{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
Polyoxins are antifungal antibiotics produced by Streptomycetes that were discovered through programs searching for new fungicides and insecticides for agricultural use. The polyoxins, first reported in the 1960s, were isolated from Streptomyces cacaoi. As inhibitors of chitin synthetase, they exhibit antifungal activity, but lack antibacterial activity. Since they also lack mammalian toxicity, they represent potentially useful models for the development of effective agents for the treatment of opportunistic fungal infections.The inhibitory effectiveness of polyoxin B (Polar) makes it a good candidate for the control of powdery mildews on grapevines, apple, and especially on nectarine trees. Polyoxin B is a chitin synthase (CHS) inhibitor with IC50 of 0.16 mM.
Centella asiatica (L. ) Urban is a tropical medicinal plant with a long history of therapeutic uses. Terminolic acid, is a constituent of Centella asiatica, significantly decreases interleukin-8 production in human colon cancer cells. In addition, its inhibitory activity of against promyelocytic leukemia HL-60 and human erythromyeloblastoid leukemia K562 cell lines was also evaluated. It was found, that terminolic acid possesses moderate antibacterial activity against Staphylococcus aureus, Escherichia coli and Enterococcus faecalis
beta-apo-Oxytetracycline is the degradation product of Oxytetracycline. It exhibits greater toxicity compared with the parent compound. The toxic effects of beta-apo-Oxytetracycline treatment could damage liver and kidney tissues of rats, as well as lead to the degeneration and necrosis in the hepatocytes.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Rhodiola rosea L. (Golden Root) has been used for a long time as an adaptogen in Chinese traditional medicine and is reported to have many pharmacological properties. Sachaliside 1 was isolated from Rhodiola rosea L. It was discovered the inhibitory effects of Sachaliside 1 on tumor necrosis factor (TNF)-alpha production in the peritoneal macrophages of mice stimulated with lipopolysaccharide (LPS).
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Deoxyadenosine 5'-monophosphate (dAMP) is a derivative of adenosine monophosphate. dAMP is a monomer of DNA. It is produced by degradation of DNA by 5'-nucleotidases and is further metabolized to adenosine.
(1'R,2'S)-nicotine-1'-N-oxide is a stereoisomer of nicotine-1'-N-oxide, an oxidation product of S-(-)-nicotine. N-1'-oxidation of nicotine is mediated via flavin-containing monooxygenase. A marked stereoselectivity has been observed in the formation of N-1'-oxide metabolites from nicotine. Mammal hepatic preparations generally produce more the N-1'R,2'S-cis diastereoisomer than N-1'S,2'S-trans diastereoisomer after incubation with S-(-)-nicotine. cis- and trans-nicotine-N'-oxides modulate the development of tumors in rats initiated with N-[4-(5-nitro-2-furyl)-2-thiazolyl]formamide.
1-(Tetrahydro-2-furanyl)-5-fluorouracil, which is named Ftorafur or FT-207 or Tegafur (FT) is used clinically as an antitumor agent. This optically inactive compound was resolved into optically active (R)-(+)- and (S)-(-) isomers. Tegafur is a prodrug of 5-fluorouracil (5-FU) and the bioactivation to 5-FU is mainly catalyzed by cytochrome P450 (CYP) in hepatic microsomes. Although 5-FU was generated from both tegafur enantiomers, R-FT was a preferred substrate than S-FT, because of the considerably higher intrinsic clearance for 5-FU formation from R-FT in liver. The distinct kinetic profiles of the stereoisomers is apparently due to the stereoselective disposition of the R-isomer relative to the S-isomer. These data suggest that the R-isomer of FT is worthy of further preclinical and clinical evaluation for safety, efficacy, and pharmacokinetics.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
2-pyridine-3-yl-methylene-indan-1,3-dione (PRT-4165) is a potent inhibitor of PRC1-mediated H2A ubiquitylation in vivo and in vitro. The drug also inhibits the accumulation of all detectable ubiquitin at sites of DNA double-strand breaks (DSBs), the retention of several DNA damage response proteins in foci that form around DSBs, and the repair of the DSBs. In vitro E3 ubiquitin ligase activity assays revealed that PRT-4165 inhibits both RNF2 and RING 1A. PRT-4165 is an inhibitor of Bmi1/Ring1A, subunits of the polycomb repressive complex 1 (PRC1); inhibits self-ubiquitination (IC50 = 3.9 uM) but does not increase cellular levels of either subunit. Prevents Bmi1/Ring1A-mediated ubiquitination and drug-induced degradation of topoisomerase 2α (Top2α). Also shown to inhibit the in vitro E3 ubiquitin ligase activity of RNF2 and a Bmi1/RNF2 complex, inhibiting H2A/H2AX ubiquitination. Blocks polycomb repressor complex (PRC) 1-mediated histone H2A ubiquitination in vitro and in vivo. PRT-4165 can be used torapidly inhibit ongoing histone H2A ubiquitylation in cells.
This drug represents the first chemical inhibitor that is available
to inhibit the PRC1 E3 ubiquitin ligase and should provide
an important tool for gene expression studies.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Cyclopenol is naturally occurring 7-membered 2,5-dioxopiperazine alkaloid isolated from the extract of fungus Penicillium cyclopium , Penicillium sclerotiorum etc. Cyclopenol can be converted into the quinolone viridicatol, by the enzyme cyclopenase present in the conidia. Cyclopenol have phytotoxic and antimicrobial activities.
Ergosterol (9alpha: 10beat isomer), lumisterol (9beta: 10alpha isomer), isopyrocalciferol (9beta: 10beta isomer) and pyrocalciferol (9alpha: 10alpha isomer) are all epimers of one another at C-9 and C-10. Isopyrocalciferol and pyrocalciferol are products of over-radiation of the provitamin D. These steroids don’t have biological activity since they are not steroids.