proteasome

Bortezomib (LDP 341) is a 20S proteasome inhibitor (Ki=0.6 nM) that is reversible and selective. Bortezomib has antitumor activity and inhibits NF-κB, which can disrupt the cell cycle and induce apoptosis.

MG-132 (Z-Leu-Leu-Leu-al) is a 26S proteasome inhibitor (IC50=100 nM) that is cell-permeable and reversible. MG-132 acts as an autophagy activator and also induces apoptosis.

Alloxan Monohydrate is a glucose analog used to induce diabetes by destroying beta-cells.

Tripterin (Celastrol) is a natural product, a proteasome inhibitor that inhibits the pancreatic rennet-like activity of the 20S proteasome (IC50=2.5 μM). Tripterin has anti-inflammatory, anti-infectious, and immunomodulatory properties.

Proteasome β2c i-IN-1 (compound 37) is a selective inhibitor of the β2c and β2i subunits of the human proteasome [1].

Proteasome-IN-5, also known as compound 5, acts as a proteasome inhibitor [1].

Proteasome-IN-6 (Compound J-80) inhibits the β5 catalytic subunit of the Trypanosoma brucei 20S proteasome, effectively blocking T. b. brucei, T. b. gambiense, and T. b. rhodesiense with EC50 values of 157 nM, 220 nM, and 156 nM, respectively. Additionally, Proteasome-IN-6 has demonstrated antitrypanosomal activity in a mouse model.

Proteasome-IN-7 (Compound 6f) is a macrolactam-based epoxyketone proteasome inhibitor with an IC50 value of 37.92 nM against the 20S proteasome ChT-L subunit. It exhibits potent antiproliferative effects on multiple myeloma, acute lymphoblastic leukemia, and non-small cell lung cancer.

Proteasome inhibitor IX (PS-IX) is an inhibitor of chymotrypsin-like activity of the 20S proteasome (IC50 ~1 μM). Proteasome inhibitor IX shows potent anticancer activity. Proteasome inhibitor IX exhibits HCT116 p53+ + cells growth inhibitory activity(IC50 = 1.49 μM).

PROTAC 20S proteasome subunit β5 degrader 2 is a PROTAC degrader targeting the 20S proteasome subunit β5 (20Sproteasomesubunit β5), with a DC50 of 0.16 μM. It inhibits the proliferation of FaDu cancer cells, showcasing an IC50 of 0.23 μM. Additionally, PROTAC20Sproteasomesubunit β5 degrader 2 demonstrates antitumor activity in a mouse model.

20S Proteasome activator 1 is a 20S proteasome activator with IC50 values of 0.3 μM for trypsin-like sites, 0.7 μM for chymotrypsin-like sites, and 1.8 μM for caspase sites. It prevents the accumulation of pathogenic alpha-synuclein (A53T) mutants through translation in the cellular system, thereby reducing the probability of disease occurrence. 20S Proteasome activator 1 can be used to study neurodegenerative diseases.

3-O-Feruloylquinic acid is a protease inhibitor, it exerts moderate inhibitory effect against AIV (H5N1) in vitro.

Proteasome-IN-1 is an inhibitor of proteasome.

Vepdegestrant (ARV-471) is an estrogen receptor (ER) α PROTAC molecule that degrades ER in ER-positive breast cancer cell lines with a DC50 of approximately 1 nM. It can reduce the expression of classically regulated ER target genes and inhibit the growth of ER-dependent cell lines (including those expressing ESR1 variants, such as Y537S and D538G) by degrading ER.

Lactacystin is a natural non-peptide proteasome inhibitor and highly specific anticancer drug that controls the UPS of cellular protein turnover and inhibits alkaline cell proliferation, and is able to be used as a model for studying dementia, induces neurite outgrowth and transiently elevated levels of cAMP, inhibits angiogenesis, triggers apoptosis in glioma cells, and can penetrate the blood-brain barrier (BBB).

PROTAC 20S proteasome subunit β5 degrader 1 (compound 12f) serves as a targeted degrader of the 20S proteasome subunit β5, exhibiting a DC50 value of 0.11 μM in FaDu cells. This compound disrupts the cell cycle and promotes apoptosis (apoptosis), while inhibiting cell proliferation and migration in both FaDu and KM3 BTZ cells. It is applicable for research into resistance to Bortezomib in pharyngeal carcinoma and multiple myeloma.

Proteasome-IN-3 is an inhibitor of proteasome-associated DUBs.

Proteasome-IN-4, a non-covalent proteasome inhibitor (IC 50 = 8.39 nM), exhibits potent antiproliferative effects on RPMI-8226, MM-1S, and MV-4-11 cell lines, making it valuable for cancer research.

Proteasome-activating peptide 1 enhances chymotrypsin-like proteasomal catalytic activity, boosting proteolytic rates both in vitro and within cultured cells. Additionally, it inhibits protein aggregation in a cellular model of amyotrophic lateral sclerosis [1].

Proteasome-activating peptide 1 TFA is a potent activator of the proteasome, enhancing chymotrypsin-like proteasomal catalytic activity and increasing proteolytic rates both in vitro and in culture. It also inhibits protein aggregation in cellular models of amyotrophic lateral sclerosis (ALS) [1].

20S Proteasome-IN-4 (Compound 7) is an orally active inhibitor of the 20S proteasome, selectively targeting the parasite form and demonstrating brain penetration capabilities. It exhibits a potent IC50 value of 6.3 nM against the T. b. brucei 20S proteasome, making it suitable for human African trypanosomiasis (HAT) research [1].

Immunoproteasome Activator 1 (compound A) is a selective immunoproteasome activator that enhances the presentation of individual MHC-I binding peptides by over 100 times. It binds to the proteasomal structural subunit PSMA1 and facilitates the association of the proteasome activators PA28α β (PSME1 PSME2) with the immunoproteasome.

Immunoproteasome inhibitor 1 is a highly potent and reversible inhibitor of both immunoproteasome and proteasome activity. It exhibits time-independent inhibitory effects on immunoproteasome subunits β5c, β1i, and β5i, with respective Ki values of 1.18 μM, 0.27 μM, and 1.91 μM. This compound shows promising potential for the treatment of select neoplastic diseases [1].

Aprotinin (Traskolan) is a broad-spectrum serine protease (BPTI) inhibitor that inhibits the activity of a number of different esterases and proteases. Aprotinin is an antifibrinolytic agent used to minimize hemorrhage during complex surgical procedures.