Neurological Disease

BEN-28010 is a selective, orally active, blood-brain barrier permeable CHK1 inhibitor with an IC₅₀ of 4.0 nM. BEN-28010 functions as a radiosensitizer, exhibits antitumor efficacy in GBM models. BEN-28010 can be used for the research of glioblastoma.

LY382884 is a selective antagonist for GluR5 kainate receptor. LY382884 prevents the induction of NMDA receptor independent long-term potentiation (LTP).

A 844606 is a highly potent and selective α4β2 nAChR agonist. A 844606 can be used in the study of schizophrenia, Huntington's disease, Alzheimer's disease, and Parkinson's disease.

Etbicyphat-¹³C₃ is the ¹³C labeled Etbicyphat (HY-139145). Etbicyphat is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors.

(S)-(+)-O-Desmethyl Venlafaxine-d₆ is the deuterium labeled (S)-(+)-O-Desmethyl Venlafaxine. O-Desmethyl Venlafaxine is an active metabolite of Venlafaxine. Venlafaxine (HY-B0196) is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI) class.

Cymserine is a blood-brain barrier-permeable butyrylcholinesterase (BuChE) inhibitor with an IC₅₀ value of 56.43 nM and a K_i of 38 nM. Cymserine binds to the catalytic domain of BuChE in a concentration-dependent manner to form a stable carbamylated enzyme complex, and exhibits BuChE selectivity over acetylcholinesterase due to its structural compatibility with the larger acyl-binding pocket of BuChE. Cymserine can be used in the research of Alzheimer's disease.

LBG30300 is a subtype-selective mGlu₂ receptor agonist EC₅₀ 0.6 nM. LBG30300 is blood-brain barrier permeable.

NZ-66 is a ULK1-Recruiting Chimera (ULKREC) and heterobifunctional chimeric molecule composed of a BL-918-derived ULK1 agonist linked to a mitochondrial outer membrane-targeting TSPO ligand via a six-carbon hexane linker. NZ-66 is a mitophagy inducer recruits ULK1 to mitochondria to induce ULK1-dependent mitophagy, enhanced by mitochondrial insult, independently of the PRKN/PINK axis. NZ-66 can be used for the research of parkinson’s disease.

Dehydrohaloperidol, Haloperidol (HY-14538) analogue, is a selective human dopamine D₂ receptor antagonist with a pK_d of 8 and a pk_i of 8. Dehydrohaloperidol can be used for the research of schizophrenia.

AnnH31 is a Dyrk1A inhibitor (IC₅₀: 81 nM). AnnH31 also inhibits MAO-A with an IC₅₀ of 3.2 μM. AnnH31 inhibits cell viability of HeLa, PC12 and SH-SY5Y cells.

SR-32685 is a NAMPT activator and neuroprotective agent. SR-32685 enhances the enzymatic activity of hNAMPT, prevents intracellular NAD depletion, and protects neurons from death induced by toxic misfolded prion proteins. SR-32685 can be used in the research of protein misfolding neurodegenerative diseases and metabolic diseases.

TIPP is a potent and selective δ-opioid antagonist with a K_i value of 1.22 nM.

NK1 receptor antagonist 2 is a neurokinin 1 (NK1) receptor antagonist. NK1 receptor antagonist 2 is applicable to research related to tinnitus and hearing loss.

RIPK1-IN-25 (WL8) is a blood-brain permeable RIPK1 inhibitor with EC₅₀ and K_d values are 19.9 and 25 nM, respectively. RIPK1-IN-25 can be used in the study of neurometabolic diseases.

Flupentixol is an orally active D₁/D₂ dopamine receptor antagonist and new PI3K inhibitor (PI3Kα IC₅₀=127 nM). Flupentixol shows anti-proliferative activity to cancer cells and induces apoptosis. Flupentixol can also be used in schizophrenia, anxiolytic and depressive research.

CB2 receptor agonist 7 (Compound 5B) is a cannabinoid 2 (CB2) receptor agonist with blood-brain barrier permeability.

Mast cell degranulating peptide (28-49) is a depolarizing agent from bee venom, it can raise the content of cGMP level in mouse cerebellar slices.

SJ44236 is a BET PROTAC degrader with activity against BRD2, BRD3 and BRD4 (DC₅₀ = 127 pM). SJ44236 induces ubiquitination and proteasomal degradation by forming a ternary complex with BET proteins and CRBN-DDB1. SJ44236 downregulates c-Myc, upregulates p53 and reduces cancer cell viability. SJ44236 can be used for the research of leukemia and medulloblastoma.

Cannabidiolic acid methyl ester (HU-580) is an orally active cannabidiolic acid analogue. Cannabidiolic acid methyl ester can enhance the activation of 5-HT_1A receptor and increase the expression of c-Fos and NeuN in specific hypothalamic nuclei of rats. Cannabidiolic acid methyl ester has anti-nausea, anti-anxiety and anti-injury effects.

2002-H20 is an inhibitor of Aβ42-induced cytotoxicity, with the activity of reducing the cytotoxicity of Alzheimer's disease Aβ peptide by binding to it. 2002-H20 protects cells and reduces Aβ toxicity by promoting fibril formation, possibly by accelerating Aβ aggregation. The screening method of 2002-H20 effectively identifies compounds that reduce Aβ toxicity and presents potential inhibitory leads.