nk3

Pavinetant (MLE-4901) is an orally available neurokinin-3 receptor (NK3R) antagonist used to improve menopausal symptoms.

Scyliorhinin II acetate is a selective agonist of the neurokinin-3 (NK3) receptor (Ki = 2.5 nM) in rat cerebral cortex.

CS-003 free base (CS-003) is a triple tachykinin receptor antagonist with high affinity for human (neurokinin) NK1, NK2 and NK3 receptors, with Ki values of 2.3 nM and 0.54 nM, respectively And 0.74 nM. CS-003 free base (CS-003) has therapeutic effects on

Fezolinetant (ESN-364) is a neurokinin-3 receptor antagonist that is being investigated for menopausal hot flashes.

Osanetant produces anxiolytic- and antidepressant-like effects. Osanetant is a selective NK3 receptor antagonist. It is researched for schizophrenia.

SB-222200 is a selective, reversible, and competitive antagonist of the human NK-3 receptor(Ki=4.4 nM).

GR 94800 acetate is a potent and selective neurokinin 2(NK-2) antagonist.

SB 218795 is an effective and selective antagonist of NK3 with a Ki 13 nM for hNK3 which is about 90-fold and 7000-fold selectivity over hNK2 and hNK1.

Elinzanetant is a dual antagonist of neurokinin (NK) receptors 1 and 3 and modulates reproductive hormone secretion.

Talnetant (SB 223412) is a selective, competitive NK3 receptor antagonist that penetrates the brain and modulates mesolimbic and mesocortical dopaminergic neurotransmission.

Senktide is an agonist of tachykinin NK3 receptor.

Senktide acetate (Senktide acetate(106128-89-6 free base)) is a selective tachykinin NK3 receptor agonist that promotes the consolidation or expression of ELM for the study of Alzheimer's disease.

Eledoisin (Eledone peptide) is an undecapeptide of mollusk origin in the tachykinin family of neuropeptides, serving as a specific agonist of NK2 and NK3 receptors.

Neurokinin B acetate(86933-75-7 free base) is the acetate form of Neurokinin B, which belongs to the tachykinin family. Neurokinin binds to neurokinin receptor 1 (NK1R), nk2r and NK3R, and mediates its biological effects.

Hemokinin 1 (human) acetate is an endogenous substance P homolog that is a selective agonist at the tachykinin NK1 receptor (IC50 values are 1.8, 370 and 480 nM for NK1, NK3 and NK2 receptors respectively). Has proliferative and antiapoptotic actions on B

JNK3 Inhibitor-4, a potent 2-aryl-1-pyrimidinyl-1H-imidazole-5-yl acetonitrile derivative, demonstrates a strong inhibitory effect on JNK3 with an IC 50 value of 1.0 nM. It exhibits exceptional selectivity against JNK3 when compared to other protein kinases, including isoforms JNK1 (IC 50 = 143.9 nM) and JNK2 (IC 50 = 298.2 nM). Additionally, JNK3 Inhibitor-4 benefits from neuroprotective properties and is predicted to permeate the blood-brain barrier effectively.

JNK3inhibitor-9 (Compound 24a) is a potent, selective JNK3 inhibitor capable of crossing the blood-brain barrier (BBB), demonstrating an IC50 value of 12 nM. It effectively inhibits GSK3α/β, which is involved in Tau phosphorylation, with IC50 values of 14 nM and 35 nM, respectively. JNK3inhibitor-9 also reduces the phosphorylation of c-Jun and APP and protects neurons from Aβ1-42 toxicity.

JNK3inhibitor-6 (Compound A53) is a selective inhibitor of JNK3 (IC50 = 78 nM) with neuroprotective properties, making it suitable for research in neurodegenerative diseases.

NK3R-IN-2 is an orally active NK3R inhibitor with an IC50 of 330.50 nM against human NK3R. It can penetrate the blood-brain barrier and exhibits excellent NK3R binding affinity in CHO-K1 cells (IC50= 87.31 nM). NK3R-IN-2 effectively suppresses luteinizing hormone (LH) levels and is applicable for research on hormone-related diseases.

NK3201, a specific chymase inhibitor, suppresses bleomycin-induced pulmonary fibrosis in hamsters.

JNK3 inhibitor-1 is a highly potent and selective compound that specifically inhibits JNK3 with an impressive IC50 value of 0.005 μM. In addition to its remarkable inhibitory effects, JNK3 inhibitor-1 possesses excellent oral bioavailability and the ability to efficiently penetrate the brain.

JNK3 inhibitor-2 is a potent and selective JNK3 inhibitor with IC50 values of >100 μM for JNK1, >100 μM for JNK2, and 0.25 μM for JNK3. JNK3 inhibitor-2 also inhibits DDR1 and EGFR (T790M, L858R) [1].

NK314 is a novel synthetic benzo[c]phenanthridine alkaloid that shows strong antitumor activity. It inhibited topoisomerase II activity and stabilized topoisomerase II-DNA cleavable complexes. The DNA breaks occurred within 1h after treatment with NK314 even without digestion of topoisomerase II by proteinase K, whereas etoposide required digestion of the enzyme protein in cleavable complex to detect DNA breaks. Pretreatment with topoisomerase II catalytic inhibitors, ICRF-193 and suramin, reduced both cleavable complex-mediated DNA breaks and proteinase K-independent DNA breaks, but protease inhibitors and nuclease inhibitors only decreased the latter.

JNK3 Inhibitor-3 (compound 15g) is a selective, blood-brain barrier permeable, and orally active inhibitor of c-Jun N-terminal kinase 3 (JNK3) with IC50 values of 147.8 nM, 44.0 nM, and 4.1 nM against JNK1, JNK2, and JNK3, respectively. This compound has been shown to significantly enhance memory in mouse models of dementia and is utilized in Alzheimer's disease research [1].