overload

Deferasirox (CGP-72670) is an oral iron chelating agent used to treat chronic iron overload.

Deferitrin (GT-56-252) is an iron chelator. It potentially for the treatment of thalassemia and iron overload.

CP-060 is a potent Ca2+ antagonist and inhibits Ca2+ overload with antioxidant and cardioprotective activities.

HBED (CHELII) is an iron chelator and can be used in research on the treatment of chronic iron overload and acute iron poisoning.

Ammonium iron(III) citrate (Ferric ammonium citrate) is a physiological form of non-ferritin-bound iron that causes intracellular iron overload leading to cellular ferroptosis and enhances protein production.

Aniline-D5 is a deuterated isotope marker of Aniline (T207053), which can be used for isotope tracing.Aniline induces toxicity to the spleen through iron overload and oxidative stress via heme oxygenase 1 up-regulation and is able to lead to a significant increase in p-IKKα and p-IKKβ, which in turn increases NF-κB and AP-1 binding activity.

Deferasirox (Fe3+ chelate) is an orally available iron chelator with potential anticancer activity, inhibits the anti-apoptotic activity of MCL-1, and can be used to study iron overload.

Bufalin is a natural product and a Na⁺/K⁺-ATPase inhibitor (IC50 ≈ 40–45 nM) with favorable cell permeability. By binding to α subunits such as ATP1A1, bufalin induces calcium overload and pyroptosis, and can be used for experimental research and therapeutic exploration in various cancers.

O-Desmethylcarvedilol (Desmethylcarvedilol) is an active metabolite of Carvedilol, a non-selective β-adrenergic receptor (β-AR) antagonist. This compound inhibits store overload-induced calcium release in HEK293 cells expressing the RyR2 R4496C mutation (IC50= 7.62 µM). Additionally, O-Desmethylcarvedilol slows the increase in heart rate and prevents diastolic pressure reduction induced by Isoproterenol in conscious rabbits (ED50s = 32 and 5 µg/kg).

CALR ligand 1 (Compound 2a) is a calreticulin (CALR) ligand with anti-tumor activity against triple-negative breast cancer (TNBC) cells, exhibiting an IC50 of 0.1 μM. It induces intracellular calcium overload, leading to apoptosis in TNBC cells, making it a promising candidate for further research on triple-negative breast cancer.

CS47 is a reversible inhibitor of thioredoxin reductase 1 (TrxR1). It activates stress-responsive glutathione (GSH) and iron regulatory pathways, leading to GSH depletion. This results in reactive oxygen species (ROS) accumulation, promoting HO-1 overexpression and causing intracellular iron overload, which ultimately induces ferroptosis in lung cancer not dependent on the KRAS gene. CS47 exhibits anticancer activity with low cytotoxicity to normal lung fibroblasts.

ZA18 is a selective TRPM2 channel inhibitor with an IC50 value of 6.2 μM. It effectively suppresses intracellular Ca2+ overload triggered by TRPM2 channel activation and significantly reduces H2O2-induced cell death in SH-SY5Y cells. ZA18 is applicable for research on ischemia-reperfusion injury, inflammation, or other neurodegenerative diseases.

ZA10 is a selective TRPM2 channel inhibitor with an IC50 value of 8.1 μM. It effectively suppresses intracellular Ca2+ overload caused by TRPM2 channel activation. Furthermore, ZA10 significantly reduces the death rate of SH-SY5Y cells induced by H2O2. This compound is useful for research on ischemia-reperfusion injury, inflammation, or other neurodegenerative diseases.

WGU55 is a selective and potent reversible type II transmembrane serine protease TMPRSS6 inhibitor with a Ki value of 12.15 nM. In KEK293 cells, WGU55 inhibits TMPRSS6 activity with an IC50 value of 138 nM. It displays a Ki value of 3510 nM for the homologous protease matriptase (SI=289) and a Ki value of 5.2 μM for the key coagulation protease factor Xa. WGU55 is applicable in the study of iron overload-related diseases, such as hereditary hemochromatosis.

Deferitazole magnesium is a potential chelator for iron overload treatment.

Secoisolariciresinol diglucoside (LGM2605) was cytoprotective in an in vitro model of iron overload-induced redox-inflammatory damage. Secoisolariciresinol diglucoside (25 mg/kg b.w.) exerts the antihyperglycemic effect by preventing the liver from peroxidation damage through inhibition of ROS level mediated increased level of enzymatic and non-enzymatic antioxidants.

Epsilon-V1-2 has been extensively investigated for its function as a PKC epsilon (PKCε) inhibitor. Epsilon-V1-2 has been widely applied in studies addressing ovarian aging, apoptosis in human granulosa cells, cerebral ischemia-reperfusion injury, brain development, hepatocyte insulin signaling, and neuronal cell death under ischemic conditions. Epsilon-V1-2 has been shown to effectively reduce PKCε activity, thereby enabling detailed exploration of regulatory pathways involving mitochondrial dynamics, calcium overload, AKT activation, brain atrophy, insulin resistance, and ferroptosis. Epsilon-V1-2 demonstrates notable therapeutic relevance in models of stroke, SHORT syndrome, hepatic steatosis, and brain injury, supporting its continued evaluation as a potential pharmacological agent across multiple disease contexts.

4-(3-Methyl-5-oxo-2-pyrazolin-1-yl)benzoic acid demonstrates hypoglycemic activity by acting through a mechanism reliant on the response to oral glucose overload.

CYP11B1-IN-2 (compound 7aa) is a selective, orally active inhibitor of CYP11B1 with an IC50 of 9 nM for human CYP11B1 and 25 nM for rat CYP11B1. It can be used to study diseases caused by cortisol overload.

NP-04634 is a calcium antagonist and protective agent against calcium overload and mitochondrial disruption.

Ferulic acid 4-O-sulfate (Ferulic acid 4-sulfate) is a metabolite of Ferulic acid.Ferulic acid 4-O-sulfate relaxes arteries, lowers blood pressure, and resists oxidative stress under conditions of iron overload in mice and HepG2 cells.Ferulic acid 4-O-sulfate is a metabolite of Ferulic acid.

HAPSBC is a potent iron chelator of the aromatic hydrazide class with high binding affinity. It induces cellular stress by depriving cells of essential iron, used in cancer metabolism and iron overload research.

Folic acid disodium is a water-soluble and essential B-complex vitamin for the human body, playing a key role in DNA synthesis and cell division. It is used to treat anaemia and foetal neural tube defects (NTDs) caused by folate deficiency.

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.