2′,3′,5′-Triacetyl-5-azacytidine is an orally active prodrug of 5-Azacytidine. 5-Azacytidine is an inhibitor of DNA methyltransferase[1].
Flufenamic acid-13C6 is the 13C6 labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
CHMFL-ABL-039 is a type II native ABL kinase and drug-resistant V299L mutant BCR-ABL inhibitor with the IC50s of 7.9 nM and 27.9 nM, respectively. CHMFL-ABL-039 is used in the research of chronic myeloid leukemia[1].
Etesevimab (JS016) is a recombinant neutralizing human IgG1 anti-SARS-CoV-2 monoclonal antibody[1].
EZH2-IN-14 is a selective EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 12 nM. EZH2-IN-14 inhibits the methyltransferase activity of EZH2/PRC2 (that is, reducing H3K27me3). EZH2-IN-14 shows >200-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1[1].
Theaflavin-3-gallate, a black tea theaflavin monomer, is regarded as the biologically important active component of black tea and provides health benefits. Theaflavin-3-gallate acts as prooxidants and induces oxidative stress in the carcinoma cells. Theaflavin-3-gallate reacts directly with reduced glutathione (GSH) in a time- and concentration-dependent manner[1].
EPI-589, a quinone derivative, is a safe and well tolerated oxidoreductase enzyme inhibitor. EPI-589 has the potential for the treatment of amyotrophic lateral sclerosis (ALS)[1].
L-DOPA-13C is the 13C labeled L-DOPA[1]. L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease[2][3][4].
Rosamultin is a 19 α-hydroxyursane-type triterpenoid isolated from Potentilla anserina L. Rosamultin has inhibitory effects against HIV-1 protease[1]. Rosamultin has the potential for treating H2O2-induced oxidative stress injury through its antioxidant and antiapoptosis effects[2].
Tigecycline hydrochloride is a first-in-class, broad spectrum antibiotic with activity against antibiotic-resistant organisms.Target: AntibacterialTigecycline hydrochloride is active against a broad range of gram-negative and gram-positive bacterial species including clinically important multidrug-resistant nosocomial and community-acquired bacterial pathogens. Tigecycline hydrochloride has been shown to inhibit the translation elongation step by binding to the ribosome 30S subunit and preventing aminoacylated tRNAs to accommodate in the ribosomal A site [1]. Tigecycline hydrochloride has also been found to be effective for the treatment of community- as well as hospital-acquired and ventilator-associated pneumonia and bacteremia, sepsis with shock and urinary tract infections. Tigecycline hydrochloride appears to be a valuable treatment option for the management of superbugs, especially where conventional therapy has failed [2].Fifteen patients received tigecycline hydrochloride for 16 episodes of CPKP infection. The main infections were pneumonia (31%), urinary tract infection (31%), peritonitis (20%), catheter-related bacteraemia (12%), and meningitis (6%). Most infections were complicated with severe sepsis (44%), septic shock (12%), and/or bacteraemia (19%). The daily maintenance dose of tigecycline hydrochloride was 200 mg in 10 episodes and 100 mg in 6 episodes. The overall 30-day mortality rate was 25%. Univariate analysis showed that mortality was significantly associated (p < 0.01) with mean APACHE II and SOFA scores and the presence of immunosuppression, but not with the tigecycline hydrochloride dose [3].Clinical indications: Acinetobacter infection; Bacterial infection; Bacterial pneumonia; Bacterial skin infection; Bacteroides fragilis infection; Bacteroides infection; Citrobacter infection; Clostridiaceae infection; Clostridium difficile infection; Clostridium infection; Enterobacter infectionFDA Approved Date: June 17, 2005 Toxicity: nausea; vomiting; diarrhea; local IV-site reaction; infection; fever; headache
Santonin is an active principle of the plant Artemisia cina, which is formely used to treat worms[1].
2,7-Dimethoxy-6-(1-acetoxyethyl)juglone is a naphthoquinone derivative found in the fungus Kirschsteiniothelia species[1].
Vocacapsaicin (CA-008), a prodrug of Capsaicin, is a first-in-class non-opioid TRPV1 agonist. Vocacapsaicin can provide meaningful and long-lasting pain relief[1].
27-Hydroxy cholesterol-d6 is deuterium labeled 27-Hydroxy cholesterol.
Rubiadin is a dihydroxy anthraquinone isolated from Rubia cordifolia. Rubiadin has a potent antixidant activity[1].
Dymanthine is an anthelminthic. Dymanthine has the potential for the research of multiple intestinal helmintic infestations[1][2].
Enoxastrobin (Enestroburin) is an anti-fungal agent. Enoxastrobin is active against P. oryzae and B. cinerea[1].
Anisatin, a pure toxic substance isolated from the seeds of a Japanese plant (Illicium anisatum) acts as a picrotoxin-like, non-competitive GABA antagonist. Anisatin suppresses GABA-induced currents in a concentration-dependent manner with an EC50 of ~1.10 μM[1].
N-(((9H-Fluoren-9-yl)methoxy)carbonyl)-N-methyl-L-threonine is a threonine derivative[1].
Delta-hemolysin is a biological active peptide. (Delta -Lysin is a 26-residue hemolytic peptide secreted by Staphylococcus aureus, it is a delta-toxin. It is produced by most of the strains of S. aureus. This toxin is lytic to many kinds of cells by solubilization of their membranes.)
Guignardone K is a meroterpene compound isolated from solid cultures of the endophytic fungus Guignardia sp.. Guignardone K has antifungal activity[1].
Izilendustat is a potent inhibitor of prolyl hydroxylase which can stabilize hypoxia inducible factor- 1 alpha (HIF- lα) and hypoxia inducible factor-2 (HIF-2). Izilendustat has the potential for researching diseases that relate to the body’s inmmune response like colitis and other inflammatory bowel diseases (extracted from patent WO2011057115A1 and WO2011057121A1)[1][1].
H-Pro-Thr-Glu-Phe-p-nitro-Phe-Arg-Leu-OH is a water-soluble polypeptide that can serve as a substrate for cathepsin D, pepsin and pepsinogen. H-Pro-Thr-Glu-Phe-p-nitro-Phe-Arg-Leu-OH has potential applications in biochemical analysis[1][2].
4-((4-((4-Aminophenyl)sulfonyl)phenyl)amino)-4-oxobutanoic acid is a sulfonamide antiinfective agent[1].
[D-Trp8]-γ-MSH is a potent and selective agonist of melanocortin 3 (MC3) receptor, with IC50s of 6.7 nM, 600 nM and 340 nM for hMC3, hMC4 and hMC5, respectively in CHO cells. [D-Trp8]-γ-MSH could provide protection against multiple inflammatory disorders such as rheumatoid arthritis and colitis[1][2].
Biotin-PEG3-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
m-PEG3-SH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Sulfadiazine sodium belongs to the class of sulfonamide antibiotics that are used for veterinary purposes worldwide, mainly in pig production. Sulfadiazine sodium is also used for toxoplasmosis[1][2].
Lercanidipine-13C,d3-1 (hydrochloride) is deuterium labeled Lercanidipine (hydrochloride). Lercanidipine hydrochloride is a lipophilic third-generation dihydropyridine-calcium channel blocker (DHP-CCB). Lercanidipine hydrochloride has long lasting antihypertensive action and reno-protective effect[1][2][3].
5-HT2A&5-HT2C agonist-1 (Example 2) is a 5-HT2A & 5-HT2C agonist, with IC50s of 196 nM and 0.9 nM respectively. 5-HT2A&5-HT2C agonist-1 can be used for research of depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headache, PTSD, seizure disorders and other CNS disorders[1].