Carbobenzoxyproline (L-Cbz-Proline) is an inhibitor of prolidase. Carbobenzoxyproline can be used for prolidase deficiency (PD) research[1].
Coelenteramine 400a (Coelenterazine 400a) hydrochloride, a derivative of Coelenterazine, is a Renilla luciferase (RLuc) substrate. In the presence of Coelenteramine 400a hydrochloride, RLuc can emit blue light at 395 nm[1][2]. Coelenteramine 400a hydrochloride will causes color change in the bioluminescence reaction of Rluc by replacing the sulfur and oxygen heteroatoms of the methylene bridge. Coelenteramine 400a hydrochloride provides higher signal resolution and can be used in the research of bioluminescence resonance energy transfer (BRET)[3].
Gallinamide A is a potent inhibitor of cathepsin L with an IC50 value of 17.6 pM.
13-Keto-8(14)-Podocarpen-18-oic acid (compound 16) is a compound isolated from Pinus massoniana Lamb[1].
Licoflavone A is a flavonoid isolated from the roots of Glycyrrhiza uralensis, inhibits protein tyrosine phosphatase-1B (PTP1B), with an IC50 of 54.5 μM[1].
Azacyclonol, also known as γ-pipradol, is a drug used to diminish hallucinations in psychotic individuals.Target: OthersAzacyclonol is a drug which is a so-called ataractive, or agent which diminishes hallucinations in psychotic individuals. The formation of Azacyclonol in human intestinal microsomes is linear with respect to time up to 60 min. The rates of formation of Azacyclonol increases linearly with microsomal protein concentration up to 2 mg/mL. The apparent Km and Vmax values of Azacyclonol are 0.82 μM and 60 pmol/min/mg protein in microsomes from human liver [1]. The formation of Azacyclonol and terfenadine alcohol from terfenadine is confirmed to be catalyzed predominantly by CYP3A(4) isozyme, and the ratio of the rate of terfenadine alcohol formation to that of Azacyclonol is 3:1 [2]. The amount of Azacyclonol eliminated renally increases on average 2-fold after rifampin dosing [3].
CP-465022 Maleate is a potent, and selective noncompetitive AMPA receptor antagonist with anticonvulsant activity. CP-465022 is against Kainate-induced response with an IC50 of 25 nM in rat cortical neurons. CP-465022 provides a new tool to investigate the role of AMPA receptors in physiological and pathophysiological processes[1][2].
Loxoribine (7-Allyl-8-oxoguanosine) is a guanosine analog with anti-viral and anti-tumor activities. Loxoribine is an orally bioavailable and selective Toll-like receptor (TLR) 7 agonist[1][2][3].
2-Amino-4,4,4-trifluorobutyric acid is an alanine derivative[1].
Oxyphyllenone A is an inhibitor of NO Synthase. Oxyphyllenone A inhibits the NO production in lipopolysaccharide-activated macrophages with an IC50 of 28 μM[1].
NH2-PEG2-methyl acetate is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Indole-3-carboxaldehyde (3-Formylindole), a cabbage extract, is the product of the oxidative degradation of indole-3-acetic acid (IAA) by crude enzyme preparations from etiolated pea seedlings. Indole-3-carboxaldehyde (3-Formylindole) is a biochemical used to prepare analogs of the indole phytoalexin cyclobrassinin[1].
CuATSP, a potent inhibitor of ferroptotic cell death, is almost 20-fold more potent than CuATSM.
5'-O-(4,4'-Dimethoxytrityl)-2'-O,4'-C-methylene-5-methyluridine is a derivative of LNA-type nucleoside.
Magnesium citrate is a magnesium salt form that provides efficient penetration into brain and muscle tissue. Magnesium citrate increases pain threshold and reduces TLR4 concentration in the brain. Orally active[1].
Artemitin is a flavonol found in Laggera pterodonta (DC.) Benth., with antioxidative, anti-inflammatory, and antiviral activity[1].
Amino-PEG4-C1-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Esculentoside A (EsA), a kind of triterpene saponin isolated from roots of Phytolacca esculenta[1].Esculentoside A (EsA) possesses anti-inflammatory activity in acute and chronic experimental models[2], has selective inhibitory activity towards cyclooxygenase-2 (COX-2)[1].Esculentoside A (EsA) suppresses inflammatory responses in LPS-induced acute lung injury (ALI) through inhibition of the nuclear factor kappa B (NF-ΚB) and mitogen activated protein kinase (MAPK) signaling pathways[3].
