Prostratin, a natural terpenoid compound, is a PKC activator, with a Ki of 12.5 nM and shows inhibitory effect on HIV-1.
HCV Core Protein (59-68) is a peptide containing residues 59-68 of the HCV core protein[1].
LED209 is a potent small molecule inhibitor of bacterial receptor QseC, is a potent prodrug that is highly selective for QseC. Target: AntibacterialLED209 has desirable pharmacokinetics and does not present toxicity in vitro and in rodents. This is a unique antivirulence approach, with a proven broad-spectrum activity against multiple Gram-negative pathogens that cause mammalian infections.The LED209 QseC inhibitor has a unique mode of action by acting as a prodrug scaffold to deliver a warhead that allosterically modifies QseC, impeding virulence in several Gram-negative pathogens.[1] LED209 is QseC sensor kinase inhibitor , as a potential lead compound to combat infections with Legionella or Mycobacterium spp. [2] LED209 inhibits the binding of signals to QseC, preventing its autophosphorylation and consequently inhibiting QseC-mediated activation of virulence gene expression. LED209 inhibits EHEC virulence traits in vitro. LED209 markedly inhibits the virulence of several pathogens in animals. Inhibition of signaling offers a strategy for the development of broad-spectrum antimicrobial drugs. [3]
Methicillin is a narrow-spectrum β-lactam antibiotic, acts by inhibiting penicillin-binding proteins (PBPs). Methicillin is active against Staphylococcus aureus and Staphylococcus epidermidis that are resistant to other penicillins.Methicillin can be used for the research of skin infections, osteomyelitis, and endocarditis[1].
Sulfamonomethoxine-d3-1 is the deuterium labeled Sulfamonomethoxine[1]. Sulfamonomethoxine is a long acting sulfonamide antibacterial agent, used in blood kinetic studies,and blocks the synthesis of folic acid by inhibiting synthetase of dihydropteroate[2].
HIV-1 inhibitor-27 (compound 5) is a potent HIV-1 inhibitor with IC50s of 16 μM, 0.5 μM and 0.39 μM for HIV-1 YU2, NL4-3 and 89.6 strain, respectively. HIV-1 inhibitor-27 has low cytotoxicity with a CC50 of 128 μM in TZM-bl cells. HIV-1 inhibitor-27 can be used for researching AIDS[1].
APJ receptor agonist 1, a biphenyl acid derivative, is a potent APJ receptor (APJ-R) agonist (EC50s 0.093 and 0.12 nM for human and rat APJ-R, respectively). APJ receptor agonist 1 displays in vitro potency to apelin-13, the endogenous peptidic ligand for the APJ receptor. APJ receptor agonist 1 has the potential for the research of heart failure[1].
CysHHC10 is a synthetic antimicrobial peptide (AMP), and exhibits strong anti-microbial properties against both Gram-positive and Gram-negative bacteria. The MIC values of CysHHC10 against E. coli, P. aeruginosa, S. aureus and S. epidermidis are 10.1 mM, 20.2 mM, 2.5 mM and 1.3 mM, respectively[1].
HPi1 is a potent, selective and orally active antimicrobial against Helicobacter pylori with an IC50 of 0.24 μM and an MIC of 0.08-0.16 μg/mL. HPi1 is inactive against other bacteria, including the gut commensals Lactobacillus casei, Lactobacillus reuteri, and Bifidobacterium longum[1].
Lysicamine, a natural compound, possesses antibacterial, anticancer and anti-inflammation activity[1].
Thiomandelic acid is a broad spectrum inhibitor of Zinc -lactamases[1].
p-Anisic acid-d4 is the deuterium labeled p-Anisic acid[1]. p-Anisic acid (4-Methoxybenzoic acid) is one of the isomers of anisic acid, with anti-bacterial and antiseptic properties[2].
Sulfathiazole Sodium is an organosulfur compound that has been used as a short-acting sulfa drug.Target: AntibacterialSulfathiazole (20 μg/L) starts to be degraded between day 31 and day 38 in one of the two batch reactors containing different wastewater matrices. Sulfathiazole is degraded at a substantially faster rate than sulfamethoxazole or sulfamethazine in the nitrification process (S3) [1]. Recovery from spiked manure slurry samples is 64% for Sulfathiazole at pH 9. Sulfathiazole has acidity constant of pKa of 7.1and retention times (tR) of 7.8. S/N values for Sulfathiazole are above 100 at the 1 mg/kg level [2]. Sulfathiazole sorption to inorganic sorbents exhibits pronounced pH dependence consistent with sorbate speciation and sorbent charge properties. Sulfathiazole cations are most important for sorption to clay minerals, followed by neutral species [3].
Trilobatin, a natural sweetener derived from Lithocarpus polystachyus Rehd[1], Trilobatin is an HIV-1 entry inhibitor targeting the HIV-1 Gp41 envelope[2]. Neuroprotective effects[1]. Trilobatin is also a SGLT1/2 inhibitor that selectively induces the proliferation of human hepatoblastoma cells[3].
