α-syn

TCH-165 is a small molecule modulator of proteasome assembly, resulting in an increase in 20S levels. The increase in the level of free 20S corresponds to enhanced proteolysis of IDPs.

α-syn aggregation inhibitor-1 (Compound 2e) acts as an inhibitor of α-syn aggregation. It is capable of inhibiting the cell viability of SH-SY5Y.

2N4R Tau/α-Syn against-1 (Compound 4d) targets α-synuclein and tau proteins, inhibiting the fibrillization and oligomerization of these proteins, and displays depolymerization activity against Aβ fibers. 2N4R Tau/α-Syn against-1 is applicable in Parkinson's and Alzheimer's disease research.

Landipirdine (RO-5025181) is a selective 5-HT6R antagonist for the study of central nervous system disorders such as dementia.

Tozadenant (SYN115) is an adenosine A2A receptor antagonist(Ki of 11.5 nM and 6 nM on human and rhesus,respectively)

Arg-PEG1-Tαsyn is a PROTAC degrader targeting α-synuclein (α-syn), with a DC50 of 0.28 μM in U251 cells. This compound utilizes arginine (Arg) as the E3 ligase ligand and a benzothiazole-aniline variant as the warhead for α-syn targeting. It effectively degrades both wild-type α-syn and its A53T mutant in mammalian cells. In vitro, Arg-PEG1-Tαsyn significantly reduces α-syn aggregation via the E3 ubiquitin ligase UBR1. In vivo, it demonstrates good safety and significantly improves dopaminergic neuron damage and motor dysfunction. Arg-PEG1-Tαsyn is useful in Parkinson's disease research.

SYN-UP is an inhibitor of fibrinolysis.

SYN20028567, an aromatase (CYP19) inhibitor, exhibits an IC50 value of 9.4 nM. It has potential applications in breast cancer research [1].

Nepicastat hydrochloride (RS-25560-197 hydrochloride) is an effective and specific inhibitor, which is used for bovine and human dopamine-β-hydroxylase with IC50 of 8.5 nM and 9 nM, respectively.The affinity of Nepicastat for twelve other enzymes and thirteen neurotransmitter receptors is negligible.

αSyn-IN-576755 is a novel inhibitor of αSyn fibrillization, blocking fibril growth and suppressing A53T αSyn neurotoxicity.

Syn-Ake acetate (Dipeptide diaminobutyroyl benzylamide) is a muscarinic acetylcholine receptor antagonist.

Tat-βsyn-degron, an α-synuclein knockdown peptide, integrates three domains: the HIV-1 Tat plasma membrane transduction domain, an α-synuclein binding domain (βsyn) representing amino acids 36-45 of β-synuclein, and a proteasomal targeting domain (degron). It effectively binds to recombinant α-synuclein, demonstrating a significant reduction in α-synuclein levels in primary rat cortical neuron cultures.

SYN1143 (AMG-1) is a potent inhibitor of human RON and c-Met.In vitro kinase assays showed that compound I is a potent inhibitor of human RON and c-Met with IC50s of 9 and 4 nmol/L, respectively.

Tat-βsyn-degron is an α-synuclein (α-synuclein) knockdown peptide that efficiently degrades the α-synuclein protein via the proteasome pathway. It effectively reduces α-synuclein protein levels in primary rat cortical neuron cultures. In Parkinson's mouse toxicity models, Tat-βsyn-degron alleviates neuronal damage and motor dysfunction induced by Parkinsonian toxins.

tau Protein/α-synuclein-IN-2 (Compound 14T) is a tau and α-synuclein inhibitor capable of crossing the blood-brain barrier. It reduces α-synuclein oligomerization in a dose-dependent manner through a thiourea linker structure. In biosensor cells, tau Protein/α-synuclein-IN-2 prevents tau aggregation seed effects. In the M17D neuroblastoma model, this compound exhibits anti-inclusion effects and reduces Aβ plaque formation. tau Protein/α-synuclein-IN-2 shows potential for Alzheimer's and Parkinson's disease research.

α-Synucleininhibitor 10 inhibits α-Syn aggregation activity with a low IC50 value of 1.08 μM and demonstrates strong binding affinity to α-Syn residues. It is applicable for research on Parkinson's disease (PD).

α-Synucleininhibitor 11 (compound 1) is a selective inhibitor of α-synuclein (α-syn) oligomer formation. It does not inhibit tau 4R (isoforms 0N4R, 2N4R) or p-tau (isoform 1N4R). α-Synucleininhibitor 11 can be utilized for Parkinson's disease (PD) research.

α-Synuclein inhibitor 12 (compound 4ce) is an inhibitor of α-Syn (α-synuclein) aggregation, suitable for research in neurological disorders.

α-Synucleininhibitor 13 is an inhibitor of α-synuclein (α-Syn). It can prevent the aggregation of α-Syn protein and disassemble already formed fibrils, primarily used in Parkinson's disease research.

α-Synuclein inhibitor 3 (Compound 7g) is a potent inhibitor of α-synuclein (α-Syn) aggregation, with potential applications in Parkinson's disease research [1].

α-Synuclein inhibitor 6 (compound 3ge) is a blood-brain barrier-permeable agent that effectively inhibits α-Synuclein (α-Syn) aggregation, demonstrating a potent IC50 value of 1.70 μM and achieving an inhibition ratio of 94.4% at 30 μM [1].

α- Synuclein inhibitor 7 (compound 3gf) is effective α- Synuclein ( α- Syn) aggregation inhibitor, IC50 is 1.95 μM, inhibition rate at 30μM was 85.8%. α- Synuclein inhibitor 7 has blood-brain barrier permeability.

α-Synuclein inhibitor 5 is a potent inhibitor of α-Synuclein (α-Syn) aggregation across the blood-brain barrier (IC50: 1.22 μM), with 94.3% inhibition at 30 μM.

α-Synuclein inhibitor 9 (Compound 20C) targets and binds to cavities within mature α-synuclein fibrils, diminishing their β-sheet content. It effectively inhibits the aggregation of A53T α-synuclein, exhibits neuroprotective properties, enhances brain functionality, and alleviates motor impairments. This compound is utilized in research related to Parkinson's disease (PD). [1]