Proteasome Inhibitor

KZR-504 is a highly selective inhibitor of immunoproteasome low molecular mass polypeptide 2 (LMP2), with IC₅₀s of 51 nM, 4.274 μM for LMP2 and LMP7, respectively. KZR-504 is of interest for the treatment of autoimmune disease.

K-7174 dihydrochloride is an orally active proteasome and GATA inhibitor. K-7174 dihydrochloride is a cell adhesion inhibitor. K-7174 dihydrochloride induces cell apoptosis. K-7174 dihydrochloride shows antitumor activities, it can be used for the research of cancer.

Z-LLY-FMK (Calpain Inhibitor IV) is a calpain inhibitor, involved in apoptosis of many cell systems. Z-LLY-FMK inhibits the intestine apoptosis after common bile duct ligation. Z-LLY-FMK reduces parasite burden in mice challenged with Taenia crassiceps cysts. Z-LLY-FMK can be used for the study of cysticercosis.

PELI1-IN-1 (compound 3d) is a potent inhibitor of PELI1, E3 ubiquitin ligase. PELI1-IN-1 has anti-tumPELI1-IN-1, a Resveratrol (HY-16561) derivative, is an orally active PELI1 Inhibitor (K_d = 8.2 μM). PELI1-IN-1 markedly interrupts the interaction of PELI1 and SNAIL/SLUG, and inhibits the K63-polyubiquitization of SNAIL/SLUG by PELI1, subsequently downregulating the protein levels of epithelial-mesenchymal transition (EMT) effectors SNAIL/SLUG. PELI1-IN-1 significantly reduces the level of SNAIL, SLUG and Vimentin without affecting the PELI1 expression. PELI1-IN-1 targets the FHA domain of PELI1 and disrupts the interaction, leading to the anti-metastasis of TNBC cells in vitro and in vivo. PELI1-IN-1 shows no evident toxicity in vivo.

Calpain-2-IN-1 (Formula 1A) is a isoform-specific calpain-2 inhibitor with K_is of 181 nM and 7.8 nM for calpain-1, and calpain-2, respectively. Calpain-2-IN-1 can be used for the research of neurodegenerative diseases and other diseases of synaptic function.

MG-262 (Z-Leu-Leu-LeuB(OH)2; ZL3B) is a reversible proteasome inhibitor. MG-262 down-regulates VEGF receptor Flt-1. MG-262 inhibits cell growth and induces apoptosis in malignant cells. MG-262 induces reactive oxygen species (ROS). MG-262 can be used for anti-cancer study.

Celastrol (Standard) is the analytical standard of Celastrol. This product is intended for research and analytical applications. Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC₅₀ of 2.5 μM.

Punicic acid is a bioactive compound of pomegranate seed oil. Punicic acid is an isomer of conjugated α-linolenic acid and ω-5 polyunsaturated fatty acids. Punicic acid has anti-inflammatory and antioxidant activities and can inhibit the expression of inflammatory mediators such as tumor necrosis factor α (TNF-α). Punicic acid can also reduce the formation of β-amyloid deposits and hyperphosphorylation of tau by increasing the expression of GLUT4 protein and inhibiting the overactivation of calpain, and is used to prevent and treat neurodegenerative diseases. In addition, punicic acid also has breast cancer inhibitor properties that depend on lipid peroxidation and PKC pathways.

TY-51469 is a chymase inhibitor with IC₅₀s for simian and human chymases of 0.4 and 7.0 nM, respectively.

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

ONX-0914 (PR-957) TFA is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 TFA blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 TFA is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (K_i=5.2 μM). ONX-0914 TFA reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1.

Fulacimstat is an orally available chymase inhibitor, with IC₅₀s of 4, 3 nM for human and hamster chymase enzyme, respectively.

UK-101 is a potent and selective immunoproteasome β1i (LMP2) inhibitor with an IC₅₀ value of 104 nM, displays 144- and 10-fold selectivity over β1c (IC₅₀=15 μM) and β5 subunit (IC₅₀=1 μM), respectivey. UK-101 induces cell apoptosis and can be used for the study of prostate cancer.

Aaptamine is an alkaloid that can be isolated from the sponge Aaptos suberitoides. Aaptamine is a competitive antagonist of the α-adrenergic receptor, as well as an inhibitor of the proteasome and cholinesterase. Aaptamine is cytotoxic to tumor cells and can induce apoptosis, cell cycle arrest of tumor cells, and the expression of p21 through a p53-independent pathway. Aaptamine has multiple activities such as anti-tumor, antioxidant, antibacterial, and analgesic effects.

4'-Hydroxychalcone is a chalcone isolated from licorice root, with hepatoprotective activity. 4'-Hydroxychalcone inhibits TNFα-induced NF-κB activation via proteasome inhibition. 4'-Hydroxychalcone induces a rapid potassium release from mitochondrial vesicles and causes deterioration of respiratory control and oxidative phosphorylation of isolated rat liver mitochondria.

BT317 is a blood-brain transmissible mitochondrial Lon peptidase I (LonP1) and CT-L proteasome inhibitor. BT317 can increase the production of reactive oxygen species (ROS) and induce apoptosis in astrocytoma cells. BT317 has antitumor activity.

LU-005i is a potent inhibitor of β5i subunit of immunoproteasomes (IC₅₀ = 6.6 nM), selective over β5c subunit (IC₅₀ = 287 nM).

Clasto-Lactacystin β-lactone, a natural active metabolite of lactacystin, which is a metabolite of Streptomyces, acts as an irreversible 20S proteasome inhibitor.

10-Undecenoic acid zinc salt (Undecylenic acid zinc salt) is an antifungal agent. 10-Undecenoic acid zinc salt inhibits Aβ oligomerization, scavenges ROS and inhibits μ-calpain activity. 10-Undecenoic acid zinc salt has neuroprotective effects. 10-Undecenoic acid zinc salt has anticancer effects on a variety of tumors. 10-Undecenoic acid zinc salt inhibits C. albicans biofilm formation and MRSA infection. 10-Undecenoic acid zinc salt inhibits quorum sensing signals of Bacillus subtilis and Pseudomonas aeruginosa.

Acetyl-Calpastatin(184-210)(human) is a potent, selective and reversible calpain inhibitor with K_i values of 0.2 nM and 6 μM for μ-calpain and cathepsin L, respectively.