ht22

B355252 protects against cell death caused by glutamate-evoked oxidative stress. B355252 shows neuroprotective effect, potentiating nerve growth factor (NGF)-induced neurite outgrowth.

(-)-Epigallocatechin Gallate (EGCG) is a phenolic antioxidant polyphenol flavonoid found in plants such as green and black tea, which inhibits telomerase and DNA methyltransferase, blocks the activation of EGF receptors and HER-2 receptors, inhibits cellular oxidation, and prevents free radical damage to cells.

Ferrostatin-1 (Fer-1) is a potent and selective inhibitor of iron death. Ferrostatin-1 potently inhibits Erastin-induced iron death in HT-1080 cells with an EC50 of 60 nM. Ferrostatin-1 also exhibits antioxidant and antifungal activities.

GNF4877 is a potent inhibitor of DYRK1A and GSK3β (IC50s: 6 nM and 16 nM, respectively), resulting in the blockade of nuclear export of nuclear factor of activated T-cells (NFATc) and increased β-cell proliferation.

Mirodenafil is a PDE-5 inhibitor developed for the treatment of erectile dysfunction.

Mirodenafil dihydrochloride is a PDE-5 inhibitor developed for the treatment of erectile dysfunction.

Aloenin B, a compound isolated from the leaves and roots of Aloe vera, has neuroprotective activity against glutamate-induced neuronal death in HT22 cells.

CMS-121, a quinolone derivative, is an orally active acetyl-CoA carboxylase 1 (ACC1) inhibitor. CMS-121 protects HT22 cells against ischemia and oxidative damage (EC50: 7 nM and 200 nM). CMS-121 shows strong neuroprotective, antioxidative, anti-inflammatory, and renoprotective activities.

GIF-0726-r is a novel compound that inhibits the accumulation of reactive oxygen species (ROS). In preclinical trials, this compound has been shown to protect the mouse hippocampal cell line HT22, combating oxidative stress and ferroptosis damage.

HBV-IN-44 (Compound (S)-2a) is an HBV inhibitor with an IC50 value of 23 nM against HbsAg. It exhibits minimal toxicity in HT22 cells and in the neurite outgrowth of ex vivo mouse DRG neurons.

P2Y1 antagonist 4 is a selective blocker of the P2Y1 receptor with excellent penetration across the blood-brain barrier. It inhibits ADP-induced increases in cytosolic Ca2+ mediated by the P2Y1 receptor in washed rabbit platelets (IC50 = 1.95 μM) and platelet aggregation (IC50 = 3.24 μM). P2Y1 antagonist 4 significantly elevates nuclear Nrf2 protein levels in H2O2-treated HT22 cells. It reduces infarct size in a mouse acute myocardial infarction model and is applicable in research on ischemic stroke and myocardial infarction.

MAO-B-IN-49 is a selective, reversible MAO-B inhibitor with an IC50 of 1 nM for human MAO-B. It demonstrates significantly higher selectivity for MAO-B over MAO-A (IC50 = 633.9 nM). MAO-B-IN-49 reduces lipopolysaccharide (LPS)-induced ROS production in HT22 cells. It possesses notable neuroprotective properties and significantly improves motor dysfunction in MPTP-induced Parkinson's disease (PD) mouse models. MAO-B-IN-49 is applicable for Parkinson's disease research.

PICK1 PDZ-IN-1 (Compound 6b) is a selective inhibitor of the protein kinase C binding protein 1 (PICK1 PDZ) domain that can cross the blood-brain barrier, with a Ki value of 27.73 μM. It competitively inhibits the interaction between PICK1 and the GluA2 subunit of AMPA receptors. This compound enhances the survival rate of glutamate-induced HT22 cells and primary cortical neuronal cells while inhibiting ROS production. PICK1 PDZ-IN-1 exhibits neuroprotective effects by reducing the area of cerebral infarction and is applicable in ischemic stroke research.

DYRK2-IN-2 (Compound C17) is a selective inhibitor of DYRK2 with an IC50 of 40.3 nM. It exhibits significantly lower inhibitory activity against DYRK1A (IC50 = 1842 nM), DYRK1B (IC50 = 1335 nM), DYRK4 (IC50 = 1931 nM), DYRK3 (IC50 = 112 nM), and CLK proteins (IC50 = 540-6496 nM). DYRK2-IN-2 hinders the phosphorylation of Tau protein at Thr212 and demonstrates moderate cytotoxicity in HT22 cells. This compound is suitable for cancer research.

