20s

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.

(20S)-Protopanaxadiol (20-Epiprotopanaxadiol) (20-Epiprotopanaxadiol), an apoptosis inducer, is an aglycon metabolic derivative of the protopanaxadiol-type ginseng saponin.

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).

TCH-165 is a small molecule modulator of proteasome assembly, resulting in an increase in 20S levels. The increase in the level of free 20S corresponds to enhanced proteolysis of IDPs.

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.

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.

Alloxan Monohydrate is a diabetogenic agent that acts as a proteasome inhibitor and induces diabetes in experimental animals by damaging the insulin-secreting β-cells in the pancreas. It is commonly used to establish diabetes models.

(1S,2S)-Bortezomib (Bortezomib) is an enantiomer of Bortezomib. Bortezomib is a reversible and selective inhibitor of the proteasome with a Ki of 0.6 nM for 20S proteasome.

Marizomib is a novel irreversible brain-permeable proteasome inhibitor that inhibits CT-L (β5), CT-T-laspase-like (C-L, β1), and trypsin-like (T-L, β2) 20S proteasomes with IC50s of 3.5, 28, and 430 nM.[3]

MLN2238 suppresses the chymotrypsin-like proteolytic (β5) site of the 20S proteasome(Ki50=0.93 nM, IC50=3.4 nM/). The biologically active form of MLN9708 (Ixazomib Citrate) is MLN2238 in aqueous solutions or plasma.

20-Hydroxyvitamin D3 (20(OH)D3) is a hydroxy metabolite of vitamin D3. It functions as a ligand for the vitamin D receptor (VDR), aryl hydrocarbon receptor (AhR), liver X receptor (LXR), and retinoic acid receptor-related orphan receptor (ROR). 20-Hydroxyvitamin D3 inhibits cell proliferation and induces differentiation. It is applicable in research on inflammatory and autoimmune diseases.

Ixazomib (MLN2238) , a second generation, boron-containing peptide proteasome inhibitor (PI), inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome (IC50/Ki: 3.4/0.93 nM, in cell-free assays), also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites (IC50: 31/3500 nM).

MG-115 (Z-LL-Nva-CHO) is a potent and reversible inhibitor of proteasome , with K i s of 21 nM and 35 nM for 20S and 26S proteasome, respectively. MG-115 specifically inhibit the chymotrypsin-like activity of the proteasome, induces p53-dependent apoptosis [1] [2] [3].

Ginsenoside Rg2 (Chikusetsusaponin I) is one of the major active components of ginseng, act as an NF-κB inhibitor.

Ginsenoside Rh2 (20(S)-Ginsenoside Rh2), an extract of red Panax ginseng, is a potent anti-inflammatory and anticancer drug.

20(S)-Ginsenoside Rg3 (Rg3) possess an ability to inhibit the lung metastasis of tumor cells via inhibition of the adhesion and invasion of tumor cells. It inhibits the proliferation of human umbilical vein endothelial cells(HUVEC) and has anti-angiogenesis activities.

Oprozomib (PR-047) (ONX 0912) , an inhibitor for CT-L activity of 20S proteasome β5(IC50=36 nM)/LMP7(IC50=82 nM), is orally bioavailable. Oprozomib also has potential antineoplastic activity.

Epoxomicin (BU-4061T,Aids010837) is a selective proteasome inhibitor with anti-inflammatory activity, inhibits primarily the CH-L activity of the 20S proteasome, while T-L and PGPH catalytic activities are also inhibited at 100- and 1000-fold reduced rate.

20S Proteasome-IN-5 (Compound 5) is a macrocyclic inhibitor of the 20S proteasome, with IC50 values of 0.19 μM for chymotrypsin-like (ChT-L) activity and 52.5 μM for peptidylglutamyl-peptide hydrolyzing-like (PGPH-L) activity.

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].

(20S)-Protopanaxadiol-3-one is a natural compound isolated from Melia azedarach and Betula pendula [1].

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.

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.