Proteasome Inhibitor

A-933548 is a potent and selective inhibitor of calpain, with a K_i of 18 nM. A-933548 can be used for the research of Alzheimer's disease.

FK-448 Free base is an effective and specific inhibitor of chymotrypsin, with an IC₅₀ of 720 nM.

MG-101 (GMP) (Calpain inhibitor I (GMP)) is MG-101 (HY-18964) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. MG-101 (ALLN) is an inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with K_is of 190, 220, 150 and 500 pM, respectively. MG-101 induces apoptosis and inhibits tumor growth, it can be used for the research of colon cancer.

8304-vs is a macrocyclic anti-Plasmodial agent that covalently and irreversibly targets the Plasmodium proteasome. 8304-vs effectively inhibits the growth of Plasmodium falciparum.

Dihydroeponemycin, an analogue of the antitumor and antiangiogenic natural product eponemycin, selectively targets the 20S proteasome. Dihydroeponemycin covalently modifies a subset of catalytic proteasomal subunits, binding preferentially to the IFN-gamma-inducible subunits LMP2 and LMP7. Dihydroeponemycin-mediated proteasome inhibition induces a spindle-like cellular morphological change and apoptosis.

Z-Gly-Pro-Phe-Leu-CHO (Z-GPFL-CHO) is a tetrapeptide aldehyde that acts as a highly selective and potent proteasomal inhibitor (K_i = 1.5 µM for branched chain amino acid preferring, 2.3 µM for small neutral amino acid preferring, and 40.5 µM for chymotrypsin-like activities; IC₅₀ = 3.1 µM for peptidyl-glutamyl peptide hydrolyzing activity).

DD1, a proteasome inhibitor, targets Bax activation and P70S6K degradation during acute myeloid leukemia (AML) apoptosis. DD1 induces apoptosis in the caspase-dependent manner. DD1 induces mitochondrial membrane depolarization and Bad dephosphorylation.

NC-002, a cell-permeable peptide, is a Trypsin-like proteasome inhibitor without inhibition of lysosomal cysteine proteases. NC-002 is the epoxyketone derivative of Leupeptin (HY-18234). NC-002 sensitizes myeloma cells to Bortezomib (HY-10227) and Carfilzomib (HY-10455). NC-002 can be used for cancers research.

Cyclotheonellazole A is a natural macrocyclic peptide and a potent elastase inhibitor (IC₅₀=0.034 nM). Cyclotheonellazole A inhibits chymotrypsin with an IC₅₀ value of 0.62 nM.

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

(+)-Catechin 3-gallate is an orally active polyphenolic compound that acts as a non-selective proteasome inhibitor. (+)-Catechin 3-gallate exerts antitumor effects by inducing apoptosis and suppressing inflammatory cytokines. (+)-Catechin 3-gallate is promising for research of cancers (e.g., breast, prostate) and neurodegenerative diseases (e.g., Alzheimer’s).

UR238 is a proteasome inhibitor. UR238 reduces levels of the immunomodulator HE4. UR238 decreases PDL1 expression on cells. UR238 exhibits anticancer activity against epithelial ovarian cancer.

Z-Leu-Leu-Tyr-COCHO is a potent chymotrypsin-like activity inhibitor with a K_i value of 3.0 nM.

JBIR-22 is a protein-protein interaction inhibitor of proteasome assembly factor 3 homodimer, which has the activity of inhibiting this interaction and exerting long-term cytotoxicity against human cervical cancer cell lines, and its stereochemical structure has been determined by total synthesis.

CEP1612 is a dipeptidyl proteasome inhibitor with the IC₅₀ of 60 nM. CEP1612 induces p21(WAF1)and p27(KIP1) expression and cell apoptosis. CEP1612 shows anticancer activity in vivo.

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

Isoginkgetin (Standard) is the analytical standard of Isoginkgetin. This product is intended for research and analytical applications. Isoginkgetin is a pre-mRNA splicing inhibitor inhibitor. Isoginkgetin also inhibits activities of both Akt, NF-κB and MMP-9. Isoginkgetin inhibits the activity of the 20S proteasome, induces apoptosis and activates autophagy.

SAP2-IN-1 is a secreted aspartic protease 2 (SAP2) inhibitor and has potent SAP2 inhibitory activity with an IC₅₀ value of 0.92 μM. SAP2-IN-1 also is a virulence factor inhibitor and is inactive in vitro. SAP2-IN-1 can be used for the research of infection.

INVA8001 (ASB17061) is a highly selective and orally active chymase inhibitor with IC₅₀ values for human chymase and mouse mast cell proteinase 4 (mMCP-4) of 0.02 and 0.03 μM, respectively. INVA8001 exhibits IC₅₀ values for bovine α-chymotrypsin and human cathesin G of 3.4 and 32.1 μM, respectively, and it shows over 1000-fold selectivity for other related serine proteases. INVA8001 inhibits mast cells in a mouse primary sclerosing cholangitis (PSC) model, improves bile duct pathology, and alleviates bile stasis, demonstrating anti-inflammatory and anti-fibrotic effects.

DB-310 is a selective immunoproteasome LMP2 inhibitor with an IC₅₀ value of 80.62 nM. DB-310 inhibits the production of IL-1α in microglia. DB-310 improves cognitive function in the Tg2576 transgenic mouse model of Alzheimer's disease. DB-310 can be used for research related to Alzheimer's disease.