NITD-916 is a novel, direct inhibitor of the mycobacterial enoyl-reductase InhA with IC50 of 0.57 uM, exhibits MIC50 of 50 nM against Mtb; shows MIC of 0.04 to 0.16 μM against MDR-Mtb strains, binds specifically to InhA in an NADH-dependent manner and blocks the enoyl substrate-binding pocket; shows in vivo efficacy in acute and established mouse models of Mycobacterium tuberculosis infection.
Antibacterial agent 108 (Compound 1h) is a potent antibacterial agent with a MIC of both 3 μM against MRSA and antibiotic resistance strains[1].
Pyrantel pamoate is a deworming agent in the treatment of hookworms (all species) and roundworms in domesticated animal; acts as a depolarizing neuromuscular blocking agent.
Bacampicillin hydrochloride is a penicillin antibiotic, is a prodrug of ampicillin with improved oral bioavailability.
Meclocycline Sulfosalicylate Salt is a tetracycline antibiotic with broad-spectrum antibacterial activities, preventing skin bacterial infections such as acne vulgaris[1].
Antituberculosis agent-6 (compound 9g) is a potent antimycobacterial agent. Antituberculosis agent-6 shows significant activity against M. tuberculosis, with a MIC of 3.49 μM. Antituberculosis agent-6 also shows good antifungal activity against A. niger, with a MIC of 62.50 μM. Antituberculosis agent-6 shows high GI absorption[1].
Methyl 3-hydroxy-4,5-dimethoxybenzoate is a gallic acid derivant isolated from myricaria Laxiflora. Methyl 3-hydroxy-4,5-dimethoxybenzoate shows obvious antimicrobial activities. Methyl 3-hydroxy-4,5-dimethoxybenzoate shows fairly active for oxidation resistance in the presence of H2O2[1].
ME1111 is an antifungal agent that is active against dermatophytes. ME1111 is an inhibitor of the succinate dehydrogenase of Trichophyton species. ME1111 has an excellent ability to penetrate human nails and is used for onychomycosis research[1][2].
Balhimycin is a glycopeptide antibiotic, found from the fermentation broth of a Amycolatopsis sp. Balhimycin shows anti-bacterial activity against staphylococci and anaerobes[1].
Chlorhexidine is an antibacterial used as an antiseptic and for other applications.Target: AntibacterialChlorhexidine belongs to a group of medicines called antiseptic antibacterial agents. It is used to clean the skin after an injury, before surgery, or before an injection. Chlorhexidine is also used to clean the hands before a procedure. It works by killing or preventing the growth of bacteria on the skin.
HHV-2 Envelope Glycoprotein G (552-574) is an immunodominant region of glycoprotein G (gG-2) reactive with all herpes simplex (HSV-2) sera[1].
Mt KARI-IN-2 (compound 5b) is a potent Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI) inhibitor with a Ki value of 2.02 μM. Mt KARI-IN-2 has inhibitory activity against Mtb H37Rv (MIC = 0.78 μM) and low cytotoxicity (HEK IC50 > 86 μg/mL)[1].
Pafuramidine (DB289) is an orally bioavailable prodrug of furamidine, which has clinical activity against Pneumocystis pneumonia.IC50 Value: 4.5 nM (In vitro inhibitory activity against Trypanosoma brucei rhodesiense) [4]Target: AntiparasiticDB289 (pafuramidine maleate; 2,5-bis[4-(N-methoxyamidino)phenyl]furan monomaleate) is a prodrug of DB75 (furamidine dihydrochloride; 2,5-bis(4-guanylphenyl)furan dihydrochloride), an aromatic dication related to pentamidine that has demonstrated good efficacy against African trypanosomiasis, Pneumocystis carinii pneumonia, and malaria, but lacks adequate oral availability. in vitro: The results of this investigation suggest that DB75 inhibits mitochondrial function. Yeast cells relying upon mitochondrial metabolism for energy production are especially sensitive to DB75 [1].in vivo: Clearance of DB289 approximated the liver plasma flow and its large volume of distribution was consistent with extensive tissue binding. Plasma protein binding of DB289 was 97 to 99% in four animal species and humans, but that of DB75 was noticeably less and more species- and concentration-dependent [2]. Despite excellent oral activity against early-stage sleeping sickness, oral administration of DB289 exhibited limited efficacy in mouse models of late-stage disease [3].Clinical trial: DB289, a novel orally active prodrug of DB75, is undergoing phase IIb clinical trials for early-stage human African trypanosomiasis, Pneumocystis jiroveci carinii pneumonia, and malaria [1].
Ledipasvir diacetone is the active pharmaceutical ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
Dimethomorph-d8 is the deuterium labeled Dimethomorph[1]. Dimethomorph is a fungicide belongs to the fungicide group of sterol biosynthesis inhibitor. Dimethomorph can inhibit fungal cell wall formation. Dimethomorph also inhibits androgen receptor (AR) activity in MDA-kb2 cells with an IC20 of 0.263 μM[2][3][4].