pc12 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).

PD 90780 is a non-peptide antagonist of nerve growth factor (NGF) that interacts with NGF and prevents it from binding to p75NTR, inhibiting the NGF-p75NTR interaction with IC50s of 23.1 and 1.8 µM in PC12 cells and PC12nnr5 cells, respectively.

Myristoyl-MEK1 Derived Peptide Inhibitor 1, the myristoylated variant of MEK1 Derived Peptide Inhibitor 1, effectively inhibits ERK activation, demonstrating an inhibitory concentration (IC50) of 10 μM [1].

Tetrahydroxystilbene-2-O-β-D-glucoside (EH-201) is a low MW inducer of erythropoietin. Tetrahydroxystilbene-2-O-β-D-glucoside induces expression of erythropoietin, PPAR-γ coactivator 1α (PGC-1α) and haemoglobin in astrocytes and PC12 neuronal-like cells. In vivo, Tetrahydroxystilbene-2-O-β-D-glucoside treatment restores memory impairment, as assessed by the passive avoidance test, in SD, Aβ and KA mouse models. In the hippocampus of mice given Tetrahydroxystilbene-2-O-β-D-glucoside in their diet, levels of erythropoietin, PGC-1α and haemoglobin were increased. Treatment with Tetrahydroxystilbene-2-O-β-D-glucoside might be a therapeutic strategy for memory impairment in neurodegenerative disease, physiological ageing or traumatic brain injury.

Iristectorin B is a natural isoflavone that inhibits breast cancer cell proliferation, modulates ferroptosis in PC12 cells, and reduces Ca²⁺, LDH, and ROS levels, making it suitable for stroke research.

5,6,7-Trihydroxy-4'-methoxyflavone is an antioxidant natural product exhibiting an IC₅₀ of 25.29 μM in DPPH radical scavenging activity assays on PC12 cells.

Rivanicline hemioxalate, also known as RJR-2403 hemioxalate or (E)-Metanicotine hemioxalate, is a chemical compound acting as a neuronal nicotinic receptor agonist with pronounced selectivity for the α4β2 receptor subtype, showing over 1,000-fold greater selectivity for this subtype (Ki=26 nM) compared to α7 receptors (Ki=3.6 μM). Its in vitro studies demonstrate no significant activation of nAChRs in PC12 cells, muscle type nAChRs, or muscarinic receptors at concentrations up to 1 mM. Furthermore, Rivanicline displayed less than one-tenth the potency of nicotine in inducing ileum contraction, with substantially lower efficacy, and failed to antagonize nicotine-induced stimulation of muscle or ganglionic nAChR functions, with an IC50 value greater than 1 mM. Chronic exposure to Rivanicline at 10 microM led to up-regulation of high-affinity nAChRs in M10 cells, mimicking effects observed with nicotine. In vivo studies revealed that Rivanicline significantly reversed scopolamine-induced amnesia and improved working and reference memory in a rat model, while being 15 to 30 times less potent than nicotine in affecting body temperature, respiration, and other physiological responses. Metanicitone's potency was approximately five times lower than nicotine in tail-flick tests following subcutaneous administration, yet slightly more potent upon central administration.

ITX3 is a specific, non-toxic, active and selective TrioN RhoGEF inhibitor with IC50 of 76 μM. ITX3 has anticancer effects, inhibits trion mediated GTP exchange on RhoG and Rac1, inhibits NGF-mediated neurite growth in PC12 cells and REF52 fibroblast structure formation induced by trion.

Zaldaride maleate inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity (IC50: 3.3 nM). Zaldaride maleate is an effective and selective inhibitor of calmodulin. Zaldaride maleate prevents estrogen-induced transcription activation by ER, re

Bryonolic acid (20-epi-Bryonolic acid), a triterpenoid extracted from Sandoricum indicum, possesses immunomodulatory, anti-inflammatory, antioxidant and anticancer activities and protects PC12 cells from NMDA-induced apoptosis by inhibiting Ca2+ in-flux and modulating gene expression in the Ca2+-CaMKII-CREB signalling pathway.