ARN726 is a potent, selective, orally bioavailable N-acylethanolamine acid amidase (NAAA) inhibitor with IC50 of 63 nM (r-NAAA) and 27 nM (h-NAAA); shows no interaction with a panel of 28 biologically relevant targets comprising lipid-metabolizing and inflammation-related enzymes; exerts profound anti-inflammatory effects in both mouse models and human macrophages.
(Val2)-Amyloid β-Protein (1-6) is a biologically active peptide.
Boscalid is an anti-fungal agent. Boscalid is a succinate dehydrogenase (SDH) inhibitor[1].
(1R,3R,4R,7S)-3-(4-Amino-5-methyl-2-oxopyrimidin-1(2H)-yl)-1-((bis(4-methoxyphenyl)(phenyl)methoxy)methyl)-2,5-dioxabicyclo[2.2.1]heptan-7-yl (2-cyanoethyl) diisopropylphosphoramidite is a phosphoramidite that can be used in the synthesis of oligonucleotides.
Thiabendazole inhibites the mitochondrial helminth-specific enzyme, fumarate reductase, with anthelminthic property. Target: Fumarate ReductaseTiabendazole serves to block angiogenesis in both frog embryos and human cells. It has also been shown to serve as a vascular disrupting agent to reduce newly established blood vessels. Tiabendazole has been shown to effectively do this in certain cancer cells. Thiabendazole works by inhibition of the mitochondrial, helminth-specific enzyme, fumarate reductase, with possible interaction with endogenous quinone [1].Thiabendazole inhibited B16F10 proliferation in vitro in a dose- and time-dependent manner with an IC50 of 532.4 +/- 32.6, 322.9 +/- 28.9, 238.5 +/- 19.8 microM at 24, 48, and 72 h, respectively. Moreover, thiabendazole inhibited the angiogenesis and the migration of B16F10 cells in vitro. Furthermore, thiabendazole restrained transcription and translation of the VEGF gene in B16F10 in vitro, and the apoptotic percentage of B16F10 cells was increased after exposure to thiabendazole [2].
Bursehernin (Methylpluviatolide) is an antitumor agent. Bursehernin induces Apoptosis and cell cycle arrest at G2/M phase. Bursehernin shows anti-proliferative activity[1][2].
Ligustrazine (hydrochloride) is a natural product.IC50 value:Target:In vitro: Ligustrazine hydrochloride displayed a protection effect on injured ECV304 cells, NOS and NO formation were significantly increased compared with the model group [1].In vivo:
18BIOder is a neuroprotective inhibitor of GSK-3β, highly selectively inhibiting HIV-1. It is the second generation derivative of 6BIO.
Pifithrin-β is a potent p53 inhibitor with an IC50 of 23 μM.
TVD-0003510 is a carboxamide derivative, and involves in synthesis of (2-((6-(2-aminopyrimidine-5-carboxamido)-8-methoxy-3,4-dihydro-2H-pyrimido[1,2-c]quinazolin-9-yl)oxy)ethyl)piperazine-l-carboxylate (C51), as a part of tert-butyl2-(4-hydroxyphenyl)acetate[1].
Djalonensone, isolated from the roots of Anthocleista djalonensis (Loganiaceae), is an important taxonomic marker of the plant species[1].
Carmofur is a derivative of fluorouracil, an antimetabolite used as an antineoplastic agent. Target: Nucleoside antimetabolite/analogCarmofur, which is used in the clinic to treat colorectal cancers, is a potent AC inhibitor and that this property is essential to its anti-proliferative effects. Carmofur inhibited AC activity with a median effective concentration (IC50) of 29 ± 5 nM (mean ± standard error of the mean, s.e.m.; n = 4), whereas 5-FU had no such effect (IC50>1 mM). systemic administration of carmofur (10 or 30 mg-kg-1, intraperitoneal, i.p.) to mice produced a dose-dependent inhibition of AC activity in various tissues, including lungs and brain cortex.