Boc-AAG-pNA is a glycine endopeptidase substrate. Boc-AAG-pNA can be used to test the amidase activity glycine endopeptidase[1].
DL-Methionine-d1 is the deuterium labeled DL-Methionine. DL-Methionine is an essential amino acid containing sulfur with oxidative stress defense effects. DL-Methionine can be used for animal natural feed. DL-Methionine also kills H. rostochiensis on potato plants[1][2][3].
Naftifine-d3 hydrochloride is the deuterium labeled Naftifine hydrochloride. Naftifine hydrochloride is an antibiotic. Naftifine hydrochloride has antifungal activity against dermatophytes, aspergilli, Sporothrix schenckii, and yeasts of the genus Candida. Naftifine hydrochloride can be used for the research of superficial dermatomycoses inhibition[1].
Ledol ((+)-Ledol) is an antifungal agent that can be isolated from the essential oil fractions of Rhododendron tomentosum. Ledol is also the expectorant and antitussive agent, which is simultaneously responsible for adverse reactions such as dizziness, nausea and vomiting[1].
M56-S2 iodide is a SARS-CoV-2 Mpro inhibitor (IC50=4.0 μM). M56-S2 iodide showed good oral bioavailability and low toxicity in ADMET prediction. M56-S2 iodide has good drug potential and can be used in antiviral (such as SARS-CoV-2) research[1].
Sulfamethazine is a sulfonamide antibacterial.Target: AntibacterialSulfamethazine is an antibiotic used to treat bronchitis, prostatitis and urinary tract infections. Sulfamethazine blocks the synthesis of dihydrofolic acid by inhibiting dihydropteroate synthase. In addition, sulfamethazine is a structural analog and competitive antagonist of para-aminobenzoic acid (PABA) and can inhibit normal bacterial utilization of PABA for the synthesis of folic acid, which is an important metabolite in DNA synthesis [1, 2].
Sulfathiazole D4 is a deuterium labeled Sulfathiazole. Sulfathiazole, an organosulfur compound, is used as a short-acting sulfonamide antibiotic[1].
(R)-4-Methoxydalbergione is a urease inhibitor with IC50s of 59.72 and 67.33 μM for Bacillus pasteurii urease and Jack bean urease. (R)-4-Methoxydalbergione also has antiplasmodial activity. (R)-4-Methoxydalbergione can be isolated from Ranunculus repens[1][2].
SC75741 is a broad and efficient NF-κB inhibitor with an IC50 of 200 nM for p65[1]. SC75741 blocks influenza viruses (IV) replication in non-toxic concentrations. SC75741 impairs DNA binding of the NF-κB subunit p65, resulting in reduced expression of cytokines, chemokines, and pro-apoptotic factors. SC75741 subsequently inhibits caspase activation and blocks caspase-mediated nuclear export of viral ribonucleoproteins[2].
WM382 is an orally active and potent dual plasmepsin IX/X (PMIX/X) inhibitor with IC50 values of 1.4 nM and 0.03 nM, respectively. WM382 has robust in vivo efficacy at multiple stages of the malaria parasite life cycle and an excellent resistance profile[1][2][3].
Nystatin A3, produced by Streptomyces noursei, a biologically active component of nystatin complex. Antibiotic activity[1]
Emetine dihydrochloride hydrate is an anti-protozoal drug previously used for intestinal and tissue amoebiasis.
Dihydroactinidiolide, existing in plant leaves and fruits, is a potent plant growth inhibitor, a regulator of gene expression and is responsible for photo acclimation in Arabidopsis. Dihydroactinidiolide has antioxidant activity, antibacterial activity, anticancer activity and neuroprotective effect[1].
NBD-557 is a potentially HIV-1 inhibitor.IC50 Value: Target: HIVNBD-557, is small molecule organic compounds with drug-like properties. It showed potent cell fusion and virus-cell fusion inhibitory activity at low micromolar levels. A systematic study showed that NBD-557 target viral entry by inhibiting the binding of HIV-1 envelope glycoprotein gp120 to the cellular receptor CD4 but did not inhibit reverse transcriptase, integrase, or protease, indicating that they do not target the later stages of the HIV-1 life cycle to inhibit HIV-1 infection. NBD-557 potent inhibitors of both X4 and R5 viruses tested in CXCR4 and CCR5 expressing cell lines, respectively, indicating that its anti-HIV-1 activity is not dependent on the coreceptor tropism of the virus. A surface plasmon resonance study, which measures binding affinity, clearly demonstrated that NBD-557 bind to unliganded HIV-1 gp120 but not to the cellular receptor CD4. NBD-557 was active against HIV-1 laboratory-adapted strains including an AZT-resistant strain and HIV-1 primary isolates, indicating that NBD-557 can potentially be further modified to become potent HIV-1 entry inhibitors.
Antitrypanosomal agent 8 (compound 3b) has potent antitrypanosomal activity against Trypanosoma brucei with an IC50 value of 0.79 μM and exhibits certain cytotoxicity in L6 cells (IC50=80.95 μM)[1].
