Tesidolumab (LFG316) is a fully-human IgG1/λ anti-C5 monoclonal antibody of 143 kDa (without glycosylation). Tesidolumab (LFG316) blocks cleavage of C5 and prevents subsequent formation of the membrane attack complex[1].
3β-Hydroxy-hop-22(29)-ene (compound 3) is a potent antiparasitic agent. 3β-Hydroxy-hop-22(29)-ene shows moderate activity against Trypanosoma cruzi and Leishmania mexicana[1].
1,1-Dibromo-3-chloroacetone is a halogenated ozone-chlorine and ozone chloramine disinfection byproducts (DBPs) at elevated bromide levels when chlorine or chloramine is used as a secondary disinfectant[1].
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel derivative with improved pharmacological features and higher water solubility.IC50 value:Target: Microtubule inhibitor10-Deacetyl-7-xylosyl paclitaxel induced mitotic cell cycle arrest and apoptosis as measured by flow cytometry, DNA laddering, and transmission electron microscopy. Pro-apoptotic Bax and Bad protein expression was up-regulated and anti-apoptotic Bcl-2 and Bcl-XL expression down-regulated, which lead to a disturbance of the mitochondrial membrane permeability and to the activation of caspase-9. In turn, caspase-9 activated downstream caspases-3 and -6, but not caspase-8. Bid was also activated by caspase-3. Reversely, treatment with a caspase-10-specific inhibitor could not protect PC-3 cells from 7-xylosyl-10-deacetyl-paclitaxel-triggered apoptosis. Moreover, 7-xylosyl-10-deacetylpaclitaxel had no effect on the expression of CD95 and NF-kappaB proteins, indicating that apoptosis was induced through the mitochondrial-dependent pathway in PC-3 cells.
YW1128 is an inhibitor of Wnt/��-catenin signaling with an IC50 value of 4.1 nM in a reporter assay.
Erythromycin stearate is a macrolide antibiotic produced by actinomycete Streptomyces erythreus with a broad spectrum of antimicrobial activity. Erythromycin stearate binds to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid[1][2]. Erythromycin stearate also exhibits antitumor and neuroprotective effect in different fields of research[3][4].
MA242 free base is a specific dual inhibitor of MDM2 and NFAT1. MA242 free base directly binds both MDM2 and NFAT1 with high affinity, induces their protein degradation, and inhibits NFAT1-mediated transcription of MDM2. MA242 free base induces apoptosis in pancreatic cancer cell lines regardless of p53 status[1].
BTTP is a tris(triazolylmethyl)amine-based ligand. BTTP can accelerate the copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC), the prototypical reaction in click chemistry[1].
3-hydroxycoumarin is a potent and redox inhibitor of human 15-LOX-1. 3-hydroxycoumarin is recently demonstrated to protect sea urchin reproductive cells against ultraviolet B damage[1][2].
(R)-Monlunabant ((R)-MRI-1891) is a CB1 receptor mediators for research of obesity and metabolic disease[1]
Dimethocaine is a local anesthetic with reported stimulant properties most similar to cocaine.
Bombesin is a tetradecapeptide originally isolated from frog skin; plays an important role in the release of gastrin and the activation of G-protein receptors.
Cimdelirsen is a novel, ligand-conjugated, hepatic-targeted investigative antisense oligonucleotide designed to reduce growth hormone receptor (GHr) synthesis, thereby inhibiting deleterious effects of growth hormone (GH) hypersecretion and reducing circulating insulin-like growth factor-1 (IGF-1) levels in acromegaly patients.
Methylenetanshinquinone is a natural compound with antiplasmodial, antitrypanosomal and antioxidative activities. Methylenetanshinquinone can be used for the research of parasite infection[1].
Lumiliximab (Anti-CD23 Recombinant Antibody) is an anti-CD23 monoclonal antibody that inhibits allergen-induced responses[1].
5-O-beta-D-Glucopyranosylmyricanol is a diarylheptane compound isolated from Myrica esculenta that has a weak inhibitory effect on angiotensin-converting enzyme (ACE)[1].
Baccatin III is a natural product isolated from Pacific yew tree and related species. Baccatin III reduces tumor progression by inhibiting the accumulation and suppressive function of MDSCs[1].
