HDAC/HSP90-IN-3 (compound J5) is a potent and selective fungal Hsp90 and HDAC dual inhibitor, with IC50 values of 0.83 and 0.91 μM, respectively. HDAC/HSP90-IN-3 shows antifungal activity against azole resistant C. albicans. HDAC/HSP90-IN-3 can suppress important virulence factors and down-regulate drug-resistant genes ERG11 and CDR1[1].
SARS-CoV-2-IN-11 is a potent and nontoxic inhibitor of SARS-CoV-2 3CL protease (3CLpro) with an IC50 and EC50 of 0.17 and 1.45 nM, respectively. SARS-CoV-2 3C-like protease (3CLpro), an enzyme essential for viral replication, is an attractive target for therapeutic intervention. SARS-CoV-2-IN-11 may lead to the emergence of effective SARS-CoV-2-specific antivirals[1].
1-Phenylsemicarbazide is an antifungal agent. 1-Phenylsemicarbazide has the potential for preventing mold growth on industrial products[1].
Gomisin M2 ((+)-Gomisin M2) is a lignan isolated from the fruits of Schisandra rubriflora with anti-HIV activity (EC50 of 2.4 μM). Gomisin M2 exhibits anti-cancer and anti-allergic activities and has the potential for Alzheimer’s disease research[1][2].
Thymol iodide is a compound of Iodide and Thymol. Thymol iodide acts as a substitute for iodoform[1]. Thymol iodide is an iodine derivative of Thymol (a phenol derived from thyme oil), which is mostly used as mild antiseptic and fungicide[2].
Reveromycin A, a benzoquinoid antibiotic isolated from the genus Streptomyces, is a selective inhibitor of protein synthesis in eukaryotic cells. Reveromycin A inhibits bone resorption by inducing apoptosis specifically in osteoclasts. Reveromycin A has antiproliferative activity against tumor cell lines and antifungal activity[1][2].
Tebuconazole is an agricultural azole fungicide which can also inhibit CYP51 with IC50s of 0.9 and 1.3 μM for Candida albicans CYP51 (CaCYP51) and truncated Homo sapiens CYP51 (Δ60HsCYP51), respectively.
Polistes mastoparan is an antimicrobial peptide. Polistes mastoparan increases S. aureus cell K+ efflux and inhibits cell viability with EC50 of 5 μM[1].
Clindamycin is an oral protein synthesis inhibitory agent that has the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla)[1].
SARS-CoV-2 Mpro-IN-2 (compound GC-14) is a selective, low cytotoxic and non-covalent Mpro inhibitor (IC50=0.40 μM) with good anti-SARS-CoV-2 activity (EC50=1.1 μM). SARS-CoV-2 Mpro-IN-2 can be used in COVID-19 studies[1].
Sulfisoxazole (Sulfafurazole) diethanolamine is an endothelin receptor antagonist with IC50 values of 0.60 μM and 22 μM against endothelin receptor A and endothelin receptor B, respectively. Sulfisoxazole diethanolamine is a sulfonamide antibacterial with an oxazole substituent. Sulfisoxazole diethanolamine inhibits breast cancer exosome release by targeting endothelin receptor A[1][2].
FNC-TP is the intracellular active form of FNC. FNC is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV[1].
Antibacterial agent 143 (Compound 5a) is an antibacterial agent with MICs of 25, 25, 50 and 50 μg/mL against B. subtilis ATCC6633, . aureus ATCC6538, P. aeruginosa ATCC13525 and E. coli ATCC35218, respectively[1].
NIM811 (SDZ NIM811) is a potent mitochondrial permeability transition inhibitor. Sequence: Cyclo[{Aaa}-{Abu}-{Sar}-Ile-Val-Leu-Ala-{D-Ala}-Leu-Leu-Val].
Kakuol is a natural compound isolated from the rhizomes of Asarum sieboldii. Antifungal activity[1].
Nimorazole (K-1900) is a nitroimidazole anti-infective.
BRD-6929 (Cpd-60) is a brain-penetrant, selective inhibitor of HDAC1 and HDAC2 (IC50= 1 and 8 nM), extracted from patent US2018360927[1]. BRD-6929 (Cpd-60) shows high-affinity to HDAC1 and HDAC2 with Ki of 0.2 and 1.5 nM, respectively[2]. BRD-6929 (TPB) potentiates the efficacy of gnidimacrin (a PKC Agonist) against latent HIV-1[3].
