Infection

SARS-CoV-2 Mpro-IN-10 (27h) is a potent M^pro inhibitor with IC₅₀ value and EC₅₀ values of 10.9 nM and 43.6 nM, respectively. SARS-CoV-2 Mpro-IN-10 can be used for the research of SARS-CoV-2 virus.

SARS-CoV-2 3CLpro-IN-15 (compound a) is a beta-nitrostyrene coronavirus SARS-CoV-2 inhibitor that targets the SARS-CoV-2 3CL protease (3CLpro). SARS-CoV-2 3CLpro-IN-15 inhibits viral replication and transcription and plays a key role in the discovery of anti-COVID-19 lead compounds.

Dapivirine-d₄ (TMC120-d₄) is deuterium labeled Dapivirine. Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations.

Scolopin-2 is an antimicrobial peptide that can be isolated from centipede venoms. Scolopin-2 shows strong antimicrobial activities against a panel of Gram-positive/negative bacteria and fungi (MIC ≤ 7.5 μg/mL) . Scolopin-2 shows moderate hemolytic activity against both human and rabbit red cells. Scolopin-2 can be used for antimicrobial research.

Valproic acid (VPA) sodium (2:1) is an orally active HDAC inhibitor, with IC₅₀ in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC₅₀, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium (2:1) activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium (2:1) is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches.

Galbinic acid (α-Acetylsalazinic acid), a lichen acid, shows antibacterial activities against the Gram-positive bacteria B. cereus, B. subtilis, and S. aureus (MICs=62.5, 62.5, 250 μg/ml, respectively). Galbinic acid inhibits the Gram-negative bacterium E. coli (MIC=125 μg/ml).

Isovalerylspiramycin II is one of the core active components of the multi-component antibiotic Bitespiramycin. Isovalerylspiramycin II shows antibacterial activity and can be used for research of bacterial infection.

HIV gp120 (318-327) is a short sequence of the HIV-1 strain IIIB envelope peptide (rgpgrafvti) that corresponds to the conserved C-terminal region of the glycoprotein. HIV gp120 (318-327) is part of the HIV vaccine V3 peptide epitope, also known as the I10 peptide. However, HIV gp120 (318-327) lacks the A2 anchor residues recognized by epitope-specific CTLs but has structural features that confer promiscuous A2 binding.

DNA Gyrase-IN-1 (compound 42) is a potent and selective DNA gyrase inhibitor with an IC₅₀ value of 2.6 µM. DNA Gyrase-IN-1 has high inhibitory activity against Mycobacterium tuberculosis (Mtb) with MIC of 0.49 µM. DNA Gyrase-IN-1 can be used for researching tuberculosis.

Antibacterial agent 56 (example 22) is a antibacterial agent (extracted from patent WO2013030735A1).

7,3′-Dihydroxy-8,4′-dimethoxyisoflavone is an isoflavone Antibacterial agent. 7,3′-Dihydroxy-8,4′-dimethoxyisoflavone is isolated from the stems of S. parviflorus. 7,3′-Dihydroxy-8,4′-dimethoxyisoflavone exhibits weak antibacterial activity against Gram-positive and Gram-negative bacterial strains. 7,3′-Dihydroxy-8,4′-dimethoxyisoflavone can be used in the research of bacterial infections.

Glutoborin is an orally active GLUT1-specific proteasome inhibitor with a K_d value of 119 nM for GLUT1. Glutoborin binds to GLUT1, inhibits proteasome activity, restricts IκBα degradation, blocks NF-κB activation, and inhibits GLUT1-mediated glucose transport to elevate blood glucose levels. Glutoborin inhibits pro-inflammatory gene expression, B cell activation, autoantibody production and macrophage function, disrupts the interaction between macrophages and B cells, and alleviates systemic inflammation, neuroinflammation and blood-brain barrier damage. Glutoborin can be used in research related to cerebral malaria.

Ciprofloxacin (lactate) (Standard) is the analytical standard of Ciprofloxacin (lactate). This product is intended for research and analytical applications. Ciprofloxacin (Bay-09867) lactate is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin lactate induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin lactate has anti-proliferative activity and induces apoptosis. Ciprofloxacin lactate is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity[4].

SARS-CoV-2 Mpro-IN-9 (compound c7) is a nonpeptidic, noncovalent SARS-CoV-2 M^pro inhibitor (IC₅₀=0.085 μM), with improved physicochemical and drug metabolism and pharmacokinetics (DMPK) properties. SARS-CoV-2 Mpro-IN-9 inhibits viral replication (EC₅₀=1.10 μM) in SARS-CoV-2-infected Vero E6 cells, while exhibits low cytotoxic effects (CC₅₀>50 μM).

Viridiol, a fungal metabolite from Trichodernza viride, shows antifungal activity.

Chelerythrine hydroxide is an alkaloid, acts as a potent and selective Ca²⁺/phospholopid-dependent PKC antagonist, with an IC₅₀ of 0.7 μM. Chelerythrine hydroxide inhibits the BclXL-Bak BH3 peptide binding with IC₅₀ of 1.5 μM. Chelerythrine hydroxide triggers Apoptosis and Autophagy. Chelerythrine hydroxide has antitumor, antidiabetic and anti-inflammatory activity. Chelerythrine hydroxide shows antibacterial activities against Gram-positive bacteria, Staphylococcus aureus (SA), MRSA.

MtTMPK-IN-5 (compound 17) is a potent M. tuberculosis thymidylate kinase (MtbTMPK) inhibitor with an IC₅₀ value of 34 μM. MtTMPK-IN-5 combines favorable enzyme inhibitory activity with significant activity against M. tuberculosis (MIC = 12.5 μM). MtTMPK-IN-5 can be used for researching tuberculosis.

Neryl arabinofuranosyl-glucoside (Geranyl 1-O-α-L-arabinofuranosyl (1→6)-β-D-glucopyranoside) is a terpene-derived glycoside. Neryl arabinofuranosyl-glucoside can be present in apricot fruits, melon stems and bitter melon stems. Neryl arabinofuranosyl-glucoside is negatively correlated with the bacterial genus Pseudomonas and the fungal genus Cladosporium, and positively correlated with unclassified fungi (unclassified_k__Fungi). Neryl arabinofuranosyl-glucoside can be used for studies on perinatal hypophosphatemia.

TSO-13 is the inhibitor for the main cysteine protease of Trypanosoma cruzi Cruzipain with an IC₅₀ of 2.2 μM. TSO-13 inhibits T. cruzi in Vero cell with an IC₅₀ of 1.9 μM.

Alalevonadifloxacin (hydrochloride) (WCK-2349 (hydrochloride)) is a oraaly active anti-methicillin-resistant Staphylococcus aureus (MRSA) antibiotic.