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)

AMK-GX (Immobilized Penicillin G acylase) is a stabilized form of penicillin acylase with enhanced temperature and pH resistance. It exhibits high recovery rates and maintains most of its original activity even after 12 cycles of use. AMK-GX catalyzes the conversion of Penicillin G (PG) into 6-aminopenicillanic acid (6-APA) and 7-amino-desacetoxycephalosporanic acid, which are crucial intermediates in the production of β-lactam antibiotics.

AMK-EX (Immobilized cephalosporin C or 7-ACA esterase) is an immobilized enzyme where cephalosporin C/7-ACA esterases are enzymes capable of hydrolyzing cephalosporin or 7-ACA ester bonds. Immobilized enzymes involve a technique that anchors enzymes onto carriers, facilitating easy separation and recovery, while enhancing the enzyme's stability, activity, and reusability.

Olamkicept (FE-301) is a soluble gp130-Fc-fusion protein that selectively inhibits interleukin 6 (IL-6) trans-signaling by binding to the soluble IL-6 receptor/IL-6 complex.

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.

SGC-CAMKK2-1 is a selective inhibitor of calcium/calmodulin-dependent protein kinase kinase 2 (CAMKK2) with an IC50 of 30 nM. It effectively inhibits AMPK phosphorylation in C4-2 cells, exhibiting an IC50 value of 1.6 µM.

CaMKK2-IN-1 is a selective and potent inhibitor of CaMKK2, exhibiting an IC50 of 7 nM.

CaMKIIδ-IN-1 (compound 15e) is a pyrimidine-based inhibitor of CaMKIIδ, with an IC50 value of 0.012 μM.

CaMKIIδ-IN-1 (Compound 15e) hydrochloride is a pyrimidine-based inhibitor of CaMKIIδ with an IC50 value of 12 nM.

CaMKII-IN-3 (Example 321) is a CaMKII inhibitor with an IC50 of less than 10 nM, and it can be utilized in the study of heart diseases.

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].

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 .

AMK318 (Immobilized cephalexin acylase) is a biocatalyst and a critical enzyme in novel biocatalyst technology. Enzyme engineering focuses on improving enzyme reaction kinetics, substrate selectivity, and activity under harsh conditions (such as low or high pH). By incorporating stimulus responsiveness into these enzyme modifications, dynamic control of activity becomes feasible.

AMK218 (Immobilized amoxicillin acylase) serves as a biocatalyst and is a key enzyme in new biocatalyst technologies. Enzyme engineering focuses on improving enzyme reaction kinetics, substrate selectivity, and activity under extreme conditions (e.g., low or high pH). Modifications that introduce stimulus responsiveness enable dynamic control of their activity.

AMK518 (Immobilized cefradine acylase) is an important biocatalyst and a key enzyme in new biocatalyst technology. Enzyme engineering focuses on improving reaction kinetics, substrate selectivity, and activity under challenging conditions, such as low or high pH. By incorporating stimulus responsiveness into these enzyme modifications, dynamic control of activity is also achievable.

AMK328 (Immobilized cefaclor acylase) is a biocatalyst and a crucial enzyme in advanced biocatalyst technology. Enzyme engineering focuses on improving reaction kinetics, substrate specificity, and activity under extreme conditions such as low or high pH. Introducing stimulus responsiveness to these enzyme modifications enables dynamic control of their activity.

AMK618 (Immobilized cefadroxil acylase) is a biocatalyst and a key enzyme in innovative biocatalysis technology. Enzyme engineering focuses on improving enzyme reaction kinetics, substrate selectivity, and activity under extreme conditions (such as low or high pH). Introducing stimulus responsiveness to these enzyme modifications enables dynamic control of their activity.

H-1152 dihydrochloride (H-1152 2HCl) is a specific inhibitor of Rho-associated protein kinase (ROCK) with an IC50 of 12 nM and a Ki of 1.6 nM. H-1152 dihydrochloride inhibits PKA, PKC, PKG, Aurora A and CaMKII with IC50 values of 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively.

XST-14 is a competitive and specific inhibitor of ULK1 (IC50: 26.6 nM).XST-14 blocks autophagy by inhibiting the phosphorylation of ULK1 downstream substrates.XST-14 induces apoptosis and inhibits the growth of HCC cells.

Elziverine is an orally available small molecule calmodulin antagonist.Elziverine in vitro treatment inhibited Ca-loading-induced acanthocyte formation in SHRSP, WKY, and Wistar rats in a concentration-dependent manner.Elziverine can be used for the treatment of neurological disorders, and may be used for the study of cognitive disorders.