Dimethomorph is a morpholine fungicide that inhibits fungal cell wall formation. Dimethomorph inhibits mycelial growth of the oomycete fungi P. citrophthora, P. parasitica, P. capsici, and P. infestans (EC50s=0.14 µg/mL, 0.38 µg/mL, <0.1 µg/mL, and 0.16-0.3 µg/mL, respectively) but is less active against the green algae species C. vulgaris or S. obliquus in vitro (EC50s=47.46 µg/mL and 44.87 µg/mL, respectively). Dimethomorph inhibits androgen receptor (AR) activity in a reporter assay in MDA-kb2 human breast cancer cells but not in a yeast antiandrogen screen (IC20s=0.263 µM and 38.5 µM, respectively).
Nintedanib-d8 is deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
(S)-3-((tert-Butoxycarbonyl)amino)-3-(4-methoxyphenyl)propanoic acid is a phenylalanine derivative[1].
CDK9-IN-18 is a potent CDK9 inhibitor. CDK9-IN-18 blocks the phosphorylation function of kinase CDK9. CDK9-IN-18 exhibits both good anticancer activity and low cellular activity. CDK9-IN-18 induces apoptosis.
CYT-1010 is a mu-opioid receptor agonist extracted from patent WO2013173730A2, with EC50s of 13.1 nM and 0.0053 nM on beta-arrestin recruitment and inhibition of cAMP production, respectively[1].
Enoxaparin (PK 10169), a low-molecular-weight heparin (LMWH) derivative. Enoxaparin exerts anticoagulant activity through antithrombin III, an endogenous inhibitor of factor Xa and thrombin IIa. Enoxaparin protect the rat hippocampus against TBI (traumatic brain injury) via antioxidant and anti-inflammatory properties. Enoxaparin can be used for the research of deep vein thrombosis (DVT), pulmonary embolism, TBI and COVID-19[1][2][3].
Quinclorac, an herbicide widely applied in agriculture, induces oxidative stress due to free radical generation and changes in the antioxidant defense system[1].
PD180970 is a highly potent and ATP-competitive p210Bcr-Abl kinase inhibitor, with an IC50 of 5 nM for inhibiting the autophosphorylation of p210Bcr-Abl. PD180970 also inhibits Src and KIT kinase with IC50s of 0.8 nM and 50 nM, respectively. PD180970 indcues apoptosis of K562 leukemic cells, and can be used for chronic myelogenous leukemia research[1][2][3].
AMOZ-CHPh-3-acid is hapten against furaltadone metabolite AMOZ. AMOZ-CHPh-3-acid can couple to BSA for immunogens and couple to OVA for coating antigen[1].
Propargyl-PEG5-PFP ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Olmesartan D4 is the deuterium labeled Olmesartan. Olmesartan is an angiotensin II receptor (AT1R) antagonist used to treat high blood pressure.
Cefepime Dihydrochloride Monohydrate is a broad-spectrum cephalosporin with enhanced coverage against Gram-positive and Gram-negative bacteria.Target: AntibacterialCefepime is an extended-spectrum parenteral cephalosporin antibiotic active in vitro against a broad spectrum of gram-positive and gram-negative aerobic bacteria. Cefepime dosing was 1-4 g/day (0.5-2.0 g twice daily) for adults; ceftazidime dosing was 1-6 g/day (0.5 g every 12 hours to 2.0 g every 8 hours). A limited number of cefepime-treated patients received 2 g every 8 hours. The median length of dosing for both cefepime and ceftazidime was 7 days [1]. Cefepime has a decreased propensity to induce beta-lactamases compared with other beta-lactam antibiotics. Cefepime has a pharmacokinetic disposition similar to that of other renally eliminated cephalosporins, with a half-life of approximately 2 hours. Cefepime has demonstrated clinical efficacy against a variety of infections, including urinary tract infections, pneumonia, and skin and skin structure infections. Cefepime is generally well tolerated [2].
