Ferritin is a protein of 450 kDa consisting of 24 subunits that is present in every cell type. Invertebrates, these subunits are both the light (L) and the heavy (H) type with an apparent molecular weight of 19 kDA or 21 kDA respectively. The ferritin fou
Ap44mSe is a potent and selective antitumor agent. Ap44mSe effectively depletes cellular Fe, resulting in transferrin receptor-1 up-regulation, ferritin down-regulation, and increased expression of the potent metastasis suppressor, N-myc downstream regula
PBT434 is a novel, brain-penetrant, small molecule inhibitor of α-synuclein aggregation. In transgenic animal models of Parkinson disease (A53T) and MSA (PLP-α-Syn), PBT434 reduced α-synuclein aggregation, preserved neurons and improved motor function. Glial cell inclusions were also reduced in a murine MSA model. PBT434 is thought to act by redistributing reactive iron across membranes, thereby blocking intracellular protein aggregation and oxidative stress. The affinity of PBT434 for iron is greater than that of α-synuclein but lower than that of iron trafficking proteins, e.g., ferritin.
CP94, an iron chelator, enhances protoporphyrin IX photobleaching and reduces the viability of A431 squamous epithelial carcinoma cells at a 150 µM concentration with photodynamic therapy (PDT) using protoporphyrin IX precursors such as aminolevulinic acid (ALA), methyl aminolevulinate (MAL), or hexylaminolevulinate (HAL). Additionally, CP94 (2 mg ml in drinking water) lowers hepatic non-heme and ferritin-bound iron levels while increasing hepatic protoporphyrin levels in mice. It also counteracts ferrocene-induced rises in rat brain iron levels at a dosage of 100 mg kg.
CP102, an iron chelator, effectively reduces total non-heme and ferritin-stored iron levels in the livers of mice when provided through drinking water at a concentration of 2 mg ml.
CN128, an orally bioavailable iron chelator, features a side chain hydroxy group serving as an alternate sacrificial glucuronidation site to mitigate metabolic inactivation at the 3-hydroxy group. When administered at doses of 150 and 450 µmol kg, CN128 enhances iron mobilization by 24.8% in a 59Fe-ferritin-loaded rat model of iron overload.