a 139

ELB-139 is a GABAA receptor agonist that can be used to study depression and epilepsy.

BMS-833923 (XL-139), an orally bioavailable Smoothened antagonist, inhibits BODIPY cyclopamine binding to SMO in a dose-dependent manner (IC50: 21 nM).

Aziridyl benzoquinone, an antineoplastic agent, has been studied as a mutagen and as a carcinogenic agent.

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)

Selective medium-chain free fatty acid receptor GPR84 agonist (EC50 = 139 nM). Exhibits no response at GPR40, GPR41, GPR119 or GPR120 at 100 μM. Activates calcium mobilization, inhibits cAMP accumulation, and induces ERK1/2 phosphorylation, receptor desensitization and internalization in vitro. Liu et al (2016) Design and synthesis of 2-alkylpyrimidine-4,6-diol and 6-alkylpyridine-2,4-diol as potent GPR84 agonists. ACS Med.Chem.Lett. 7 579 PMID:27326330 |Zhang et al (2016) Discovery and characterization of a novel small-molecule agonist for medium-chain free fatty acid receptor G protein-coupled receptor 84. J.Pharmacol.Exp.Ther. 357 337 PMID:26962172

Imidafenacin metabolite M4 is a metabolite of the muscarinic acetylcholine receptor antagonist imidafenacin.1It is formed from imidafenacin by the cytochrome P450 (CYP) isoform CYP3A4. 1.Kanayama, N., Kanari, C., Masuda, Y., et al.Drug-drug interactions in the metabolism of imidafenacin: Role of the human cytochrome P450 enzymes and UDP-glucuronic acid transferases, and potential of imidafenacin to inhibit human cytochrome P450 enzymesXenobiotica37(2)139-154(2007)

WZ4003, a highly selective NUAK kinase inhibitor, is with IC50 of 20 nM and 100 nM for NUAK1 and NUAK2, respectively. It is no significant inhibition on 139 other kinases.

Plp(139-151) trifluoroacetate is a useful organic compound for research related to life sciences and the catalog number is T64674.

BOLD-100 free base (NKP-1339; IT-139), a ruthenium-based anticancer agent, inhibits stress-induced GRP78 upregulation, thus disrupting endoplasmic reticulum (ER) homeostasis. This action induces ER stress and unfolded protein response (UPR), interfering with the intricate relationship between ER-stress response, lysosome dynamics, and autophagy execution.

Osteostatin (human), a fragment derived from parathyroid hormone-related protein (PTHrP) 107-139, effectively promotes bone repair in animal models with bone defects and inhibits bone erosion in cases of inflammatory arthritis [1].

Brazikumab (AMG 139) is a humanized antibody targeting IL-23 by binding to the P19 subunit. It is a selective IL23p19 antagonist and can be used in Crohn's disease research.

Compound 6h (Anticancer Agent 139) exhibits potent anticancer activity, engaging in a π-cationic interaction with Lys352 of Tubulin and demonstrating high efficacy against SNB-19, OVCAR-8, and NCI-H460 with PGIs of 86.61, 85.26, and 75.99, respectively. Moreover, it shows moderate activity against a range of other cancer cell lines — HOP-62, SNB-75, ACHN, NCI ADR-RES, 786-O, A549 ATCC, HCT-116, and MDA-MB-231 — with PGIs between 51.88 and 67.55 [1].

PLP (178-191), an immunodominant encephalitogenic epitope from the proteolipid protein (PLP) fragment spanning amino acids 178 to 191, plays a pivotal role in SJL mice. It initiates disease onset earlier compared to the other major encephalitogenic epitope, PLP (139-151), though both epitopes result in similar incidence, severity, and histologic characteristics.

GK718, a selective HDAC1 3 inhibitor with IC50 values of 259 nM and 139 nM, respectively, elevates acetylated histone H3 levels in cells and mitigates Bleomycin-induced pulmonary fibrosis in mice [1].

7-Desmethylmicrocystin-LR, a toxic heptapeptide, can be isolated from an axenic strain of Microcystis aeruginosa (K-139) [1].

[Leu144,Arg147]-PLP (139-151) is a mutated fragment of the myelin proteolipid protein (PLP), featuring substitutions of tryptophan to leucine and histidine to arginine at positions 144 and 147, respectively. Immunizing mice with this peptide (50 µg) mixed in complete Freund's adjuvant (CFA) elevates IL-4 levels in the spleen. While it suppresses Th1 cell activation in vitro, it does not do so in vivo; instead, it promotes the development of regulatory T cells. Preimmunization with [Leu144, Arg147]-PLP (139-151) postpones the onset of experimental autoimmune encephalomyelitis (EAE) triggered by encephalitogenic peptides from PLP (178-191), myelin oligodendrocyte glycoprotein (MOG) (92-106), or myelin basic protein (MBP) in mice.

E3 Ligase Ligand 22 (compound 139) serves as a cereblon binder, facilitating the degradation of Ikaros or Aiolos via the ubiquitin proteasome pathway [1].

Sodium cyclamate-d4 is a deuterated compound of Sodium cyclamate. Sodium cyclamate has a CAS number of 139-05-9. Cyclamic acid sodium is a carbonic anhydrase inhibitor and one of the most widely used artificial sweeteners in food and pharmaceuticals.Cyclamic acid sodium shows moderate anticonvulsant activity in a maximal electroshock convulsive seizure model.Cyclamic acid sodium is used in cancer research.

[SER140]-PLP(139-151) is a polypeptide fragment derived from the myelin-associated lipid protein.

[SER140]-PLP(139-151) acetate is a peptide fragment from myelin proteolipid protein (PLP).

[SER140]-PLP(139-151) (TFA) is a polypeptide fragment of the myelin lipid protein.

[L144-PLP(139-151)], a peptide ligand of the T cell receptor (TCR), acts as a TCR antagonist specifically inhibiting the activation of encephalitogenic Th1 clones [1].

CD36 Peptide P (139-155), Cys conjugated, a Cys-labelled variant of CD36 Peptide, can inhibit CD36's immunoadsorption by OKM5 [1].