Proteasome Inhibitor

ML604440 is a specific and cell-permeable Proteasome β1i (LMP2) subunit inhibitor. ML604440 can be used in experimental colitis, EAE and autoimmune disease research. ML604440 shows synergistic effects and advantageous when combined with LMP7 inhibitor.

Octaarginine acetate is a cell-penetrating peptide and proteasome inhibitor. Octaarginine acetate exhibits mixed-type inhibition against 20S proteasome chymotrypsin-like, caspase-like, and trypsin-like activities, and inhibits 26S proteasome activity with decreased efficiency. Octaarginine acetate induces ubiquitin-conjugated protein accumulation, mediates HSPG-dependent cellular internalization via macropinocytosis, enhances liposomal cargo uptake and gene delivery. Octaarginine acetate can be used for the research of cervix carcinoma, collagen antibody-induced arthritis, and bacterial infections.

PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.

LU-002i is a subunit-selective human proteasome β2c and β2i inhibitor with an IC₅₀ value of 220 nM for β2i.

Carfilzomib (Standard) is the analytical standard of Carfilzomib. This product is intended for research and analytical applications. Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC₅₀ of 5 nM in ANBL-6 and RPMI 8226 cells.

RA375 is a RPN13 (26S proteasome regulatory subunit) inhibitor. RA375 activates UPR signaling, ROS production and apoptosis. RA375 exhibits ten-fold greater activity against cancer lines than RA190, reflecting its nitro ring substituents and the addition of a chloroacetamide warhead.

Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC₅₀ value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53^+/+ cells growth inhibitory activity with an IC₅₀ value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity.

Zetomipzomib (KZR-616), a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC₅₀: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC₅₀: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. Zetomipzomib has the potential for the research of multiple autoimmune diseases.

Dazcapistat (BLD-2660) is an orally active small-molecule inhibitor of calpain 1, 2, and 9 (calpain 1, 2, 9). Dazcapistat reduces the expression/production level of IL-6 in injured lung tissue and alleviates fibrosis. Dazcapistat exerts anti-fibrotic effects in various animal models of fibrosis in the skin, liver and lung. Dazcapistat can be used in research related to coronavirus disease 2019 (COVID-19) and idiopathic pulmonary fibrosis.

PR-924 is a selective tripeptide epoxyketone immunoproteasome subunit LMP-7 inhibitor with an IC₅₀ of 22 nM. PR-924 covalently modifies proteasomal N-terminal threonine active sites. PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities.

NIC-0102 is an orally active proteasome inhibitor (pIC₅₀=7.55) that specifically inhibits NLRP3 inflammatory vesicle activation. NIC-0102 shows potent anti-inflammatory effects in a model of dextran sulfate sodium (DSS)-induced ulcerative colitis. NIC-0102 also inhibits production of pro-IL-1β.

AK 295 (CX 295) is a selective calpain inhibitor. AK 295 can inhibit apoptosis through a calpain-dependent pathway. AK 295 shows potent neuroprotective effect. AK 295 can inhibit the activity of the cysteine protease calpain and reduce myocardial injury. AK 295 can be used for the researches of infection, inflammation, cardiovascular and neurological disease, such as stroke and viral myocarditis.

Biotin-(Oaa)₃-epoxomicin is a biotin-labeled form of Epoxomicin (HY-13821), prepared by conjugating Epoxomicin with biotin via three hydrophilic oxaacetyl amino acid (Oaa) linkers. Biotin-(Oaa)₃-epoxomicin is primarily used in proteomic studies for the capture, identification and target validation of proteasome complexes, to determine the intracellular targets of epoxomicin. Epoxomicin acts as a proteasome inhibitor and NF-κB inhibitor, which effectively blocks inflammatory responses in mouse ear edema assays. It inhibits proteasome activity via covalent binding to catalytic subunits including LMP7, X, MECL1 and Z, with the strongest inhibitory effect on chymotrypsin-like activity, and does not interfere with non-proteasomal proteases such as trypsin and papain.

DPLG3 is a specific chymotryptic-like β5i subunits inhibitor, with an IC₅₀ of 4.5 nM. DPLG3 inhibits mouse i-20S with IC₅₀ of 9.4 nM. DPLG3 downregulates the protein levels of NF-κB p50 and p65. DPLG3 can be used for immune disease research.

PSI (Proteasome Inhibitor 1) is a potent proteasome inhibitor. PSI inhibits the proliferation of primary effusion lymphoma (PEL) cells. PSI has the potential for the research of Kaposi’s sarcoma-associated herpesvirus (KSHV) infection and KSHV-associated lymphomas.

Bepridil (CERM 1978 (free base); Org 5730) is an orally active non-selective calcium channel antagonist with multi-ion channel blocking activity. Bepridil modulates Calmodulin, the 20S proteasome, T-type/L-type calcium channels, cardiac sodium channels, multiple potassium channels, γ-secretase, β-secretase, and mitoK_ATP/sarcK_ATP channels. Bepridil acts as a hydroxyl radical scavenger, regulates mitochondrial and intracellular calcium handling, and exerts antiarrhythmic, antianginal, and cardioprotective effects. Bepridil alters amyloid precursor protein processing, reduces β-amyloid and thalamic calcium levels, restores seladin-1/DHCR24 expression, and improves sensorimotor recovery after cerebral ischemia. Bepridil also exhibits potent inhibitory effects on SARS-CoV-2 replication. Bepridil is used in studies related to stable angina, arrhythmias, cerebral ischemia, Alzheimer's disease, and SARS-CoV-2 infection.

Bortezomib-pinanediol is a proteasome inhibitor and a prodrug of Bortezomib (HY-10227). Bortezomib-pinanediol inhibits cell growth and can be used for study of multiple myeloma.

Calpain Inhibitor VI (SJA6017) is a synthesized peptide aldehyde inhibitor of calpain. Calpain Inhibitor VI inhibits purified m-calpain with the IC₅₀ of 80 nM. Calpain Inhibitor VI can be used for the research of cataract.

PI-1840 is a potent and selective chymotrypsin-like (CT-L) inhibitor for with an IC₅₀ value of 27 nM. PI-1840 inhibits cell proliferation and arrest cell cycle at G2/M phase. PI-1840 induces apoptosis and induces autophagy. PI-1840 induces the accumulation of proteasome substrates p27, Bax, and IκB-α.

Aclacinomycin A (Aclarubicin) hydrochloride is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A hydrochloride is an inhibitor of topoisomerase I and II. Aclacinomycin A hydrochloride inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A hydrochloride might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis.