proteasome

Proteasome inhibitor IX (PS-IX) is an inhibitor of chymotrypsin-like activity of the 20S proteasome (IC50 ~1 μM). Proteasome inhibitor IX shows potent anticancer activity. Proteasome inhibitor IX exhibits HCT116 p53+/+ cells growth inhibitory activity(IC50 = 1.49 μM).

Proteasome-IN-1 is an inhibitor of proteasome.

20S Proteasome activator 1 is a 20S proteasome activator with IC50 values of 0.3 μM for trypsin-like sites, 0.7 μM for chymotrypsin-like sites, and 1.8 μM for caspase sites. It prevents the accumulation of pathogenic alpha-synuclein (A53T) mutants through translation in the cellular system, thereby reducing the probability of disease occurrence. 20S Proteasome activator 1 can be used to study neurodegenerative diseases.

Bortezomib (LDP 341) is a 20S proteasome inhibitor (Ki=0.6 nM) that is reversible and selective. Bortezomib has antitumor activity and inhibits NF-κB, which can disrupt the cell cycle and induce apoptosis.

MG-132 (Z-Leu-Leu-Leu-al) is a 26S proteasome inhibitor (IC50=100 nM) that is cell-permeable and reversible. MG-132 acts as an autophagy activator and also induces apoptosis.

Aprotinin (Traskolan) is a broad-spectrum serine protease (BPTI) inhibitor that inhibits the activity of a number of different esterases and proteases. Aprotinin is an antifibrinolytic agent used to minimize hemorrhage during complex surgical procedures.

Carfilzomib (PR-171) is a proteasome inhibitor that irreversibly binds to the chymotrypsin of the 20S proteasome. Carfilzomib has antitumor activity and may be used to treat multiple myeloma.

Tripterin (Celastrol) is a natural product, a proteasome inhibitor that inhibits the pancreatic rennet-like activity of the 20S proteasome (IC50=2.5 μM). Tripterin has anti-inflammatory, anti-infectious, and immunomodulatory properties.

Alloxan Monohydrate is a diabetogenic agent that acts as a proteasome inhibitor and induces diabetes in experimental animals by damaging the insulin-secreting β-cells in the pancreas. It is commonly used to establish diabetes models.

Ixazomib citrate (MLN9708) is a prodrug of Ixazomib (MLN-2238) and an orally bioavailable second-generation proteasome inhibitor with an IC50 of 3.4 nM, exhibiting potential antineoplastic activity.

PD151746 is a calpain inhibitor with a 20-fold selectivity for u-calpain (Ki = 0.26 ± 0.03 μM) over m-calpain (Ki = 5.33 ± 0.77 μM). Its IC50 values are 0.26 ± 0.03 μM (Ki for μ-calpain) and 5.33 ± 0.77 μM (Ki for m-calpain) [1]. In vitro, PD151746 targets calpain and reduces oxLDL-induced cytotoxicity [2].

VR23 is a potent proteasome inhibitor. Data shows IC50 =1 nM for trypsin-like proteasomes, IC50=50-100 nM for chymotrypsin-like proteasomes, and IC50=3 μM for caspase-like proteasomes.

DD1 (HUN85111) is a proteasome inhibitor that induces human myeloid tumor-selective apoptosis.

MUN57694 is an inhibitor of 26S proteasome.

(1S,2S)-Bortezomib (Bortezomib) is an enantiomer of Bortezomib. Bortezomib is a reversible and selective inhibitor of the proteasome with a Ki of 0.6 nM for 20S proteasome.

K-7174 dihydrochloride is a proteasome and GATA inhibitor that inhibits neuronal degeneration and induces apoptosis.

ML604440 is a cell permeable proteasome β1i (LMP2) subunit inhibitor.

RAMB4 (PTP1B-IN-9) is a ubiquitin-proteasome system (UPS)-stressor,with anticancer activity.

(R)-MG-132 (Z-Leu-D-leu-leu-al) is the enantiomer of MG-132.

RA190 inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.

Marizomib is a novel irreversible brain-permeable proteasome inhibitor that inhibits CT-L (β5), CT-T-laspase-like (C-L, β1), and trypsin-like (T-L, β2) 20S proteasomes with IC50s of 3.5, 28, and 430 nM.[3]

TCH-165 is a small molecule modulator of proteasome assembly, resulting in an increase in 20S levels. The increase in the level of free 20S corresponds to enhanced proteolysis of IDPs.

MLN2238 suppresses the chymotrypsin-like proteolytic (β5) site of the 20S proteasome(Ki50=0.93 nM, IC50=3.4 nM/). The biologically active form of MLN9708 (Ixazomib Citrate) is MLN2238 in aqueous solutions or plasma.

Ixazomib (MLN2238) , a second generation, boron-containing peptide proteasome inhibitor (PI), inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome (IC50/Ki: 3.4/0.93 nM, in cell-free assays), also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites (IC50: 31/3500 nM).