GTS-21 dihydrochloride is a selective α7 nicotinic acetylcholine receptor agonist, has recently been established as a promising treatment for inflammation. Target: nAChRin vitro: GTS-21 is one of the most potent α7nAChR agonists, has been reported to attenuate pro-inflammatory cytokine production, improve outcomes in sepsis models, pancreatitis, and ischemia-reperfusion injury, and inhibit the production of endotoxin-induced TNF in lung tissue. In addition, recent studies have demonstrated that GTS-21 inhibits the activities of endothelial cells and monocyte macrophages, as well as the secretion of pro-inflammatory cytokines in peripheral blood samples, by regulating the JAK2-STAT3 pathway. [1] in vivo: In septic animals, GTS-21 significantly ameliorated GI motility, lowered systemic and colonic levels of IL-6, decreased colonic permeability, and decreased the number of positive cultures obtained from blood and mesenteric lymph nodes. Splenectomy prevented animals from developing sepsis-induced ileus. Chrna7 mice displayed a more severe septic phenotype, whereas GTS-21 remarkably was also beneficial in these animals. [2]
Eburicoic acid protects the liver from CCl4-induced hepatic damage via antioxidant and anti-inflammatory mechanisms[1]. And Eburicoic acid has antidiabetic and antihyperlipidemic effects[2].
Theaflavine-3,3'-digallate, a bioactive black tea phenolic, can be used for the research of gut microbiota composition modulatory effects[1].
Eucalyptin is a flavonoid. Eucalyptin can be isolated from Myrcia citrifolia[1].
GSK3β inhibitor II is an inhibitor of GSK3β. GSK3β inhibitor II can be used for research of Alzheimer’s disease (AD)[1].
Dacomitinib (PF-00299804) hydrate is an orally active, irreversible pan-ErbB inhibitor. Dacomitinib hydrate can be used in the research of cancers such as metastatic non-small cell lung cancer (NSCLC)[1].
PF-184298 is a potent, selective dual serotonin and noradrenaline monoamine reuptake inhibitor (SNRI) with IC50 of 6 nM and 21 nM, respectively; displays good selectivity over dopamine reuptake inhibition (DRI) (IC50=544 nM); possesses good in vitro metabolic stability, weak CYP inhibition and drug-like physicochemical properties consistent with CNS target space.
Boc-Glu(OBzl)-Gly-Arg-AMC is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development[1].
Hu7691 free base is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 free base inhibits tumor growth and enables decrease of cutaneous toxicity in mice[1].
4-Chloro-7-(2-deoxy-β-D-erythro-pentofuranosyl)-5-iodo-7H-pyrrolo[2,3-d]pyrimidine is a pyrimidine nucleoside analog. Pyrimidine nucleoside analogs have a wide range of biochemical and anticancer activities. These include DNA synthesis inhibition, RNA synthesis inhibition, antiviral effects, and immunomodulatory effects[1].
E3 ligase Ligand 18 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 18 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins[1].
Phenylthiourea (Phenylthiocarbamide) is an inhibitor of phenoloxidase. Phenylthiourea inhibits enzymatic oxidation of DOPA by phenoloxidase (Ki: 0.21?μM)[1].
Acetylexidonin is a diterpenoid compound with anti-inflammation and cancer activity. Acetylexidonin inhibits tumor cells with IC50s of 3.69 μM (NB4) and 26.22 μM (SHSY5Y), respectively[1].
Bosutinib isomer is a ligand or inhibitor with high binding affinity for both Wee1 and Wee2, with Kd values of 43.7 ± 10.0 and 4.7 ± 2.3 nM, respectively[1].
P1 is a broad-spectrum antimicrobial peptide. P1 shows antibacterial activity against Gram-positive and Gram-negative bacteria,such as B. anthracis spores and Carbapenem-resistant A. baumannii and K. pneumoniae[1].
Sodium cyanoboronhydride-d3 is the deuterium labeled Sodium cyanoboronhydride[1].
ACTH (1-13) is a 13-aa peptide, with cytoprotective effects in the model of ethanol induced gastric lesions in rats.