Bifonazole is an imidazole antifungal drug.Target: AntifungalBifonazole, a new broad-spectrum antimycotic, interferes with sterol biosynthesis. In dermatophytes bifonazole additionally inhibits directly HMG-CoA-reductase. bifonazole possesses a sequential mode of action, namely inhibition of cytochrome P450-dependent C14-demethylation of sterols and direct inhibition of HMG-CoA-reductase. In vitro bifonazole shows a strongly pH-dependent efficacy. The uptake kinetics of bifonazole have been measured with different pathogens [1]. Bifonazole additionally leads to a generally decreased rate of sterol biosynthesis as compared to clotrimazole, due to a direct inhibition of microsomal HMG-CoA-reductase. The additional fungicidal effects of bifonazole are considered to originate from a sequential action by inhibition of HMG-CoA-reductase and of cytochrome P450 [2]. bifonazole were affected by choice of medium with Kimmig's agar generally giving the lowest MIC's. Bifonazole MICs were shown to vary with pH (maximal activity at pH 6 . 5) with selected yeasts when tested on Kimmig's agar [3].
Ecabet sodium (TA-2711) is currently applied to some clinical gastrointestinal disease by inhibiting the ROS production and improving Helicobacter pylori eradication[1]. Ecabet sodium reduces apoptosis[2]
Antibacterial agent 116 is a benzophenone-containing salicylanilide compound. Antibacterial agent 116 has potent antibacterial activity by inhibiting the peptidoglycan formation. Antibacterial agent 116 is used as a photoaffinity probe to label Acinetobacter baumannii penicillin-binding protein (PBP1b), block the propagation pathway to disrupt the growth of peptidoglycan chain[1].
Bacitracin Zinc is a dephosphorylation of the C55-isoprenyl pyrophosphate interference for inhibition of cleavage of Tyr from Met-enkephalin with IC50 of 10 μM.Target: AntibacterialBacitracin is a mixture of related cyclic polypeptides produced by organisms of the licheniformis group of Bacillus subtilis var Tracy. Its unique name derives from the fact that the bacillus producing it was first isolated in 1943 from a knee scrape from a girl named Margaret Tracy. As a toxic and difficult-to-use antibiotic, bacitracin doesn't work well orally. However, it is very effective topically. Bacitracin is synthesised via the so-called nonribosomal peptide synthetases (NRPSs), which means that ribosomes are not involved in its synthesis [1, 2].
GS-441524 could strongly inhibits feline infectious peritonitis virus (FIPV), with an EC50 of 0.78 μM.
Cefilavancin (TD-1792) is a potent multivalent glycopeptide-cephalosporin heterodimer antibiotic with effective activity against Gram-positive bacteria. Cefilavancin has been used to research skin infections[1][2][3].
Enrofloxacin is an effective antibiotic with an MIC90 of 0.312 μg/mL for Mycoplasma bovis.
HSV-gB2 (498-505) is an immunodominant epitope from herpes simplex virus (HSV) glycoprotein B residues 498-505, acts as H-2Kb-restricted and HSV-1/2-cross-reactive cytotoxic T-lymphocyte (CTL) recognition epitope[1].
Cloxacillin sodium monohydrate is a semi-synthetic antibiotic that is a chlorinated derivative of oxacillin.Target: AntibacterialCloxacillin sodium (Cloxacap) is a sodium salt of cloxacillin that is a penicillinase-resistant, acid resistant, semi-synthetic penicillin. Cloxacillin sodium exerts a bactericidal action against susceptible microorganisms during the stage of active multiplication. Cloxacillin sodium acts through the inhibition of biosynthesis of cell wall mucopeptides. Cloxacillin sodium is readily absorbed following i.m. administration and rapidly reaches therapeutically effective blood levels. Serum levels are approximately proportional to dosage. Peak plasma concentrations of 15 ug/ml have been observed 30 minutes after an i.m. injection of cloxacillin (Cloxapen, Cloxacap and Orbenin) 500 mg; plasma concentrations may be doubled by administration of a doubled dose. At the end of a 3-hour i.v. infusion of cloxacillin (Cloxapen, Cloxacap and Orbenin) 250 mg given to normal subjects, its plasma concentrations were 15 ug/ml. After 2 hours, plasma concentrations were 0.6 ug/ml [1].
Temephos-d12 is the deuterium labeled Temephos[1]. Temefos is an organophosphate larvicide, used to treat water infested with disease-carrying insects including mosquitoes, midges, and black fly larvae. Temefos affects the central nervous system through inhibition of cholinesterase, results in death before reaching the adult stage[2][3].
β-Lactamase-IN-6 is a β-Lactamase inhibitor that shows high antibacetrial activity.
Antitubercular agent-31 (Compound 2) is an antitubercular agent with an MIC of 0.03 μM against M. tuberculosis H37Rv. Antitubercular agent-31 also inhibits DprE1 with an IC50 of 1.1 μM[1].
5'-O-DMT-N4-Bz-2'-F-dC is a nucleoside with protective and modification effects.
Vibunazole is a new antifungal azole.
Kuwanon G is a flavonoid isolated from Morus alba, acts as a bombesin receptor antagonist, with potential antimicrobial activity[1][2].