Proteasome Inhibitor

Alicapistat (Standard) is the analytical standard of Alicapistat (HY-109001). This product is intended for research and analytical applications. 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.

JBJ-08-178-01 is a mutant-selective tyrosine kinase inhibitor against human epidermal growth factor receptor 2 (HER2) with an antitumoral activity. JBJ-08-178-01 reduces both the kinase activity and protein levels of HER2 by inducing proteasomal degradation of the receptor in lung cancer. JBJ-08-178-01 is promising for research of non-small-cell lung cancer.

Proteasome-IN-1 (Compound 130) is a proteasome inhibitor. Proteasome-IN-1 exhibits antiparasitic activity against P. faciparum 3D7.

Ixazomib-¹³C₂,¹⁵N is ¹³C and ¹⁵N labeled Ixazomib. Ixazomib (MLN2238) is a selective, potent, and reversible proteasome inhibitor, which inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC₅₀ of 3.4 nM (K_i of 0.93 nM).

Proteasome-IN-6 (Compound J-80) inhibits the β5 catalytic subunit of the Trypanosoma brucei 20S proteasome, inibits T. b. brucei, T. b. gambiense and T. b. rhodesiense with EC₅₀s of 157 nM, 220 nM and 156 nM, respectively. Proteasome-IN-6 exhibits antitrypanosomal activity in mouse model.

10-Undecenoic acid (zinc salt) (Standard) is the analytical standard of 10-Undecenoic acid (zinc salt). This product is intended for research and analytical applications. 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.

Pf20S-IN-1 is a selective inhibitor of the 20S proteasome β5 subunit of Plasmodium falciparum. Pf20S-IN-1 exhibits antiparasitic activity against Plasmodium falciparum, with an EC₅₀ of 20.1 nM against the Plasmodium falciparum W2 strain. Pf20S-IN-1 shows weak inhibitory effect on human 20S proteasome, has no obvious toxicity to human foreskin fibroblasts (HFF), and has a selectivity index > 25000. Pf20S-IN-1 can be used in malaria research.

(R)-MG-132 (Standard) is the analytical standard of (R)-MG-132 (HY-13259C). This product is intended for research and analytical applications. (R)-MG-132 ((S,R,S)-(-)-MG-132) is the enantiomer of MG-132. (R)-MG-132 is a proteasome inhibitor with weaker cell cytotoxicity than MG-132.

Proteasome inhibitor IX (Standard) is the analytical standard of Proteasome inhibitor IX (HY-107412). This product is intended for research and analytical applications. 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.

Capzimin (Standard) is the analytical standard of Capzimin (HY-110404). This product is intended for research and analytical applications. Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor.

WZ-1831 is a selective inhibitor of the constitutive proteasome β5c subunit (IC₅₀ 0.01 μM). WZ-1831 exhibits anticancer activity against multiple myeloma. WZ-1831 synergizes with the β5i-selective inhibitor PKS21265 to induce cytotoxicity. WZ-1831 can be used for research on multiple myeloma.

Kaempferidinidin chloride is a chymotrypsin-like site inhibitor of the Proteasome. Kaempferidinidin chloride can be used in the research of neurodegenerative diseases.

Calpeptin (Standard) is the analytical standard of Calpeptin. This product is intended for research and analytical applications. Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID50 of 40 nM for Calpain I in human platelets. Calpeptin is also an inhibitor of cathepsin K.

Argyrin A, a cyclical peptide, is a potent antitumoral agent. Argyrin A exerts its effects through a potent inhibition of the proteasome. Argyrin A leads to increased endogenous p27^kip1 levels by preventing protein turnover.

Phepropeptin A, a microbial secondary metabolite, is a proteasome inhibitor with an IC₅₀ of 21 μg/mL.

Phepropeptin C, a microbial secondary metabolite, is a proteasome inhibitor with an IC₅₀ of 12.5 μg/mL.

BI-1942, a chemical probe, is a chymase inhibitor and has an IC₅₀ of 0.4 nM for human chymase. BI-1942 can be used in the research of ophthalmic diseases.

KZR-504 (Standard) is the analytical standard of KZR-504 (HY-101786). This product is intended for research and analytical applications. 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.

SARS-CoV-2 3CLpro-IN-34 (Compound 55) is a highly efficient non-covalent inhibitor of the SARS-CoV-2 3CL^pro protease (b. SARS-CoV-2 3CL^pro protease) with an IC₅₀ of 1.9 μM. SARS-CoV-2 3CLpro-IN-34 can inhibit the 3CL^pro protein of SARS-CoV-1, with its IC₅₀ being 3.2 μM, and it shows high selectivity towards host cysteine proteases (such as cathepsins L/K and calpain). SARS-CoV-2 3CLpro-IN-34 exhibits antiviral activity in cells infected with SARS-CoV-2, with its EC₅₀ being 25 μM, and it is not affected by P-gp inhibitors and shows no significant cytotoxicity. SARS-CoV-2 3CLpro-IN-34 can be used for research on SARS-CoV-2 infection.

RA190 (Standard) is the analytical standard of RA190 (HY-100739). This product is intended for research and analytical applications. RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.