Raloxifene-d10-1 is the deuterium labeled Raloxifene[1]. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research[2].
Potassium tert-butyl malonate is an intermediate in the synthesis of malonate monoester potassium salt[1].
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]
Cinnamycin is tetracyclic lantibiotic produced from S. cinnamoneus that contains four unusual amino acids: erythro-β-hydroxyaspartic acid, mesolanthionine, threo-β-methyllanthionine, and lysinoalanine.1 Cinnamycin has demonstrated antiviral activity against herpes simplex virus type 1 KOS strain infection in Vero cells via a cytopathic effect reduction assay. Cinnamycin recognizes the structure of phosphatidylethanolamine and forms an equimolar complex with the phospholipid on biological membranes. This peptide has been used as a probe for analyzing the transbilayer movement of phosphatidylethanolamine.
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].
Coumarinic acid is a brain-penetrating inhibitor of AChE and β-amyloid. Coumarinic acid can be used in study anti-Alzheimer drug[1].
Theaflavine-3,3'-digallate, a bioactive black tea phenolic, can be used for the research of gut microbiota composition modulatory effects[1].
(R)-(-)-α-Methylhistamine dihydrochloride is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a Kd of 50.3 nM[1][2]. (R)-(-)-α-Methylhistamine dihydrochloride can enhance memory retention, attenuates memory impairment in rats[3][4][5].
Eucalyptin is a flavonoid. Eucalyptin can be isolated from Myrcia citrifolia[1].
Iopanoic acid is an inhibitor of 5'-Deiodinase and also an iodinated contrast medium.
(S,R,S)-AHPC-C3-NH2 (dihydrochloride) is the dihydrochloride form of (S,R,S)-AHPC-C3-NH2 (HY-130711). (S,R,S)-AHPC-C3-NH2 (VH032-C3-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader[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].
Elastatinal is a potent and competitive inhibitor of elastase, with a Ki of 0.21 μM. Elastatinal more potently inhibits pancreatic elastase versus leucocyte elastase. Elastatinal shows no activity on human leucocyte chymotrypsin-like protease[1][2][3][4].
PAβN dihydrochloride (MC-207110 dihydrochloride) is an efflux pump inhibitor.
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].
Ethyl (4-(trifluoromethoxy)phenyl)glycinate is a Glycine (HY-Y0966) derivative[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].
Antimycobacterial agent-1 (compound 33) has selectively antimycobacterial activity against Mycobacterium tuberculosis (M. tuberculosis) H37Ra with a MIC value of 1 μg/ml. Antimycobacterial agent-1 has relatively low cytotoxicity in normal cells (Vero cells IC50 = 143.2 μg/ml)[1].
Cefroxadine (CGP 9000) is an orally active cephalosporin antibiotic. Cefroxadine is more effective than cephalexin against Escherichia coli and Klebsiella pneumoniae with MIC values of 3.13 and 1.56 μg/mL respectively with a concentration of 106 μg/mL. Cefroxadine can be used for the research of infection[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].
Phenylthiourea (Phenylthiocarbamide) is an inhibitor of phenoloxidase. Phenylthiourea inhibits enzymatic oxidation of DOPA by phenoloxidase (Ki: 0.21?μM)[1].
Ganoderenic acid C is a triterpenoid isolated from Ganoderma lingzhi. Ganoderenic acid C is abundant in fruit bodies at an early growth stage[1].
Tetrakis (4-carboxyphenyl) porphyrin (TCPP) plays the role of a metal remover[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].
Schisandrol B is one of its major active constituents of traditional hepato-protective Chinese medicine, Schisandra sphenanthera.IC50 value:Target:in vitro: SolB pretreatment significantly attenuated the increases in alanine aminotransferase and aspartate aminotransferase activity, and prevented elevated hepatic malondialdehyde formation and the depletion of mitochondrial glutathione (GSH) in a dose-dependent manner. SolB also dramatically altered APAP metabolic activation by inhibiting the activities of CYP2E1 and CYP3A11, which was evidenced by significant inhibition of the formation of the oxidized APAP metabolite NAPQI-GSH [1]. SolB abrogated APAP-induced activation of p53 and p21, and increased expression of liver regeneration and antiapoptotic-related proteins such as cyclin D1 (CCND1), PCNA, and BCL-2.
Alpha-cyperone is associated with the down-regulation of COX-2,IL-6,Nck-2,Cdc42 and Rac1, resulting in reduction of inflammation. which would be highly beneficial for treatment of inflammatory diseases such as AD.In vitro: The anti-inflammatory activity of alpha-cyperone is associated with the down-regulation of COX-2 and IL-6 via the negative regulation of the NFκB pathway in LPS-stimulated RAW 264.7 cells.[1]Alpha-Cyperone binds and interacts with tubulin and is capable of distinctly destabilizing microtubule polymerization. The effect of this interaction could result in reduction of inflammation which would be highly beneficial for treatment of inflammatory diseases such as AD. One microliter of alpha-Cyperone was dissolved in DMSO (1:1 v/v) and it was further diluted in double distilled water (ddH2O) to a final volume of 20 microliter. [2]