proteasome pathway | Proteasome activity | Proteasome function | ubiquitin-Proteasome degradation | Proteasome assay | Proteasome structure | Proteasome purification | Proteasome inhibitors in cancer therapy | Proteasome cleavage | 20s Proteasome activity | 26s Proteasome structure | Proteasome inhibition assay | Proteasome inhibitor drugs | Proteasome inhibitor review | Proteasomal inhibitor | Proteasomal inhibitors