Triaziquone is an alkylating agent that can react with DNA to form intrastrand crosslinks.

β-Interleukin I (163-171), human Acetateis a peptide that participate in the regulation of immune responses, inflammatory reactions, and hematopoiesis.

JIP-1 (153-163) acetate(438567-88-5 free base) is a peptide inhibitor of c-Jun N-terminal kinase (JNK), based on residues 153-163 of JNK-interacting protein-1 (JIP-1). JIP-1 (153-163) acetate(438567-88-5 free base) binds to JNK with affinity in the micromolar range and minimally inhibits p38 and ERK.

NRX-103095 is a potent enhancer of the interaction of β-catenin with the homologous E3 ligase SCFβ-TrCP and enhances the affinity of pSer33/Ser37 β-catenin for β-TrCP with an EC50 of 163 nM.

EM 163 is a TIR-TIR interaction inhibitor, which is a TIR (Toll/interleukin-1 receptor) structural domain mimic of the MyD88 protein. EM 163 targets the TIR structural domain in the IL-1 receptor and blocks the interaction with MyD88. EM 163 inhibits the production of inflammatory cytokines in vivo caused by staphylococcal enterotoxin B (SEB). EM 163 protects mice from SEB shock-induced death. In rat hippocampal neurons in vitro, EM 163 blocked the activation of p38 and the inhibitory effect of IL-1β on chemically induced long-term potentiation (LTP)-triggered protein synthesis.

ThioGlo1 is a thiol-reactive fluorescent probe.1,2,3Upon reaction with a thiol group, a fluorescent adduct is formed that displays excitation/emission maxima of 384/513 nm, respectively.2,3It also reacts with sulfite to form a fluorescent adduct with similar spectral characteristics, and interference from sulfite during thiol determination must be accounted for using secondary methods. ThioGlo1 has been used to monitor the oxidative stability of beer. 1.Yang, J.-R., and Langmuir, M.E.Synthesis and properties of a maleimide fluorescent thiol reagent derived from a naphthopyranoneJ. Heterocycl. Chem.28(5)1177-1180(1991) 2.Hoff, S., Larsen, F.S., Anderson, M.L., et al.Quantification of protein thiols using ThioGlo 1 fluorescent derivatives and HPLC separationAnalyst138(7)2096-2103(2013) 3.Lund, M.N., and Andersen, M.L.Detection of thiol groups in beer and their correlation with oxidative stabilityJ. Am. Soc. Brew. Chem.69(3)163-169(2011)

Niaprazine is a histamine H1-receptor antagonist with marked sedative properties. Niaprazine has antihistamine and antiserotonin activities and can be used for sleep disorder research[1][2]. Niaprazine exhibits a low affinity for the vesicular monoamine transporter and for D2, α2, β, H1 and mAch receptors. Niaprazine, particularly the (+)stereoisomer, has a higher affinity for α1 (Ki = 77 nM) and 5-HT2 (Ki = 25 nM) binding sites, but is poorly recognized by 5-HT1A and 5-HT1B binding sites[2]. Niaprazine (60 mg/kg; i.p.; once) treatment increases rat brain 5-hydroxyindole acetic acid (5-HIAA) concentrations 30 min after treatment, and reduced them at 3-8 hr after treatment. Niaprazine also produces a short-lasting depletion of rat brain noradrenaline (NA) and dopamine (DA)[3]. Animal Model: Male Sprague-Dawley rats (150-200 g)[3] [1]. D Scherman, et al. Molecular pharmacology of niaprazine. Prog Neuropsychopharmacol Biol Psychiatry. 1988;12(6):989-1001. [2]. P G Rossi, et al. Niaprazine in the treatment of autistic disorder. J Child Neurol. 1999 Aug;14(8):547-50. [3]. P E Keane, et al. The effect of niaprazine on the turnover of 5-hydroxytryptamine in the rat brain. Neuropharmacology. 1982 Feb;21(2):163-9.

Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective PKC inhibitor (IC50: 158 nM for rat brain PKC). It has IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively.

Antibacterial agent 163 (compound 1), a hydroxyquinoline derivative, potently inhibits methicillin-resistant Staphylococcus aureus (MRSA) [1].

JIP-1(153-163) is a peptide inhibitor of c-Jun N-terminal kinase (JNK), based on residues 153-163 of JNK-interacting protein-1 (JIP-1). JIP-1(153-163) binds to JNK with affinity in the micromolar range and minimally inhibits p38 and ERK.

