sh-sy5y cells

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).

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).

YM-244769 dihydrochloride is an effective inhibitor of Na+/Ca2+ exchange 3 (NCX3) with an IC50 of 18 nM. YM-244769 dihydrochloride has efficient protective effects on neurons and kidneys.

YM-244769 (3-Pyridinecarboxamide, N-[(3-aminophenyl)methyl]-6-[4-[(3-fluorophenyl)methoxy]phenoxy]-) is an effective inhibitor of Na+/Ca2+ exchange 3 (NCX3) with an IC50 of 18 nM. YM-244769 has efficient protective effects on neurons and kidneys.

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.

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.

Oligomycin A (MCH 32) is an inhibitor of ATP synthase, inhibits oxidative phosphorylation and all the ATP-dependent processes occurring on the coupling membrane of mitochondria.

Moracin P, a 2-arylbenzofuran derivative isolated from Mori Cortex Radicis, shows potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1). This compound reduces oxygen-glucose deprivation-induced reactive oxygen species generation while demonstrating neuroprotective and anti-inflammatory properties.

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.

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

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

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.

D-688 serves as an inhibitor of Tau and Aβ. It can reverse the cytotoxicity in SH-SY5Y cells induced by Aβ1–42, displaying significant neuroprotective characteristics. Additionally, D-688 enhances the survival rate of transgenic fruit flies expressing the human tau protein isoform (2N4R).

D-687 is an inhibitor of Tau and Aβ. It effectively reverses the cytotoxicity induced by Aβ1–42 in SH-SY5Y cells, demonstrating significant neuroprotective properties.

Aβ-IN-10 (Compound Alz-5) is a bifunctional copper chelator and an inhibitor of beta-amyloid (Aβ), interacting with Aβ aggregates to reduce their neurotoxicity. This compound also displays antioxidative properties and exhibits moderate cytotoxicity in SH-SY5Y and HepG2 cells in the presence of CuCl2, with IC50 values of 65.5 and 31.2 μM, respectively. Additionally, Aβ-IN-10 reduces the increase in cell rigidity caused by Aβ.

CL-13 is an inhibitor of butyrylcholinesterase (BChE), exhibiting an IC50 of 1.15 μM and a selectivity index (SI) of 9.2 for acetylcholinesterase. It demonstrates antioxidative activity in SH-SY5Y cells with a DPPHEC50 of 47.01 μM and has the capacity to chelate metals involved in Aβ aggregation and/or oxidative stress, showing no neurotoxicity at concentrations up to 50 μM. CL-13 can also reverse scopolamine-induced cognitive impairments without affecting motor abilities in mice.

Sesaminol is an orally active activator of the Nrf2-ARE signaling pathway, promoting the nuclear translocation of Nrf2 and boosting the expression of NQO1 to enhance cellular defense against oxidative stress. It inhibits 6-OHDA-induced ROS production and apoptosis in SH-SY5Y cells. Sesaminol also provides neuroprotective effects against Rotenone-induced Parkinson's disease.

(3R,5R)-Octahydrocurcumin (Compound 7) is a metabolite of Curcumin produced by gut microbiota. It exhibits neuroprotective effects against Aβ25-35-induced cell damage in SH-SY5Y cells and possesses anti-inflammatory properties in LPS-stimulated BV-2 mouse microglia.