Proteasome Inhibitor

Z-LLNle-CHO (Z-Leu-Leu-Nle-CHO) is a γ-secretase inhibitor I. Z-LLNle-CHO induces caspase and ROS-dependent apoptosis by blocking the Akt-mediated pro-survival pathway. Z-LLNle-CHO can be used in cancer research, such as breast cancer and leukaemia.

Galeflaprit (LXE408) is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. Galeflaprit has an IC₅₀ of 0.04 μM for L. donovani proteasome and an EC₅₀ of 0.04 μM for L. donovani. Galeflaprit has a low propensity to cross the blood brain barrier. Galeflaprit has the potential for visceral leishmaniasis (VL) research.

Ub4ix is a DUB/26S proteasome inhibitor. Ub4ix can protect K48-linked Ub chains from being chopped up by deubiquitinating enzymes (DUBs) and prevent the proteasomal degradation of Ub-tagged proteins. Ub4ix can reduce the viability of Hela cells and induce apoptosis, with an IC₅₀ value of 1.6 μM.

6-Chlorooxindole (compound 2) is a selective chymase inhibitor with an IC₅₀ of 470 μM. 6-Chlorooxindole shows >100-fold selectivity for chymase over cathepsin G. 6-Chlorooxindole can be used for the study of cardiovascular disease.

Thrombin inhibitor 5 (compound 385) is a thrombin inhibitor, with IC₅₀s ranging from 0.1 μM to 1 μM. Thrombin inhibitor 5 can be used for research of venous thromboembolism.

Bortezomib-d₈ is the deuterium labeled Bortezomib. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (K_i=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Bortezomib can be used for the study of multiple myeloma (MM). Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs).

BC-23 (NSC 45382) is a proteasome inhibitor. BC-23 exhibits good inhibition of CT-L activity of the proteasome and is selective for malignant over normal cells.

10-Undecenoic acid (Standard) is the analytical standard of 10-Undecenoic acid. This product is intended for research and analytical applications. 10-Undecenoic acid (Undecylenic acid) is an antifungal agent. 10-Undecenoic acid inhibits Aβ oligomerization, scavenges ROS and inhibits μ-calpain activity. 10-Undecenoic acid has neuroprotective effects. 10-Undecenoic acid has anticancer effects on a variety of tumors. 10-Undecenoic acid inhibits C. albicans biofilm formation and MRSA infection. 10-Undecenoic acid inhibits quorum sensing signals of Bacillus subtilis and Pseudomonas aeruginosa.

GSK3494245 (DDD01305143) is a potent, orally active, and selective inhibitor of the chymotrypsin-like activity of the parasite proteasome binding in a site sandwiched between the β4 and β5 subunits (IC₅₀=0.16 μM for WT L. donovani proteasomes). GSK3494245 moderately inhibits chymotrypsin-like activity of human proteasome (IC₅₀: purified 26S=13 µM; enriched THP-1 extracts IC₅₀=40µM). GSK3494245 exhibits attractive biological and biosafety properties.

Carfilzomib-d₈ is deuterium labeled Carfilzomib. Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.

Immunoproteasome inhibitor 1 is a potent, reversible, time-independent immunoproteasome and proteasome inhibitor (K_is of 1.18, 0.27, 1.91 μM in β5c, β1i, β5i submits, respectively). Immunoproteasome inhibitor 1 can be used for the research of certain neoplastic diseases.

(Rac)-Calpain Inhibitor XII is a reversible and selective inhibitor of calpain I (μ-calpain, K_i=19 nM). (Rac)-Calpain Inhibitor XII has lower affinities for calpain II (m-calpain, K_i=120 nM) and cathepsin B (K_i=750 nM). (Rac)-Calpain Inhibitor XII has the potential for studying the role of calpains in diverse processes, including neutrophil chemotaxis, neuronal signaling, and cardiac response to injury.

Ac-Leu-Leu-Norleucinol (ALLN) is a calpain inhibitor, can be used for research of Acetaminophen (HY-66005) induced acute liver damage, and lowers glutamic-oxalacetic transaminease (ALT) and glutamic-pyruvic transaminase (AST).

RAMB4 is a ubiquitin-proteasome system (UPS)-stressor. RAMB4 inhibits ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activites. RAMB4 triggers a ubiquitin-proteasome-system (UPS)-stress response without affecting 20S proteasome catalytic activities. Anticancer activity.

(1S,2R)-Alicapistat ((1S,2R)-ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD). (1S,2R)-Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC₅₀ value of 395 nM.

Calpain Inhibitor-1 (compound 36) is a potent and selective cysteine protease calpain 1 (Cal1) inhibitor (IC₅₀=100 nM; K_i=2.89 μM).

Enzyme-IN-1 (compound 1) is a peptide-based inhibitor of N-terminal nucleophile (Ntn) hydrolases. Specifically, Enzyme-IN-1 inhibits the chymotrypsin-like activity (CT-L) of the 20S proteasome. Enzyme-IN-1 may has potential antiinflammatory properties.

Z-GGF-CMK is an Antibacterial agent, an inhibitor of the ClpP1P2 serine protease complex (with an IC₅₀ of 50 μM against intracellular ClpP1P2 protease activity in Mycobacterium bovis BCG), and a selective inhibitor of the mycobacterial Proteasome (with an IC₅₀ of 50 μM against the proteasome in M. bovis BCG). Z-GGF-CMK inhibits the growth of mycobacteria. Z-GGF-CMK exhibits cytotoxic activity against liver cancer cells. Z-GGF-CMK can be used in the research of tuberculosis.

CH 5450 (Z-Ile-Glu-Pro-Phe-Ome) is a selective short peptide human cardiac chymase inhibitor. CH-5450 inhibits the action of rat MAB elastase 2 on substrate Ang I with an IC₅₀ value of 49 µM and N-succinyl-Ala-Ala-Pro-Phe-p-nitroanilide with an IC₅₀ value of 4.8 µM.

Chymase-IN-1 is a potent, selective, orally active, nonpeptide inhibitor of human mast cell chymase with an IC₅₀ of 29 nM.