Angiogenesis inhibitor 4 is a potent angiogenesis inhibitor. Angiogenesis inhibitor 4 can be used in research of cancer[1].
KX2-391 Mesylate is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.
Presatovir (GS-5806) is a novel, orally bioavailable RSV fusion inhibitor with a mean EC50 value of 0.43 nM.
5-[(2-Nitrophenyl)methylene]-2,4-thiazolidinedione (Compound 4) has antimicrobial, anti-diabetic and antioxidant activities. 5-[(2-Nitrophenyl)methylene]-2,4-thiazolidinedione inhibits B. subtilis, S. aureus, K. pneumonia, E. coli, and S. typhi with MICs of 4.5-9.9 μΜ/mL, and inhibits A. niger and C. albicans with MICs of 4.99 μΜ/mL[1].
KU14R is a new I(3)-R antagonist, which selectively blocks the insulin secretory response to imidazolines.IC50 Value:Target: Insulin ReceptorA new I(3)-R antagonist, KU14R (2 (2-ethyl 2,3-dihydro-2-benzofuranyl)-2-imidazole), which selectively blocks the insulin secretory response to imidazolines. KU14R partially attenuated responses to Imidazole-4-acetic acid-ribotide (IAA-RP). The effects of KU14R on stimulus secretion-coupling in normal mouse islets and beta cells was compared by measuring KATP channel activity, plasma membrane potential, cytosolic calcium concentration ([Ca2+]c) and dynamic insulin secretion. In the presence of 10 mmol/l but not of 5 mmol/l glucose, KU14R (30, 100 or 300 micromol/l) was ineffective. KATP channel was blocked by KU14R (IC50 31.9 micromol/l, Hill slope -1.5). KU14R does not act as an antagonist of either efaroxan or S22068 at an imidazoline site in vivo.
Avanafil (TA-1790) dibenzenesulfonate is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil dibenzenesulfonate activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil dibenzenesulfonate inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil dibenzenesulfonate can be used for the research of erectile dysfunction and osteoporosis[1][2][3].
AChE/Nrf2 modulator 1 is an orally active acetylcholinesterase (AChE)/nuclear factor erythroid 2-related factor 2 (Nrf2) modulator. AChE/Nrf2 modulator 1 has Nrf2 inductive activity and AChE inhibitory activity for eeAChE and hAChE with IC50 values of 0.07 μM and 0.38 μM, respectively. AChE/Nrf2 modulator 1 can be used for the research of Alzheimer's disease[1].
Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with an IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65 .
Fulvotomentoside B is a saponin isolated from Lactobacillus flavus. Fulvotomentoside compounds can significantly reduce serum glutamate pyruvate transaminase (SGPT) and triacylglycerol (GT) levels in mice poisoned by CCl4, d-galactosamine (d-gal) and acetaminophen, and significantly alleviate liver pathology. damage[1].
Yamogenin (Neodiosgenin) is a diastereomer of diosgenin. Yamogenin (Neodiosgenin) antagonizes the activation of the liver X receptor (LXR) in luciferase ligand assay. Yamogenin (Neodiosgenin) inhibits triacylglyceride (TG) accumulation through the suppression of gene expression of fatty acid synthesis in HepG2 hepatocytes[1].
L-β-Homoglutamine hydrochloride is a glutamine derivative[1].
Erythro-Guaiacylglycerol beta-coniferyl ether (compound 22) can be isolated from the stems and leaves of mung beans. Erythro-Guaiacylglycerol beta-coniferyl ether inhibits α-Glycosidase activity with EC50 value of 18.71 μM[1].
(+)-KCC2 blocker 1 is a selective K+-Cl- cotransporter KCC2 blocker with an IC50 of 0.4 μM. (+)-KCC2 blocker 1 is a benzyl prolinate and a enantiomer of KCC2 blocker 1[1].
Isophysalin A is a physalin with alpha and beta unsaturated ketone components. Isophysalin A binds to GSH and targets multiple cysteine residues on IKKβ. Isophysalin A also inhibits inducible NO synthase (iNOS) and nitric oxide (NO) production, showing anti-inflammatory activity[1].
Levofloxacin hydrate is an antibacterial agent that inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication.Target: AntibacterialLevofloxacin reduced bacterial load compared with placebo by 4.9-fold (95% confidence interval, 1.4-25.7; P=0.02) at day 7 but had no effect at any point on any marker of neutrophilic airway inflammation. In patients with a baseline bacterial load of more than 10(6) cfu/mL, levofloxacin treatment was associated with a 26.5% (95% confidence interval, 1.8%-51.3%; P=0.04) greater reduction in the percentage neutrophil count compared with placebo at day 7 [1]. Levofloxacin was found to significantly improve the clinical and microbiological parameters in CP individuals [2]. A 30-day course of levofloxacin does not significantly improve BK viral load reduction or allograft function when used in addition to overall reduction of immunosuppression [3].
