Alloxan

Alloxan is a 26S and 20S proteasome (proteasome) inhibitor and diabetes inducer. Alloxan directly inhibits the chymotrypsin-like and trypsin-like peptidase activities of purified proteasomes. Alloxan induces the accumulation of ubiquitinated proteins by impairing proteasome function. Alloxan is taken up by pancreatic β cells, increases ROS levels, triggers necrosis, reduces insulin production and induces β cell death. Alloxan induces vertebral tissue damage, chondrocyte disorder and growth retardation in rat offspring. Alloxan can be used in research related to type 1 diabetes and diabetes^[1][2][3]. In Vitro:Alloxan (5 mM; 24 h) causes significant accumulation of ubiquitinated proteins in NRK cells, indicating impaired ubiquitin-proteasome system function^[1].
Alloxan (10 mM; 0-7 hours) significantly slows the clearance of proteasome-specific substrate GFP-CL1 in 293 cells, confirming impairment of ubiquitin-proteasome system function^[1].
Alloxan (5 mM; 24 h) significantly inhibits chymotrypsin-like and trypsin-like peptidase activities in NRK cell nuclear extract^[1].
Alloxan (1 μM-333 mM) dose-dependently inhibits chymotrypsin-like and trypsin-like peptidase activities in NRK cell nuclear extract in vitro, with maximum inhibition observed at 3.3 mM^[1].
Alloxan (5 mM; 30 min) inhibits proteasomal degradation of GST-Sp1 in NRK cell nuclear extract in vitro^[1].
Alloxan (1 μM-333 mM) directly and dose-dependently inhibits chymotrypsin-like and trypsin-like peptidase activities of purified 26S proteasomes in vitro^[1].
Alloxan (1 μM-333 mM) directly and dose-dependently inhibits chymotrypsin-like and trypsin-like peptidase activities of purified 20S proteasomes in vitro, indicating it acts on the catalytic core of the proteasome^[1]. In Vivo:Alloxan (150 mg/kg; i.p.; single injection) induces diabetes (maternal blood glucose >300 mg/dL) and causes significant growth retardation and structural/ultrastructural damage to lumbar vertebrae in offspring at newborn, 3-week-old, and 2-month-old ages, alongside pancreatic β-cell damage and reduced insulin expression^[2].
Alloxan (150 mg/kg; i.p.; single dose) induces stable hyperglycemia in Swiss albino mice, with eligible animals maintaining elevated blood glucose levels for at least 21 days^[3].