psd95

Tramiprosate (Alzhemed) is an orally active, blood-brain-barrier-crossing, naturally occurring amino acid found in a variety of red seaweeds that binds soluble Aβ and maintains it in a non-protofibrillar form.It is a GABA analog with neuroprotective, anticonvulsant, and antihypertensive activity.

IC87201 is a nNOS-PDZ/PSD-95-PDZ inhibitor. IC87201 showed great promise in cellular experiments and animal models of ischemic stroke and pain.

Tat-NR2B9c (NA-1) is a postsynaptic density-95 (PSD-95) inhibitor with neuroprotective and antiepileptic effects.Tat-NR2B9c inhibits PSD-95d2, PSD-95d1, and PSD-95, which prevents the activation of NMDA-induced NADPH oxidase in neurons, thereby blocking the production of superoxide, which reduces ischemic injury in the acute phase after stroke.

Tat-NR2B9c TFA is a 20-aa peptide, and acts as an inhibitor of postsynaptic density-95 (PSD-95)(EC50 of 6.7 nM for PSD-95d2), and possesses neuroprotective efficacy.

PSD-95/nNOS PPI-IN-1 is an inhibitor targeting the interaction between PSD-95 and nNOS, potentially crossing the blood-brain barrier. It binds with high affinity to the PSD-95 PDZ2 domain (Ki= 19.45 μM). By reducing intracellular ROS levels and inhibiting apoptosis, it counteracts glutamate-induced excitotoxicity. In rat tMCAO models, PSD-95/nNOS PPI-IN-1 significantly decreases brain infarct volume. This compound is useful for research in acute ischemic stroke.

Perfluoroenanthic acid (Perfluoroheptanoic acid) is a perfluoroalkyl substance (PFAS) that negatively impacts spermatogenic development and testicular m6A RNA methylation in offspring exposed during gestation, thus impeding spermatogenesis and inducing reproductive toxicity. Additionally, in primary cortical neuron cultures, Perfluoroenanthic acid alters dendritic spine morphology and synaptogenesis, enhances neural activity and synaptic transmission, and increases the expression of excitatory synapse-associated proteins Synaptophysin and PSD95.

Rodin-A is an orally active, brain-penetrant, and selective inhibitor of the histone deacetylase (HDAC) CoREST complex, exhibiting an IC50 value of 1.80 μM for the CoREST complex, 0.15 μM for HDAC1, and 0.43 μM for HDAC2. It enhances acetylation of histone H3K9 and upregulates neuronal gene expression, leading to increased dendritic spine density, co-localization of synaptic proteins (SV2A and PSD95), and improved hippocampal long-term potentiation (LTP), thus providing synaptic protection and repair. Rodin-A is a promising compound for the study of neurodegenerative diseases associated with synaptic dysfunction, particularly Alzheimer's disease.

Rodin-B is an orally active, brain-penetrant, and selective inhibitor of the histone deacetylase (HDAC)-suppressor of transcription factor corepressor element-1 silencing transcription factor (CoREST) complex. It exhibits an IC50 value of 0.50 μM for the CoREST complex, 0.27 μM for HDAC1, and 0.28 μM for HDAC2. Rodin-B enhances the acetylation level of histone H3K9 and upregulates neuron-related gene expression, promoting increased dendritic spine density, colocalization of synaptic proteins (SV2A and PSD95), and improved hippocampal long-term potentiation (LTP), thereby exerting synaptic protection and repair effects. Rodin-B holds potential for research into neurodegenerative diseases related to synaptic dysfunction, particularly Alzheimer's disease.

LY836 is an orally active, neuroprotective compound that effectively inhibits the PSD95-nNOS association in cortical neurons. It has potential applications in the study of ischemic stroke [1].

TAT-GluR6-9c is a blocker of GluR6-PSD95 interaction. It inhibits JNK activation and c-Jun phosphorylation by regulating GluR6-mediated signaling pathways, thereby reducing Fas L expression and decreasing apoptosis. TAT-GluR6-9c is applicable in the study of cerebral ischemia and neuroprotection strategies.