20s proteasomes

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.

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.

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]

DPLG3, a specific inhibitor of the chymotryptic-like β5i subunits, effectively inhibits mouse i-20S proteasomes with an IC50 value of 9.4 nM. This compound has applications in the research of immune diseases [1].