PXYC2 is a ribosomal protein S1 (RpsA) antagonist with Kds of 6.35 and 5.11 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of Mycobacterium Tuberculosis (Mtb)[1].
GAK inhibitor 49 is a potent, selective, ATP-competitive inhibitor of cyclin G-associated kinase (GAK, cell IC50=56 nM) with favourable NAK family selectivity (AAK1, STK16, BMP2K); shows binding to only GAK and RIPK2 in an unbiased MIB/MS experiment in cell lysate.
Lactucin is an anti-inflammatory agent. Lactucin induces cancer cell apoptosis. Lactucin also shows analgesic, anticancer and antimalarial activities[1][2][3][4].
Dianemycin (Nanchangmycin free base), produced by Streptomyces nanchangensis NS3226, inhibits gram-positive bacteria[1]. Dianemycin is a broad spectrum antiviral active against Zika virus[2].
2,2'-Bipyridine is the unique molecular scaffold of the bioactive natural products represented by caerulomycins (CAEs) and collismycins (COLs). 2,2'-Bipyridine is extensively used as the core structure of many chelating ligands by acting as a bridge in the arrangement of the catalytic center[1].
20-O-Demethyl-AP3 is a minor metabolite of Ansamitocin P-3. Ansamitocin P-3, a microtubule inhibitor, is a macrocyclic antitumor antibiotic[1].
4-Decanol is an antimutagenic compound, that can be isolated from mustard leaves. 4-Decanol inhibits mutagenic activities of $AFB_1$ and MNNG in Salmonella typhimurium TA100[1][2].
Norfunalenone exhibits weak cytotoxic activity in mouse myeloma NS-1 cell line (ATCC TIB-18) with an IC50 of 70 μM. Norfunalenone also exhibits weak antibacterial activity against B. subtilis (MIC=100 μg/mL; IC50=265 μM)[1].
Spinosyn D is one of the major components of Spinosad (HY-138800). Spinosad is a natural pesticide that shows biological activity against a range of insects including Lepidoptera[1].
JNJ 2408068 is a potent RSV (respiratory syncytial virus) inhibitor. JNJ 2408068 significantly inhibits replication of RSV A and B subtypes in the lungs of cotton rats without any evidence of toxicity. The minimum protective dose of JNJ 2408068 appears to be approximately 0.39 mg/kg[1].
Influenza Matrix Protein (61-72) is a peptide fragment derived from matrix protein of influenza viruses, corresponds to amino acids 61-72. Influenza Matrix Protein (61-72) is a specific epitope which can induce CD4+ T-cell response[1].
EP3 is an antimicrobial peptide. EP3 has antibacterial and antifungal activities. EP3 inhibits E. gallinarum, P. pyocyanea, A. baumanii, K. terrigena with a MIC value of 12.85 μg/mL. EP3 also shows antitumor activity against cancer cells, and induces cell apoptosis[1].
SPR206 acetate is a polymyxin analog with antibiotic activity against Gram-negative pathogens, including multidrug-resistant (MDR) variants. SPR206 acetate has an anti-bacterial infection effect by interacting with the bacterium’s outer membrane. The MIC values of SPR206 acetate against Pseudomonas aeruginosa Pa14 and Acinetobacter baumannii NCTC13301 are both 0.125 mg/L[1][2].
Carbadox is a quinoxaline-di-N-oxide antibiotic compound which is widely fed to nursery-age pigs to control enteric diseases and improve feed efficiency.
Yadanzioside I is a potent anti-tobacco mosaic virus (TMV) quassinoid with an IC50 of 4.22 μM[1].
DEPN-8 is a WNV protease substrate. DEPN-8 is used for dengue virus protease inhibitor development[1].
BPH-1358 free base (NSC50460 free base) is a potent human farnesyl diphosphate synthase (FPPS) and undecaprenyl diphosphate synthase (UPPS) inhibitor with IC50s of 1.8 μM and 110 nM, respectively, and is active against S. aureus in vitro (MIC ~250 ng/mL)[1][2].