α,β-Methylene ATP trisodium, a phosphonic analog of ATP, is a P2X3 and P2X7 receptor ligand[1].
Dibenzo(a,i)pyrene-d14 is the deuterium labeled Dibenzo(a,i)pyrene[1].
Ontuxizumab (MORAb-004) is a humanized IgG1/κ anti-endosialin (TEM-1 or CD248) monoclonal antibody with antitumor effects. Ontuxizumab can be used for the research of cancer[1].
PROTAC BRD4 ligand-1 is a potent BET inhibitor and a ligand for target BRD4 protein for PROTACT[1].
β3-AR agonist 1 (compound 15) is a highly potent, selective, and orally available β3-adrenergic receptor (β3-AR) agonist (EC50=18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold)[1].
Aristolactam BIII is a potent DYRK1A inhibitor and inhibits the kinase activity of DYRK1A in vitro (IC50= 9.67 nM. Aristolactam BIII rescues the proliferative defects of DYRK1A transgenic (TG) mouse-derived fibroblasts and neurological and phenotypic defects of DS-like Drosophila models[1].
Indirubin(Couroupitine B) is a purple 3,2- bisindole and a stable isomer of indigo isolated from Indigo naturalis (Apiaceae); anti-inflammatory and anticancer activities.IC50 value:Target:in vitro: The activation of EGF receptor, known to be highly expressed in psoriatic lesions, was inhibited by indigo naturalis or indirubin. The cell proliferation and CDC25B expression of epidermal keratinocytes were induced by EGF alone and confirmed to be inhibited by indigo naturalis or indirubin [2]. indirubin inhibited prostate tumor growth through inhibiting tumor angiogenesis. indirubin inhibited angiogenesis in vivo. We also showed the inhibition activity of indirubin in endothelial cell migration, tube formation and cell survival in vitro [3].in vivo: Indirubin treatment suppressed skin inflammation in DNCB-exposed mice. The skin lesions were significantly thinner in the Indirubin-treated group than in untreated controls, and the hyperkeratosis disappeared. Indirubin reduced the total serum IgE level and cytokines production. In addition, it normalized NF-κB, IκB-α and MAP kinase expression [1]. Indirubin dose-dependently inhibited intersegmental vessel formation in zebrafish embryos. It also inhibited HUVEC proliferation by the induction of cellular apoptosis and cell-cycle arrest at the G0/G1 phase [4].
AR7 is a retinoic acid receptor α (RARα) antagonist.
(S)-Falcarinol (Panaxynol), one of the major polyacetylenes isolated from Panax ginseng, has antitumor activity. (S)-Falcarinol (Panaxynol) is the most potent antiplatelet agent in ginseng and its mechanism of action is chiefly due to the inhibition of thromboxane formation. (S)-Falcarinol (Panaxynol) is a potent Nrf2 activator[1][2][3].
Peptide R, a cyclic peptide, is a specific CXCR4 antagonist. Peptide R shows outstanding capacities to profoundly remodel the tumor stroma. Peptide R has the potential for tumor research[1][2].
Aspartyl-alanyl-diketopiperazine (DA-DKP) is an immunomodulatory molecule generated by cleavage and cyclization from the N-terminus of human albumin and can modulate the inflammatory immune response through a molecular pathway implicated in T- lymphocyte anergy[1][2].
Efalizumab is a targeted T cell modulator, and is a humanized monoclonal antibody of CD11a, the α subunit of LFA-1. Efalizumab inhibits T cell activation, cutaneous T cell trafficking, and T cell adhesion to keratinocytes, can be used for plaque psoriasis research[1].
GEMSA is a potent inhibitor of enkephalin convertase (Ki=8.8 nM). GEMSA elicites analgesia[1].
Efaproxiral is a synthetic allosteric modifier of haemoglobin (Hb), decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy.in vitro: Efaproxiral increases oxygen levels in hypoxic tumor tissues by binding non-covalently to the hemoglobin tetramer and decreasing hemoglobin-oxygen binding affinity. Increasing tumor oxygenation reduces tumor radioresistance. Efaproxiral can enhance the oxygenation of hypoxic tumours and function as a radiation sensitiser, increasing the effectiveness of RT.
Ganglioside GM3 is a precursor of a-, b-, and c-series gangliosides, interacts with transmembrane receptors such as the epidermal growth factor and insulin receptors, and regulates receptor functions by creating a specialized lipid environment. Ganglioside GM3 is synthesized by GM3 synthase and can be used for the research of hypercholesterolemia[1].