Laccaic acid C is an potent inhibitor of RNase H with an IC50 of 8.1 μM. Laccaic acid C also inhibits viral proliferation in cell [1].
α-Melanocyte-Stimulating Hormone (MSH), amide stimulates melanocortin 1 receptor that results in the activation of adenylyl cyclase.
BJE6-106 (B106) is a potent, selective 3rd generation PKCδ inhibitor with an IC50 of 0.05 μM and targets selectivity over classical PKC isozyme PKCα (IC50=50 μM). BJE6-106 (B106) induces caspase-dependent apoptosis. BJE6-106 (B106) possesses tumor-specific effect.
Isavuconazonium sulfate (BAL8557-002), the prodrug of the active triazole Isavuconazole, is an orally active antifungal agent. Isavuconazonium sulfate is used for invasive aspergillosis and mucormycosis[1][2].
Antibacterial agent 83 (compound 17h) displays potent antibacterial activity against various vancomycin-resistant Enterococcus faecalis (VRE) and methicillin-resistant Staphylococcus aureus (MRSA). Antibacterial agent 83 can significantly reduce the biofilm formation of MRSA and exhibited promising selectivity. Antibacterial agent 83 is metabolically stable in human liver microsomes[1].
Scabioside C is a main triterpenoid saponin for total secondary saponin (TSS). TSS, from A. raddeana, exhibits the potential anti-breast cancer effect[1].
GDC-0623 is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAFV600E, EC50=7 nM).
NK-252 is a potential Nrf2 activator, which exhibits a great Nrf2-activating potential.
Methyl undecanoate is an internal standard in gas-liquid chromatogram[1].
Antibiotic A-338533, an antibiotic, can be isolated from Streptomyces strain. Antibiotic A-338533 has anti-bacterial activity against Staphylococcus aureus, Mycoplasma gallisepticum with MIC values of 2 μg/mL and ≤1.56 μg/mL, respectively[1].
(2E,4E)-8-Hydroxy-2,7-dimethyl-decadien-(2,4)-disaeure-(1,10)-dioic acid is a nature product that could be isolated form bunge auriculate flower. (2E,4E)-8-Hydroxy-2,7-dimethyl-decadien-(2,4)-disaeure-(1,10)-dioic acid has antioxidant and anti-inflammatory active[1].
3-Nitropropanoic acid is an irreversible inhibitor of succinate dehydrogenase.
RSV/IAV-IN-1 (compound 14e) is a potent and dual inhibitor of RSV/IAV. RSV/IAV-IN-1 has lesser cytotoxicity than the clinical drug, Ribavirin. RSV/IAV-IN-1 has the potential for the research of RSV and/or IAV infections[1].
N2-iso-Butyroyl-2’-O-propargylguanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7)[1].
Bamlanivimab (Anti-Human SARS-CoV-2) is the first COVID-19 monoclonal antibody (mAb) to be granted Emergency Use Authorization (EUA) in November 2020 by the U.S. Food and Drug Administration (FDA). However, Bamlanivimab is withdrawn in April 2021 following the rise of SARS-CoV-2 virus variants resistant to Bamlanivimab[1].
5-(Azidomethyl)-2’-O-(2-methoxyethyl)uridine is a thymidine analogue. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].
JAK-IN-27 (compound 1) is an orally active and potent JAKS family kinase inhibitor with IC50s of 3.0 nM (TYK2), 7.7 nM (JAK1), 629.6 nM (JAK3), respectively. JAK-IN-27 inhibits IFN-α2B-induced phosphorylation of STAT3 in Jurkat cells (IC50=23.7 nM)[1].
Antibacterial agent 160 is a potent antibacterial agents. Antibacterial agent 160 can rapidly kill bacterial and inhibits bacterial biofilm formation. Antibacterial agent 160 affects the normal function of DNA and leads cell death[1].