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SH-5, an AKT inhibitor potentiates apoptosis and inhibits invasion through the suppression of anti-apoptotic, proliferative and metastatic gene products regulated by IκBα kinase activation.

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

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.

m-PEG5-SH is a PEG-based linker used in PROTACs, joining two critical ligands necessary for forming PROTAC molecules. This linker facilitates selective protein degradation by utilizing the ubiquitin-proteasome system within cells.

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

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.

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.

PUC-10 is a 5-HT6 receptor antagonist with a Ki of 14.6 nM and an IC50 of 32 nM. Computer simulations suggest that PUC-10 is orally active and capable of crossing the blood-brain barrier. It induces autophagy in SH-SY5Y cells by inhibiting the mTOR pathway. PUC-10 is applicable in the study of neurological disorders.

MJ210 is an orally active and blood-brain barrier-permeable modulator of the NF-κB and MAPK pathways, exhibiting neuroprotective properties. In vitro, 5 μM MJ210 can increase the survival rate of rotenone-treated SH-SY5Y cells to 81.9% and reduce levels of ROS. In vivo, 5 mg/kg MJ210 improves motor dysfunction in rat models of Parkinson's disease. MJ210 is useful for research in neurological disorders, including Parkinson's disease.

MK-0752, a γ-secretase inhibitor, reduces Aβ40 production(IC50=5 nM).

SB 242084 hydrochloride is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.IC50 value: 9.0(pKi) [1]Target: 5-HT2C antagonistin vitro: SB 242084 had over 100-fold selectivity over a range of other 5-HT, dopamine and adrenergic receptors. In studies of 5-HT-stimulated phosphatidylinositol hydrolysis using SH-SY5Y cells stably expressing the cloned human 5-HT2C receptor, SB 242084 acted as an antagonist with a pKb of 9.3, which closely resembled its corresponding receptor binding affinity [1].in vivo: SB 242084 potently inhibited m-chlorophenylpiperazine (mCPP, 7 mgkg i.p. 20 min pre-test)-induced hypolocomotion in rats, a model of in vivo central 5-HT2C receptor function, with an ID50 of 0.11 mg/kg i.p., and 2.0 mg/kg p.o. SB 242084 (0.1-1 mg/kg i.p.) exhibited an anxiolytic-like profile in the rat social interaction test, increasing time spent in social interaction, but having no effect on locomotion. SB 242084 (0.1-1 mg/kg i.p.) also markedly increased punished responding in a rat Geller-Seifter conflict test of anxiety, but had no consistent effect on unpunished responding [1].

HUP-55 is a prolyl endopeptidase inhibitor with an IC50 of 5 nM, shown to mitigate α-synuclein dimerization in Neuro2a cells, stimulate autophagy in HEK293 cells, and lower hydrogen peroxide-evoked reactive oxygen species (ROS) production in SH-SY5Y cells at a 10 µM concentration. Additionally, administration of HUP-55 at a dosage of 10 mg kg reduces ipsilateral paw use and diminishes striatal oligomeric α-synuclein concentrations in a Parkinson's disease mouse model, which is induced through adenoviral vector-mediated overexpression of α-synuclein (AAV-αSyn).

2-Hexynyl-5′-N-ethylcarboxamidoadenosine (HENECA) acts as a selective A2A adenosine receptor agonist. This compound elevates intracellular cAMP levels and inhibits the release of MMP-3 induced by TNFα. Additionally, it induces the production of Aβ42 in SH-SY5Y cells.

5-HT7 receptor ligand 2 (compound 32) is an arylpiperazine hydrazone ligand of the 5-HT7R (Ki=178 nM). This compound exhibits high plasma protein binding, good membrane permeability, and low hepatotoxicity and cardiotoxicity. Additionally, it demonstrates neuroprotective effects in SH-SY5Y cells, making it suitable for research on central nervous system-related diseases.

SH5-07 is a hydroxamic acid-based Stat3 inhibitor (IC50: 3.9 μM).

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