Beclabuvir is an allosteric inhibitor that binds to thumb site 1 of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, and inhibits recombinant NS5B proteins from HCV genotypes 1, 3, 4, and 5 with IC50 of < 28 nM.
Antifungal agent 36 is a potent anti-fungal agent. Antifungal agent 36 shows anti-fungal activity for Basidiomycetes[1].
Fmoc-Glu(OMe)-OH is a glutamic acid derivative[1].
Phe-Gly hydrate is a Glycine (HY-Y0966) derivative[1].
Cinacalcet hydrochloride is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
Homatropine Bromide is muscarinic AChR antagonist that is an anticholinergic medication.Target: mAChRHomatropine is an anticholinergic medication that is an antagonist at muscarinic acetylcholine receptors and thus the parasympathetic nervous system. Homatropine (20 μM) alone produces a dose ratio of 259 in atrium from guinea-pigs. Homatropine (20 μM) produces a dose ratio of only 95.0 when combined with hexamethonium in atrium from guinea-pigs [1]. Homatropine has similar affinities for muscarinic receptors in stomach (pA2 = 7.13) and for those in atria mediating force (pA2 = 7.21) and rate (pA2 = 7.07) responses [2]. Homatropine [14C]methylbromide administrated rectal achieves higher and rapid peak plasma concentrations than by the other routes in rats whether HMB-14C is administered in a water-soluble suppository base or in aqueous solution, retained 28% of the 14C has been excreted in the urine while 56% remained in the large intestine after 12 hours. Unlabelled Homatropine methylbromide, given in rectal suppositories to anaesthetized rats, causes prompt blockade of the effects of vagal stimulation on pulse rate and of intravenous acetylcholine on blood pressure [3].
Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ, PKCδ and PKCζ with IC50 of 7 nM, 7 nM, 6 nM, 10 nM and 60 nM, respectively.
Methyl pentadecanoate-d29 is the deuterium labeled Methyl pentadecanoate[1].
5-Hydroxy-3,7-dimethoxyflavone (compound 1) can be isolated from Kaempferia parviflora, but has no significant toxicity to malaria parasites, fungi, and bacteria[1].
β-Boswellic acid is isolated from the gum resin of Boswellia serrate.β-Boswellic acid is a nonreducing-type inhibitor of the 5-lipoxygenase (5-LO) product formation either interacting directly with the 5-LO or blocking its translocation[1]. β-Boswellic acid inhibits the synthesis of DNA, RNA and protein in human leukemia HL-60 cells[2].
Pefloxacin mesylate dehydrate is a an antibacterial agent and prevents bacterial DNA replication by inhibiting DNA gyrase (topoisomerse)Target: DNA gyrasePefloxacin is a synthetic chemotherapeutic agent used to treat severe and life-threatening bacterial infections. Pefloxacin is commonly referred to as afluoroquinolone (or quinolone) drug and is a member of the fluoroquinolone class of antibacterials. It is an analog of norfloxacin. It is a synthetic fluoroquinolone, belonging to the 3rd generation of quinolones. Pefloxacin is extensively prescribed in France. Pefloxacin has not been approved for use in the United States.The bactericidal action of pefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited.
PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC50s of 450 nM and 622 nM, respectively[1][2]. PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor[3].
6-[(1R,2S)-2,3-dihydroxy-1-methoxy-3-methylbutyl]-7-methoxy- can be isolated from Angelica dahurica stem, for the first time from a plant source[1].
Malotilate is a liver protein metabolism improved compound, which selectively inhibit the 5-lipoxygenase. IC50 Value:Target: 5-lipoxygenasein vitro: In an in vitro invasion assay using rat lung endothelial (RLE) cells, invasion of tumor cells which had been treated with MT (10 ng/ml, 24 h) was not affected; however, when RLE cells had been treated with MT, invasion was significantly inhibited in three cell lines (SAS, Ca9-22 and HSC-4) and a tendency to inhibition was also observed in other cell lines [1].in vivo: The improvement rates for choline esterase activity were significantly greater in the malotilate group than in the control group. Serum albumin levels significantly increased in the malotilate group but not in the control group [2]. In the rats treated with MT for 19 days after i.v. inoculation of c-SST-2 cells, lung metastasis was also significantly suppressed [3]. Malotilate prevented increases in serum markers of type III and IV collagen synthesis as well as accumulation of the collagens, laminin and fibronectin in the liver [4].Toxicity: Malotilate cytotoxicity to PBMCs, assessed by trypan blue dye exclusion and lactate dehydrogenase (LDH) release into the culture media, was found to be markedly increased by the addition of the NADPH generating system, indicating that metabolites play a significant role in toxicity [5].
CFI-402257 is a highly selective and orally bioavailable TTK and Mps1 inhibitor with Kis of 0.1 and 0.09 nM, respectively.
Glutamic acid protease only can be found in fungi. Glutamic protease is a proteolytic enzyme containing a glutamic acid residue[1].
Mavacamten-d6 (MYK461-d6; SAR439152-d6) is deuterium labeled Mavacamten (HY-109037). Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
Levomecol (Chloramphenicol), made up of Chloramphenicol, Methyluracil, is a broad-spectrum antibiotic that is derived from the bacterium Streptomyces venezuelae. Levomecol (Chloramphenicol)) stops bacterial growth by binding to the bacterial ribosome (blocking peptidyl transferase) and inhibiting protein synthesis[1].
Andrograpanin, a bioactive compound from Andrographis paniculata, exhibits anti-inflammatory and anti-infectious properties[1][2].
Terminal deoxyribonucleotidyltransferase (TdT) catalyses the condensation of deoxyribonucleotide triphosphates onto the 3' hydroxyl ends of DNA strands and adds N-regions to gene segment junctions during V(D)J recombination. Terminal deoxyribonucleotidyltransferase is expressed in immature, pre-B, pre-T lymphoid cells, and acute lymphoblastic leukemia/lymphoma cells[1].
PI3K/mTOR Inhibitor-3 (compound 12), an imidazoline, is a potent PI3K and mTOR dual inhibitor. PI3K/mTOR Inhibitor-3 has anti-cancer activity[1].
Boc-D-Phe-OH is a phenylalanine derivative[1].
Tibenelast sodium is a phosphodiesterase inhibitor.
Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist.
4-Nitrophenyl 2-O-(β-L-Fucopyranosyl)-β-D-Galactopyranoside is a synthetic chromogenic substrate and can be used in the assay of α-fucosidases which hydrolyze the glycosidic linkage Fuc α1-2Gal. The assay is based on the sequential action of α-fucosidase and an exogenously added exo-β-d-galactosidase to release the easily measurable p-nitrophenol moiety[1].
Sanshool is a major component in Zanthoxylum bungeanum. Sanshool improves UVB-induced skin photodamage by targeting JAK2/STAT3-dependent autophagy[1].
Z-Glu-OtBu is a glutamic acid derivative[1].
Bis-PEG13-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Isocupressic acid ((+)-Isocupressic acid) is an abortifacient compound[1].