H3R antagonist 4 (compound 11l) serves as a dual inhibitor of cholinesterases and histamine H3 receptors (H3R), demonstrating IC50 values of 7.04 μM (eeAChE), 9.73 μM (hAChE)(reversible), and 1.09 nM (H3R). It effectively inhibits both self and Cu2+-induced Aβ1-42 aggregation at 95.48% and 88.63%, respectively, and degrades Aβ1-42 protofibrils with 80.16% and 89.30% efficiency under similar conditions. Additionally, H3R antagonist 4 possesses the chelating capability for biometals Cu2+, Zn2+, Al3+, and Fe2+. It significantly reduces tau protein hyperphosphorylation induced by Aβ1-42, inhibits RSL-3 induced apoptosis and ferroptosis in PC12 cells, and shows optimal blood-brain barrier permeability and intestinal absorption characteristics in hCMEC/D3 and hPepT1-MDCK cells, respectively. Moreover, the compound improves learning and memory impairments in an Alzheimer's mouse model induced with scopolamine.

Res-Glu3, a derivative of Resveratrol, exhibits antioxidant activities in a rat ischemia-reperfusion model and reduces ROS accumulation. It also provides neuroprotection against H2O2-induced cellular damage in PC12 cells.

Perfluorododecanoic acid (PFDoA) is a perfluoroalkyl substance (PFAS) identified in environmental samples such as lake trout tissue. Perfluorododecanoic acid reduces the viability of PC12 neuronal cells, elevates reactive oxygen species and malondialdehyde levels, and decreases mitochondrial membrane potential, collectively indicating its strong oxidative and mitochondrial toxicity, thereby highlighting its environmental and toxicological significance as a persistent organic pollutant.

AChE/BChE-IN-16 (compound C7) is a potent cholinesterase (ChE) inhibitor, exhibiting IC50 values of 30 nM for human acetylcholinesterase (hAChE) and 48 nM for human butyrylcholinesterase (hBuChE). It demonstrates remarkable protective effects on PC12 cells against H2O2-induced apoptosis and effectively inhibits the production of reactive oxygen species (ROS).

HDAC6-IN-36 (compound 11d) is an HDAC6 inhibitor with an IC50 value of 8.64 nM. It promotes neurite outgrowth in PC12 cells without causing any toxic effects.

HDAC6-IN-45 (Compound 15) is a selective inhibitor of HDAC6, with an IC50 of 15.2 nM. It exerts neurotrophic effects by upregulating GAP43 and Beta-3 Tubulin markers. Additionally, HDAC6-IN-45 activates the Nrf2 signaling pathway, reduces H2O2-induced ROS production, and inhibits apoptosis in PC12 cells. In zebrafish models of Alzheimer's disease, it demonstrates neuroprotective properties. Moreover, HDAC6-IN-45 exhibits antioxidant activity and has favorable blood-brain barrier (BBB) permeability.

UCF 101 is a specific inhibitor of HtrA2 and reduces apoptosis in PC12 cells.

Halenaquinone is a phosphatidylinositol 3-kinase inhibitor. Halenaquinone specifically inhibits the secondary DNA binding of RAD51. Halenaquinone inhibits RANKL-induced osteoclastogenesis. Halenaquinone induces apoptosis in PC12 cells.

Crocin (Gardenia Yellow) is a water-soluble carotenoid pigment of saffron (Crocus sativus L. ) that has been used as a spice for flavoring and coloring food preparations, and in Chinese traditional medicine as an anodyne or tranquilizer. Crocin suppresses tumor necrosis factor (TNF)alpha-induced apoptosis of pheochromocytoma (PC12) cells by modulating mRNA expressions of Bcl-2 family proteins, which trigger downstream signals culminating in caspase-3 activation followed by cell death. Crocin prevented the activation of nSMase by enhancing the transcription of gamma-glutamylcysteinyl synthase, which contributes to a stable glutathione supply that blocks the activity of nSMase.

Phillyrin (Forsythin) is a novel AMPK activator, has anti-obesity effects in nutritive obesity mice, it can prevent lipid accumulation in HepG2 cells by blocking the expression of SREBP-1c and FAS through LKB1/AMPK activation. Phillyrin(Forsythin) may be a new preventive agent of acute lung injury in the clinical setting, it potentially contributes to the suppression of the activation of MAPK and NF-κB pathways, it also has protective effects on H2O2-induced oxidative stress and apoptosis in PC12 cells.

5-OH-HxMF is an inducer of neurite growth in PC12 cells through the camp / PKA / CREB pathway.

ACAF4 is a neurotrophic agent which significantly increases survival in PC12 neuronal cells and enhances the effect of nerve growth factor (NGF). ACAF4 induces neurite outgrowth, and modulates ERK1/2 and AKT signaling pathways.

Pinoresinol dimethyl ether is a nonphenolic furan lignan isolated from the stem bark of Magnolia kobus with neurological activity. It stimulates upstream MAPK, PKC and PKA pathways and induces neural protrusion growth in PC12 cells.