sh-sy5y

Deferoxamine Mesylate (DFOM) is an iron chelator and ferroptosis inhibitor. Deferoxamine Mesylate binds free iron into a stable complex and reduces iron accumulation. Deferoxamine Mesylate up-regulates HIF-1α levels and induces apoptosis.

Olanzapine (LY170053) is an atypical antipsychotic that is used currently in the treatment of schizophrenia and bipolar illness.

Bilobalide ((-)-Bilobalide), a bioactive from Gingko Biloba, is active on hypoxia-induced alterations.

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

PKR-IN-C16 is a specific protein kinase (PKR) inhibitor. PKR-IN-C16 is able to inhibit the autophosphorylation of PKR and unlock the translation blockade induced by PKR in primary neuronal cultures.PKR-IN-C16 binds the ATP-binding site of PKR and blocks autophosphorylation with an IC50 value of 186-210 nM. PKR-IN-C16 protects human neuroblastoma cells against cell damage triggered by tunicamycin-mediated endoplasmic reticulum stress.

Apostatin-1 (Apt-1) is a novel TRADD inhibitor that binds to a pocket on the N-terminal TRAF2 binding domain of TRADD.

Rutin (Quercetin 3-O-rutinoside), a flavonoid, has a variety of biological activities including antiallergic, anti-inflammatory, antiproliferative, and anticarcinogenic properties.

Lipopolysaccharides (LPS), derived from Escherichia coli O55:B5, are essential components of the outer membrane of Gram-negative bacteria. Composed of lipid A, a core oligosaccharide, and an O-specific polysaccharide, LPS exhibits strong immunogenicity. It activates immune cells via the TLR4 receptor, induces chemotactic cell migration and cytokine secretion, and helps maintain the integrity of the bacterial outer membrane, protecting against bile salts and lipid-based antibiotics. LPS is commonly used to establish inflammatory models, including arthritis, chronic obstructive pulmonary disease (COPD), acute respiratory distress syndrome (ARDS), and gastrointestinal disease models.

SCH772984 is an ERK inhibitor that inhibits ERK1 and ERK2 (IC50=4/1 nM) and is highly selective and ATP-competitive. SCH772984 exhibits antitumor activity against BRAF or RAS mutant cells.

SAK3 is a novel modulator of nAChR activity that enhances T-type voltage-gated Ca2+ channel (T-VGCC) activity, and has potentiating effects on both Cav3.1 and Cav3.3 T-type Ca2+ channel currents.SAK3 is neuroprotective against scopolamine-induced cholinergic dysfunction in human neuroblastoma SH-SY5Y cells.SAK3 is used for the study of memory deficits and Alzheimer's disease. SAK3 can be used to study memory deficits and Alzheimer's disease.

Vutiglabridin (HSG4112) is a novel and safe modulator of PON2, a racemic compound. vutiglabridin is an optimized structural analogue of Glabridin and is superior to Glabridin in terms of weight loss and chemical stability. vutiglabridin ameliorates mptp-induced neurodegeneration in Parkinson's disease mice by targeting mitochondrial paraoxonase-2. Vutiglabridin is a clinical phase 2 drug for the treatment of obesity and has therapeutic effects on p-mitochondrial PON2 in a PD model. vutiglabridin penetrates the brain, binds PON2, and restores 1-methyl-4-phenylpyridine (MPP*)-induced neuroblastoma in SH-SY5Y Vutiglabridin significantly attenuated 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced dyskinesia and dopaminergic neuronal damage in mice modeled with PD in mouse experiments.

Zonisamide (AD 810), a sulfonamide anticonvulsant, is approved for use as an adjunctive treatment in adults with partial-onset seizures. It may inhibit a carbonic anhydrase although this is not one of the main mechanisms of action. Zonisamide may act by blocking repetitive firing of voltage-gated sodium channels results in a reduction of T-type calcium channel currents, or by binding allosterically to GABA receptors. This latter action may lower the uptake of the inhibitory neurotransmitter GABA while increasing the uptake of the excitatory neurotransmitter glutamate.

Oxidopamine hydrobromide (6-OHDA hydrobromide) is a widely used neurotoxin and an antagonist of the neurotransmitter dopamine. It selectively destroys dopaminergic neurons, promotes COX-2 activation, induces PGE2 synthesis, and stimulates the secretion of the pro-inflammatory cytokine IL-1β. It is commonly used to establish animal models of Parkinson’s disease (PD).

Trolox is a vitamin E analogue, used in reducing oxidative stress or damage.

Sodium dichloroacetate (BCA) , a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to derepress a mitochondrial potassium-ion channel axis, trigger apoptosis in cancer cells, and inhibit tumor growth.

Isoborneol (DL-Isoborneol) is a monoterpene alcohol, with neuroprotective and antiviral activities

MPP+ iodide, the metabolite of a neurotoxin MPTP, causes symptom of Parkinson's disease (PD) in animal models by selectively destroying dopaminergic neurons in substantia nigra. MPP+ induces dopamine transporter (DAT) externalization in dopaminergic (DA) neurons, but internalization of serotonin transporter (SERT) in serotonergic (5-HT) neurons. MPP+ induces autophagic cell death in SH-SY5Y cells.

Oxidopamine hydrochloride (6-Hydroxydopamine hydrochloride) is a widely used neurotoxin and an antagonist of the neurotransmitter dopamine. It selectively destroys dopaminergic neurons, promotes COX-2 activation, induces PGE2 synthesis, and stimulates the secretion of the inflammatory cytokine IL-1β. It is commonly used to establish animal models of Parkinson’s disease (PD).

AM 281, a cannabinoid antagonist, reduces neurologic dysfunction and mortality rate after cecal ligation and puncture in rats.

GPP78 is a potent inhibitor of Nampt (IC50: 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion). GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells (IC50: 3.8 nM by inducing autophagy). GPP78 has anti-cancer and anti-inflammatory effect

SIRT3 activator2 (compound 2a) acts as an activator of SIRT3. It is presumed to bind directly with SIRT3 in SH-SY5Y cells, as inferred through thermal stability, facilitating the SIRT3-dependent clearance of α-Syn. Furthermore, SIRT3 activator2 enhances motor functions in Parkinsonian mice and dose-dependently prevents the loss of dopaminergic (DA) neurons in the substantia nigra.

FO-4-15 is an activator of mGluR1 CaMKIIα. It exhibits protective effects against H2O2 in human neuroblastoma (SH-SY5Y) cells. In mice with Alzheimer's disease, FO-4-15 enhances cognitive function by activating the mGluR1 CaMKIIα pathway, reducing Aβ accumulation, Tau hyperphosphorylation, and synaptic damage.

ADH-353 inhibits Aβ fibrillization and mitigates Aβ-induced cytotoxicity in SH-SY5Y and N2a cells, making it useful for studies related to Alzheimer's disease.

HDAC6-IN-49 (Compound 3) is an inhibitor of HDAC, with IC50 values of 0.012 and 0.735 µM against HDAC6 and HDAC1, respectively. Additionally, it inhibits MAO-B, cholinesterase (ChE), histamine receptor (H3R), and serotonin 6 receptor (5-HT6R). HDAC6-IN-49 exhibits neuroprotective effects in SH-SY5Y cells and enhances cognitive functions and motor abilities in fruit fly models of Parkinson's disease and C. elegans models of Alzheimer's disease.