Taniborbactam hydrochloride (VNRX-5133 hydrochloride) is a reversible and selective boronic acid-containing pan-spectrum β-lactamase inhibitor with IC50s of 8-530 nM. Taniborbactam hydrochloride has IC50s of 30 nM, 32 nM, 42 nM, 20 nM for KPC-2, AmpC, OXA-48, and VIM-2. Taniborbactam hydrochloride is against Gram-negative bacteria[1][2].
Resomelagon (AP1189) is a potent, orally active melanocortin receptor (MR) agonist. Resomelagon induces ERK1/2 phosphorylation and Ca2+ mobilization. Resomelagon has anti-inflammatory activity. Resomelagon can be used for obesity and chronic inflammation research[1][2].
PGD2-IN-1 is an antagonist of DP extracted from patent WO 2006044732 A2, example 15 (d); has an IC50 of 0.3 nM.
4,6-O-ethylidene-α-D-glucose (Ethylidene-glucose), a glucose derivative, is a competitive exofacial binding-site inhibitor on glucose transporter 1 (GLUT1) with a Ki of 12 mM for wild-type 2-deoxy-D-glucose transport[1][2][3].
AZD4547 is a potent inhibitor of the FGFR family with IC50s of 0.2 nM, 2.5 nM, 1.8 nM, and 165 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.
Flumatinib mesylate (HH-GV-678 mesylate), a derivative of imatinib, is a multi-kinase inhibitor with IC50 Values of 1.2 nM, 307.6 nM and 2662 nM for c-Abl, PDGFRβ and c-Kit respectively.IC50 Value: 1.2 nM (c-Abl); 307.6 nM(PDGFRβ); 2662 nM (c-Kit) [1]Target: c-Abl; c-Kit; PDGRFβin vitro: HH-GV-678 can predominantly inhibit the autophosphorylation of Bcr-Abl in K562 cell. In higher concentration, HH-GV-678 can inhibit the phosphorylation of c-Kit in Mo7e cell and the phosphorylation of PDGFR in Swiss3T3 cell, however, HH-GV-678 has no or little effect on other tyrosine kinase including EGFR/KDR/c-Src andHER2 [1]. Flumatinib effectively overcame the drug resistance of certain KIT mutants with activation loop mutations (i.e., D820G, N822K, Y823D, and A829P) [2].in vivo: The purpose of this study was to identify the metabolites of flumatinib in CML patients, with the aim of determining the main metabolic pathways offlumatinib in humans after oral administration. Ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry revealed 34 metabolites; 7 primary metabolites were confirmed by comparison with synthetic reference standards. The results show that the parent drugflumatinib was the main form recovered in human plasma, urine, and feces. The main metabolites of flumatinib in humans were the products of N-demethylation, N-oxidation, hydroxylation, and amide hydrolysis [3].
Tomuzotuximab (Anti-Human EGFR Recombinant Antibody) is a fully human glycoengineered IgG1 monoclonal antibody against EGFR. Tomuzotuximab has anticancer effects[1].
P-gp inhibitor 5 (compound 10) is a potent P-glycoprotein (P-gp) inhibitor with P-gp inhibition fold of 2.5 and 3.0 at 1.25 μM and 2.5 μM. P-gp inhibitor 5 has antiproliferative activity against certain cancer cell lines. P-gp inhibitor 5 is effective in reversing the multidrug resistance (MDR) phenotype in ABCB1/Flp-InTM-293 and KBvin cells by restoring their sensitivity to Vincristine and Paclitaxel[1].
Methyl decanoate is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
C13-113-tri tail is a cationic lipid-like compound containing a polar amino alcohol head group, three hydrophobic carbon-13 tails, and a tertiary amine linker. C13-113-tri tail can be formulated into a lipid nanoparticle (LNP).
Xylose-5-13C is the 13C labeled Xylose.
Tetramethylammonium-d12 (chloride) is the deuterium labeled Tetramethylammonium chloride[1].
C80-1324 is a furoxan compound. C80-1324 reveals marked dilator activity in the coronary circulation of isolated working hearts.