amk

AMK is an active metabolite of the neurohormone melatonin .1,2,3,4It is formed from melatoninviathe metabolic intermediate AFMK that is then deformylated by catalase or formamidase.5,6AMK scavenges singlet oxygenin vitrowhen used at a concentration of 200 μM.1It inhibits the epinephrine- and arachidonic acid-induced production of prostaglandin E2and PGD2in ovine seminal vesicle microsomes in a concentration- and time-dependent manner, as well as LPS-induced increases in COX-2 levels in RAW 264.7 macrophages when used at a concentration of 500 μM.2,3AMK (20 mg/kg) decreases MPTP-induced increases in lipid peroxidation in the cytosol and mitochondria from substantia nigra and striatum in a mouse model of MPTP-induced Parkinson’s disease.4 1.Schaefer, M., and Hardeland, R.The melatonin metabolite N1-acetyl-5-methoxykynuramine is a potent singlet oxygen scavengerJ. Pineal Res.46(1)49-52(2009) 2.Kelly, R.W., Amato, F., and Seamark, R.F.N-acetyl-5-methoxy kynurenamine, a brain metabolite of melatonin, is a potent inhibitor of prostaglandin biosynthesisBiochem. Biophys. Res. Commun.121(1)372-379(1984) 3.Mayo, J.C., Sainz, R.M., Tan, D.-X., et al.Anti-inflammatory actions of melatonin and its metabolites, N1-acetyl-N2-formyl-5-methoxykynuramine (AFMK) and N1-acetyl-5-methoxykynuramine (AMK), in macrophagesJ. Neuroimmunol.165(1-2)139-149(2005) 4.Tapias, V., Escames, G., López, L.C., et al.Melatonin and its brain metabolite N1-acetyl-5-methoxykynuramine prevent mitochondrial nitric oxide synthase induction in parkinsonian miceJ. Neurosci. Res.87(13)3002-3010(2009) 5.Tan, D.-X., Manchester, L.C., Reiter, R.J., et al.Melatonin directly scavenges hydrogen peroxide: A potentially new metabolic pathway of melatonin biotransformationFree Radic. Biol. Med.29(11)1177-1185(2000) 6.Hirata, F., Hayaishi, O., Tokuyama, T., et al.In vitro and in vivo formation of two new metabolites of melatoninJ. Biol. Chem.249(4)1311-1313(1974)

CaMKP Inhibitor can inhibit CaMKP.

CaMKII-IN-1, a potent and highly selective inhibitor of CaMKII (IC50 = 63 nM), exhibits over 100-fold higher selectivity for CaMKII compared to CaMKIV, MLCK, p38a, Akt1, and PKC.

CaMKIIα-PHOTAC is a photochemically targeted chimera (PHOTAC) that specifically targets Ca2+ calmodulin-dependent protein kinase II α (CaMKIIα), facilitating its ubiquitination and subsequent proteasome-mediated degradation when exposed to specific light wavelengths. Under illumination, CaMKIIα-PHOTAC diminishes synaptic functions and weakens evoked field excitatory postsynaptic potentials in the mouse hippocampus, impacting physiological responses and sustaining long-term potentiation and memory functions within dendritic domains [1].

Eramkafusp alfa is a human IgG1 antibody that targets the murine B lymphocyte antigen CD20, also known as MS4A1 [1].

CaMKII inhibitory peptide KIIN serves as a potent inhibitor of CaMKII [1] [2].

CaMKI (299-320) is a peptide representing residues 299-320 of Calcium calmodulin-dependent protein kinase I (CaMKI). This segment, functioning as a protein kinase, exhibits a strong interaction with Ca 2+ -CAM (K d ≤1 nM), enabling it to phosphorylate specific substrate proteins and regulate their activity. It encompasses both the CAM-binding domain and the self-inhibition domain. CaMKI (299-320) is applicable for researching cellular physiological processes such as proliferation, differentiation, and apoptosis .

CaMKIIα-IN-1 (Compound 4d) is an orally active inhibitor of Ca 2+ calmodulin-dependent protein kinase II α (CaMKIIα) with a Kd of 219 nM for CaMKIIα WT hub, and it demonstrates good metabolic stability [1].