RC363 is an inhibitor of ferroptosis and a derivative of the antioxidant and hypocholesterolemic agent probucol .1It reduces 2,2-diphenyl-1-picrylhydrazyl radicals by approximately 40% in a cell-free assay when used at a concentration of 25 μM. RC363 prevents glutamate-induced toxicity in HT22 cultured hippocampal cells (IC50= 234.5 nM) but does not reduce oxidant levels in these cells. It increases the levels of glutathione peroxidase 1 (GPX1) and the activity of GPX in glutamate-challenged HT22 cells when used at a concentration of 3 μM. RC363 inhibits ferroptosis induced by the GPX4 inhibitor RSL3 in HT22 cells (IC50= 173.6 nM). 1.Bueno, D.C., Canto, R.F.S., de Souza, V., et al.New probucol analogues inhibit ferroptosis, improve mitochondrial parameters, and induce glutathione peroxidase in HT22 cellsMol. Neurobiol.57(8)3273-3290(2020)

Jatrorrhizine chloride (Neprotine chloride) is a potent and orally active uptake-2 transporter inhibitor. It exhibits a critical neuroprotective role in H2O2-induced apoptosis via inhibition of the MAPK pathway in HT22 hippocampal neurons.

1. Isocorynoxeine (7-Isocorynoxeine) shows the effects of lowering blood pressure, vasodilatation, and protection against ischemia-induced neuronal damage. 2. Isocorynoxeine exhibits a significant neuroprotective effect against glutamate-induced HT22 cell death at the maximum concentration.

CP21 is an iron chelator that binds to iron in a 3:1 (ligand:iron) ratio. It is active against P. falciparum when used at concentrations of 10 and 100 µM. CP21 inhibits production of prostaglandin I2 induced by epinephrine, arachidonic acid, or A23187 in isolated rat aortic rings with IC50 values of 1.3, 1.3, and 1.4 mM, respectively. It inhibits glutamate-induced oxytosis, as well as decreases iodoacetic acid-induced cytotoxicity in an in vitro model of ischemia, in HT22 mouse hippocampal cells (EC50s = 13 and 9.5 µM, respectively). CP21 (200 mg/kg) increases the excretion of iron, but not copper, zinc, calcium, or magnesium, in rabbits.

Compound 3, 2,5-Dihydroxy-4-methoxyacetophenone, is isolated from the 80% methanol extract of the roots of Cynanchum paniculatum Kitagawa and has been shown to inhibit glutamate-induced cytotoxicity in the hippocampal HT22 cell line [1].

Aβ42 agonist-2 is a protein aggregation modulator that promotes Aβ42 aggregation. It facilitates non-toxic fibril formation to protect hippocampal neurons from Aβ42-induced toxicity.

(+)-Afzelechin (Afzelechin) is isolated from Eysenhardtia subcoriacea. It is an α-glucosidase activity inhibitor, offering neuroprotective effects against glutamate-induced neurotoxicity in HT22 cells and improving reduced glutathione levels in rat pancreas homogenates.

Effusol is a natural product, exhibits potent scavenging activity for DPPH and ABTS radicals(IC50 values of 79 μM and 2.73 μM, respectively). Effusol rescues CA1 LTP attenuated by corticosterone, defending the hippocampal function against stress-induced cognitive decline. Effusol can induce caspase-3-mediated cytotoxicity in HT22 cells.

1,7-Diphenyl-4-hepten-3-one is a compound isolated from Alpinia officinarum, which activates the Nrf2 pathway to suppress pyroptosis. It alleviates cognitive impairment and pathological damage in APP/PS1 mice and prevents oxidative stress damage while reducing levels of pyroptosis-related proteins. 1,7-Diphenyl-4-hepten-3-one enhances Aβ-induced proliferation in HT22 cells and can be used in Alzheimer’s disease research.

Morachalcone A displays significant tyrosinase inhibitory activity (IC50, 0.013 uM); it also exerts strong pancreatic lipase inhibition with IC 50 value of 6.2 uM. Morachalcone A exhibits neuroprotective effects on HT22-immortalized hippocampal cells agai