Vesencumab (MNRP-1685A) is IG1 antibody against neuropilin-1 (NRP-1). Vesencumab binds to NRP-1 and prevents the subsequent coupling of NRP-1 to VEGFR-2. Vesencumab has anti-angiogenic and anti-neoplastic activities. Vesencumab can be used in the research of metastatic solid tumors, including ovarian cancer[1][2].
DMEA-PNU-159682 (molecule D12) is a ADC cytotoxin molecule including metabolites of nemorubicin (MMDX) from liver microsomes and a potent ADCs cytotoxin PNU-159682[1][2].
Sodium 2-aminoacetate is a Glycine (HY-Y0966) derivative[1].
Myristoyl tetrapeptide-12 directly activates SMAD2 and induces the linking of SMAD3 with DNA. Myristoyl tetrapeptide-12 is capable of stimulating hair growth, especially at the level of eyelashes[1][2].
ALK-IN-1 is a potent and selective active inhibitor of anaplastic lymphoma kinase(ALK), Patent US20140066406 A1.
Harmine Hydrochloride (Telepathine Hydrochloride) is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM[1].
Thymidine-5'-diphosphate-L-rhamnose disodium can be isolated from Occhromonas malhamensis[1].
Blonanserin(AD-5423) is a D2/5-HT2 receptor antagonist, atypical antipsychotic. Target: D2 receptor; 5-HT2 receptorBlonanserin(AD-5423) is a relatively new atypical antipsychotic for the treatment of schizophrenia. Blonanserin belongs to a series of 4-phenyl-2-(1-piperazinyl)pyridines and acts as an antagonist at dopamine D2, D3, and serotonin 5-HT2A receptors. Blonanserin has low affinity for 5-HT2C, adrenergic α1, histamine H1, and muscarinic M1 receptors, but displays relatively high affinity for 5-HT6 receptors [1]. AD-5423 bound preferentially to dopamine (DA)-D2 (Ki, 14.8 nM; cf. haloperidol, 8.79 nM; and clozapine, 149 nM) and serotonin (5-HT)-S2 (Ki, 3.98 nM; cf. haloperidol, 26.8 nM; and clozapine, 8.66 nM) receptors. It displayed low affinity for adrenaline (Ad)-alpha-1 (Ki, 56.3 nM) receptors and was virtually devoid of binding to DA-D1 (Ki, 2870 nM), 5-HT-S3, Ad-alpha-2, Ad-beta, muscarine, tau-aminobutyric acid and benzodiazepine receptors. In addition, AD-5423 was only a weak inhibitor of DA, 5-HT and noradrenaline uptake systems. AD-5423 (0.2-2 mg/kg p.o.) decreased exploratory activity in mice. AD-5423 (10 mg/kg p.o.), unlike haloperidol, did not antagonize SKF38393-induced vacuous oral movements in rats. Head twitches induced by 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane in mice and by para-chloroamphetamine in rats were antagonized by AD-5423 at much lower doses (0.5-2 mg/kg p.o.) than those of haloperidol and clozapine [2].
Z-D-Dbu(N3)-OH is a click chemistry reagent containing an azide group. Z-D-Dbu(N3)-OH can be used for the research of various biochemical[1].
Conglobatin (FW-04-806), a macrolide dilactone, is isolated from the culture of Streptomyces conglobatus. Conglobatin is an orally active Hsp90 inhibitor. Conglobatin can bind to the N-terminal domain of Hsp90 and disrupt Hsp90-Cdc37 complex formation. Conglobatin induces apoptosis in human breast cancer cells and esophageal squamous cell carcinoma cells, and exhibits antitumor activity in vivo[1][2][3].
PBB3, a selective PET ligand, recognizes tau pathology in Alzheimer's disease brains, where dystrophic neurites and diffuse neurofibrils are more clearly detected Tangles with calcification[1].
FATP1-IN-2, as an arylpiperazine derivative, is an orally active fatty acid transport protein 1 (FATP1) inhibitor (human IC50=0.43 μM, mouse IC50=0.39 μM)[1].
Rose-β-D-Gal is a flurescent dye, is also a β-galactosidase substrate. Rose-β-D-Gal creates a pink/magenta color after the reaction and has been used for detection of β-gal activity[1][2].