16α-hydroxy Dehydroepiandrosterone is a metabolite of the endogenous steroid hormone dehydroepiandrosterone .116α-hydroxy Dehydroepiandrosterone is formed from dehydroepiandrosteronevia16-hydroxylation by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP3A5 in adult human liver microsomes, as well as by fetal recombinant CYP3A7. It is a precursor to fetal estrogens, including estriol .2 1.Miller, K.K.M., Cai, J., Ripp, S.L., et al.Stereo- and regioselectivity account for the diversity of dehydroepiandrosterone (DHEA) metabolites produced by liver microsomal cytochromes P450Drug. Metab. Dispos.32(3)305-313(2004) 2.Hampl, R., and Starka, L.Minireview: 16α-Hydroxylated metabolites of dehydroepiandrosterone and their biological significanceEndocr. Regul.34(3)161-163(2000)

12-hydroxy Stearic acid is a hydroxy fatty acid produced by the hydrogenation of ricinoleic acid .1It is a low molecular weight gelator that self-assembles to form organogels.2Administration of paclitaxel in 12-hydroxy stearic acid-containing gel nanocarriers enhances tumor growth suppression in an H22 murine hepatocellular carcinoma model.3Formulations containing 12-hydroxy stearic acid have been used in cosmetic products as emollients. 1.Fameau, A.-L., and Rogers, M.A.The curious case of 12-hydroxystearic acid — the Dr. Jekyll & Mr. Hyde of molecular gelatorsCurr. Opin. Colloid Interface Sci.4568-82(2020) 2.Burkhardt, M., Noirez, L., and Gradzielski, M.Organogels based on 12-hydroxy stearic acid as a leitmotif: Dependence of gelation properties on chemical modificationsJ. Colloid Interface Sci.466369-376(2016) 3.He, W., Lv, Y., Zhao, Y., et al.Core-shell structured gel-nanocarriers for sustained drug release and enhanced antitumor effectInt. J. Pharm.484(1-2)163-171(2015)

163-bp3 is an effective photoaffinity probe and can be used as a target γ Secretory enzyme.

N-Desbutyl dronedarone is an active metabolite of the antiarrhythmic agent dronedarone .1,2,3It is formed from dronedarone by cytochrome P450s (CYPs) and monoamine oxidase (MAO) in human hepatocyte preparations.4N-Desbutyl dronedarone inhibits the binding of 3,3’,5-triiodo-L-thyronine to the thyroid hormone receptors TRα1and TRβ1(IC50s = 59 and 280 μM for the chicken and human receptors, respectively).1It inhibits CYP2J2-mediated formation of 14,15-EET from arachidonic acid and soluble epoxide hydrolase-mediated formation of 14,15-DHET from 14,15-EET (IC50s = 1.59 and 2.73 μM, respectively, in cell-free assays).2N-Desbutyl dronedarone decreases intracellular ATP levels in H9c2 rat cardiomyocytes (IC50= 1.07 μM) and inhibits mitochondrial complex I, also known as NADH dehydrogenase, and mitochondrial complex II, also known as succinate dehydrogenase, activities in isolated rat heart mitochondria (IC50s = 11.94 and 24.54 μM, respectively).3 1.Van Beeren, H.C., Jong, W.M.C., Kaptein, E., et al.Dronerarone acts as a selective inhibitor of 3,5,3’-triiodothyronine binding to thyroid hormone receptor-α1: in vitro and in vivo evidenceEndocrinology144(2)552-558(2003) 2.Karkhanis, A., Tram, N.D.T., and Chan, E.C.Y.Effects of dronedarone, amiodarone and their active metabolites on sequential metabolism of arachidonic acid to epoxyeicosatrienoic and dihydroxyeicosatrienoic acidsBiochem. Pharmacol.146188-198(2017) 3.Karkhanis, A., Leow, J.W.H., Hagen, T., et al.Dronedarone-induced cardiac mitochondrial dysfunction and its mitigation by epoxyeicosatrienoic acidsToxicol. Sci.163(1)79-91(2018) 4.Klieber, S., Arabeyre-Fabre, C., Moliner, P., et al.Identification of metabolic pathways and enzyme systems involved in the in vitro human hepatic metabolism of dronedarone, a potent new oral antiarrhythmic drugPharmacol. Res. Perspec.2(3)e00044(2014)

JIP-1(153-163) TFA (TI-JIP TFA), a c-JNK peptide inhibitor derived from residues 153-163 of the JNK-interacting protein-1 (JIP-1), exhibits modifications at Phe-11 with a C-terminal amide [1].

Ens-163 phosphate is a muscarinic M1 receptor agonist. It is selective.