Murrayanol is a natural carbazole alkaloid with a variety of biological activities. Murrayanol shows anti-inflammatory, topoisomerase I and topoisomerase II (Topoisomerase) inhibition activities. Murrayanol also as a mosquitocidal and antimicrobial[1].
Chrysomycin B is an antibiotic isolated from a strain of Streptomyces. Chrysomycin B causes DNA damage in the human lung adenocarcinoma A549 cell line and inhibits topoisomerase II. Chrysomycin B suppresses the growth of transplantable tumors in mice.
Benznidazol (Ro 07-1051) is an antiparasitic medication, with an IC50 of 20.35 μM for Colombian T. cruzi strains, and has been used in the treatment of Chagas disease[1][2].
Moxifloxacin-d3 is the deuterium labeled Moxifloxacin. Moxifloxacin is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia.
Trifloxystrobin (CGA 279202) is a fungicide, with EC50s of 23.0 μg/L and 1.7 μg/L for Daphnia magna neonate and embryos, respectively, after treatment for 48 h[1].
Cephalexin-d5 is deuterium labeled Cephalexin. Cephalexin (Cefalexin; Cephacillin) is a potent, orally active and the first-generation cephalosporin antibiotic. Cephalexin kills gram-positive and some gram-negative bacteria by disrupting the growth of the bacterial cell wall. Cephalexin monohydrate is used for the research of pneumonia, strep throat, and bacterial endocarditis, et al[1].
4-O-Methylepisappanol (compound 9) is nature product that could be isolated from heartwood of Caesalpinia sappan. 4-O-Methylepisappanol is a potent neuraminidase inhibitor on the surface of influenza viruses with IC50 values of 42.8, 63.2, and 63.2 µM for A/Chicken/Korea/MS96/96 [H9N2], A/PR/8/34 [H1N1], and A/Hong Kong/8/68 [H3N2], respectively[1].
Antibacterial agent 18 is a multi-arm AIE molecule extracted from patent CN110123801A, compound 23. Antibacterial agent 18 can be used for resisting Gram-positive and Gram-negative bacteria. Antibacterial agent 18 can be conjugated in the cell wall of rigid arm configuration insertion bacterium, and block cell wall turns sugar and turns peptide process, to inhibit or kill bacterium[1].
MK-2048 is a potent inhibitor of integrase and INR263K with IC50 of 2.6 nM and 1.5 nM, respectively.IC50 Value: 2.6 nM for HIV IntegraseTarget: HIV IntegraseMK-2048 is a second generation integrase inhibitor, intended to be used against HIV infection. MK-2048 inhibits subtype B and subtype C integrase activities. MK-2048 inhibits R263K mutants slightly more effectively than G118R mutants. MK-2048 inhibits S217H intasome and, by contrast, MK-2048 remains fully active against the N224H intasome. MK-2048 displays substantially lower dissociation rates compared with raltegravir, another integrase inhibitor. MK-2048 is active against viruses resistant to RAL and EVG. MK-2048 exposure leads to the selection of G118R as a possible novel resistance mutation after 19 weeks. MK-2048, with continued pressure, subsequently leads to an additional substitution, at position E138K, after 29 weeks, within the IN gene. Although the G118R mutation alone confers only slight resistance to MK-2048 but not to RAL or EVG, its presence arouses a dramatic reduction in viral replication capacity compared to wild-type NL4-3. E138K both partially restores viral replication capacity and also contributes to increased levels of resistance against MK-2048.
Valopicitabine (NM283) dihydrochloride is a nucleoside analog and the orally bioavailable prodrug of the potent anti-HCV agent 2'-C-methylcytidine (NM107). NM107competitively inhibits NS5B polymerase, causing chain termination[1][2].
Metham sodium (Carbathion) is a broad-spectrum soil microbial suppressant. Metham sodium controls soil-borne pests and weeds. Metham sodium inhibits weed seeds, plant-parasitic nematodes, plant pathogenic fungi and soil insects[1].
GLP-26 is a HBV capsid assembly modulators (CAM), inhibits HBV DNA replication in Hep AD38 system (IC50=3 nM), and reduces cccDNA by >90% at 1 μM.GLP-26 disrupts the encapsidation of pre-genomic RNA, causes nucleocapsid disassembly and reduces cccDNA pools[1].
Penicillin V (Phenoxymethylpenicillin) is a potent and orally active antibiotic. Penicillin V shows antibacterial activity for Streptococci, Clostridium difficile and staphylococcus aureus. Penicillin V has the potential for the research of otitis, sinusitis, pharyngitis and tonsillitis[1][2][3][4].