HCV-IN-37 (Compound 3d) is a potent inhibitor of HCV. HCV-IN-37 is orally available and long-lasting in rat plasma after oral administration to rats by a single dose of 15 mg/kg. The high potency of active derivative HCV-IN-37 is primarily driven by the inhibitory effect on the virus entry stage[1].
Quorum Sensing-IN-2 (compound 23e) is a quorum sensing inhibitor, which can reduce the pathogenicity of bacteria without affecting bacterial growth. Quorum Sensing-IN-2 inhibits bacterial infections with little hemolytic activity. Quorum Sensing-IN-2 shows synergistic effect with Ciprofloxacin (HY-B0356) in the bacteremia model infected with P. aeruginosa PAO1[1].
Ciclopirox (Penlac) is a synthetic antifungal agent.Target: AntifungalCiclopirox is a synthetic antifungal agent for topical dermatologic treatment of superficial mycoses. It is most useful against Tinea versicolor. The mechanism of action of ciclopirox is poorly understood [1]. However, loss of function of certain catalase and peroxidase enzymes has been implicated as the mechanism of action, as well as various other components of cellular metabolism. In a study conducted to further elucidate ciclopirox's mechanism, several Saccharomyces cerevisiae mutants were screened and tested. Results from interpretation of the effects of both the drug treatment and mutation suggested that ciclopirox may exert its effect by disrupting DNA repair, cell division signals and structures (mitotic spindles) as well as some elements of intracellular transport [2]. It acts by inhibiting the membrane transfer system by interrupting the Na+ K+ ATPase [1]. It is currently being investigated as an alternative treatment to ketoconazole for seborrhoeic dermatitis as it suppresses growth of the yeast Malassezia furfur. Initial results show similar efficacy to ketoconazole with a relative increase in subjective symptom relief due to its inherent anti-inflammatory properties [3].
Atevirdine is a potent non-nucleoside HIV-1 reverse transcriptase inhibitor. Atevirdine inhibits non-nucleoside reverse transcriptase that leads to viral multiplication[1].
Alalevonadifloxacin HCl is a novel l-alanine ester prodrug of levonadifloxacin.
PNU288034 is a potent oxazolidinone antibiotic.
SARS-CoV-2 nsp14-IN-3 (4975) is an inhibitor of the SARS-CoV-2 Nsp14 N7-Methyltransferase (IC50: 3.5 μM)[1].
Lobetyol is a natural compound that can be isolated from Lobelia chinensis. Lobetyol induces apoptosis and cell cycle arrest in MKN45 cells. Lobetyol shows anti-virus, anti-inflammation and anti-tumor activity[1][2].
Diethylamine NONOate (DEA NONOate, diethylammonium salt) is a nitric oxide donor. Diethylamine NONOate is a potent antimicrobial agent, which can inhibit Escherichia coli growth. Diethylamine NONOate also can enhance preservation of the donor rat heart[1][2].
PknB-IN-2 (Compound 10) is a Mycobacterium tuberculosis protein kinase B (PknB) inhibitor with an IC50 of 12.1 μM[1].
L-Alanosine (NSC-153353), an antibiotic from Streptomyces alanosinicus, has antineoplastic activity. L-Alanosine (NSC-153353) inhibits adenylosuccinate synthetase, which converts inosine monophospate (IMP) into adenylosuccinate. L-Alanosine (NSC-153353) blocks the common de novo purine biosynthesis pathway and, thereby, inhibits tumor cells with MTAP deficiency[1][2][3].
GS-9822 is a potent, non-catalytic site HIV integrase inhibitor with wild type EC50 of 3 nM.
Halofantrine hydrochloride (SKF-102886) is a blocker of delayed rectifier potassium current via the inhibition of human-ether-a-go-go-related gene (HERG) channel and a potent antimalarial compound[1][2].