Infection

Octaarginine acetate is a cell-penetrating peptide and proteasome inhibitor. Octaarginine acetate exhibits mixed-type inhibition against 20S proteasome chymotrypsin-like, caspase-like, and trypsin-like activities, and inhibits 26S proteasome activity with decreased efficiency. Octaarginine acetate induces ubiquitin-conjugated protein accumulation, mediates HSPG-dependent cellular internalization via macropinocytosis, enhances liposomal cargo uptake and gene delivery. Octaarginine acetate can be used for the research of cervix carcinoma, collagen antibody-induced arthritis, and bacterial infections.

BEPP hydrochloride is a double-stranded RNA-dependent protein kinase (PKR) modulator. BEPP hydrochloride enhances the phosphorylation levels of PKR and eIF2α, activates caspase-3, upregulates the pro-apoptotic protein BAX, and downregulates the anti-apoptotic protein Bcl-2. BEPP hydrochloride inhibits vaccinia virus replication and exhibits selective cytotoxicity in cells expressing PKR. BEPP hydrochloride can be used in research related to cancer and viral infections.

Bis-propargyl-PEG3 is a PEG-based PROTAC linker used in the synthesis of PROTACs. Bis-propargyl-PEG3 is used in the synthesis of zinc-dipicolylamine (ZnDPA) complexes with antiplasmodial activity . Bis-propargyl-PEG3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Dehydrocorydaline (13-Methylpalmatine) hydroxyl is an alkaloid that regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline hydroxyl elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities. Dehydrocorydaline hydroxyl shows strong anti-malarial effects (IC50=38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.

Verruculogen is a tremorgenic mycotoxin and inhibitor of the M phase of the mammalian cell cycle. Verruculogen is produced by Penicillium and Aspergillus species. Verruculogen enhances the binding of ChTX to maxi-k channels with a K_1/2 value of 170 nM. Verruculogen inhibits the amplitude of Ca²⁺-activated K⁺ currents. Verruculogen induces severe tremors in infected animals.

SRX3177 is a triple inhibitor of CDK4/6, PI3K, and BRD4, with IC₅₀s of <2.5 nM (CDK4), 3.3 nM (CDK6), 33 nM (BRD4 BD1), 89 nM (BRD4 BD2), 79 nM (PI3Kα), 83 nM (PI3Kδ), 3.18 μM (PI3Kγ) , respectively. SRX3177 blocks the interaction between the SARS-CoV-2 E protein and the BRD2/4 BD1 domain, restores E protein-attenuated NF-κB activity. SRX3177 exerts broad cytotoxic activity against cancer cells. SRX3177 can be used for the study of anti-SARS-CoV-2 and cancer.

Prothionamide is an orally active thioamide antibacterial agent. Prothionamide is a substrate of OCT1 with a K_m value of 805.8 μM. Prothionamide reacts with NAD to form a covalent adduct, with the adduct being a tight-binding inhibitor of Mycobacterium tuberculosis and Mycobacterium leprae InhA. Prothionamide can effectively inhibit the growth of Mycobacterium tuberculosis (MIC = ~0.5 µg/mL) and Mycobacterium leprae. Prothionamide is used in the research of tuberculosis and leprosy.

Rupestonic acid, a sesquiterpene, can inhibit influenza virus.

Hexahydrofarnesyl acetone (6,10,14-Trimethyl-2-pentadecanone) is a oral active sesquiterpene with oral activity, exhibiting antibacterial, anti-inflammatory, and anticancer properties, and is used in pain relief research.

Cyclomarin monomer-1 (Compound 5), a cyclomarin monomer, is a pre-dimerization precursor that can form Homo-BacPROTACs targeting the degradation of ClpC1. Cyclomarin monomer-1 binds to the Mtb ClpC1 protein with a K_D of 3.5 nM. The MIC of Cyclomarin monomer-1 against the Mtb H37Rv standard strain is 1.6 μM. Cyclomarin monomer-1 can be used as a key intermediate in the development of Homo-BacPROTACs.

Rifabutin-d₇ is the deuterium labeled Rifabutin. Rifabutin (Ansamycin) is a semisynthetic ansamycin antibiotic with potent antimycobacterial properties. Rifabutin inhibits DNA-dependent RNA polymerase.

Strictosamide is a compound that can be isolated from Nauclea officinalis. Strictosamide has various activities such as anti-inflammatory, analgesic, anti-Plasmodium, antifungal, and promoting wound healing.

Skeletal muscle-targeted peptide MSP is a 7-amino-acid (ASSLNIA) muscle-targeting peptide (MTP). Skeletal muscle-targeted peptide MSP can target the virus through a different binding ligand to the muscle. Skeletal muscle-targeted peptide MSP can be used for the research of diseases of the heart and skeletal muscles.

PAMAM Dendrimer G0.0 amine is a pore-forming channel antagonist, including anthrax toxin protective antigen 63 (PA63, IC₅₀ = 231 nM) and C. botulinum C2 toxin subunit (C2IIa, IC₅₀ = 940 nM). At concentrations of 10 and 20 µM, PAMAM Dendrimer G0.0 amine reduces C2 toxin-induced death in HeLa cells. Additionally, PAMAM Dendrimer G0.0 amine is a chelator of nickel. In complexes with polysulfone membrane-bound chitosan, PAMAM Dendrimer G0.0 amine selectively captures and stores carbon dioxide (CO2) in a gas-feed system. PAMAM Dendrimer G0.0 amine has been used in the synthesis of PAMAM Dendrimer G0.5 Carboxylate (CAS 339334-01-9) and PAMAM Dendrimer G1.0 Amine (CAS 142986-44-5). PAMAM Dendrimer G0.0 amine can be used in research related to infections, cancer, and drug delivery systems.

Cyclic ADP-ribose ammonium (cADPR ammonium) is a potent second messenger for calcium mobilization that is synthesized from NAD⁺ by an ADP-ribosyl cyclase. Cyclic ADP-ribose ammonium increases cytosolic calcium mainly by Ryanodine receptor-mediated release from endoplasmic reticulum and also by extracellular influx through the opening of TRPM2 channels.

Recombinant Streptolysin O is a cholesterol-targeting, thiol-activated pore-forming toxin. Recombinant Streptolysin O binds to cholesterol via its C-terminal domain 4, oligomerizes to form arc-shaped or ring-shaped structures, inserts amphipathic helices into the lipid bilayer, and forms transmembrane β-barrel pores, resulting in cell permeabilization. Recombinant Streptolysin O enables controllable cell membrane permeabilization, fluorescent probe delivery, and exogenous molecule uptake.

Halofuginone lactate (RU-19110 lactate), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a K_i of 18.3 nM. Halofuginone lactate is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone lactate is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca²⁺ channels. Halofuginone lactate has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.

D75-4590, a pyridobenzimidazole derivative and a β-1,6-glucan synthesis inhibitor, possesses antifungal activity.

Bafilomycin C1 is a macrolide antibiotic isolated from Streptomyces sp. Bafilomycin C1 is a potent, specific and reversible inhibitor of vacuolar-type H⁺-ATPases (V-ATPases). Bafilomycin C1 inhibits growth of gram-positive bacteria and fungi. Bafilomycin C1 induces cell apoptosis and can be used for the study of hepatocellular carcinoma (HCC).

Puromycin-d₃ is the deuterium labeled Puromycin. Puromycin dihydrochloride is the dihydrochloride salt of puromycin. Puromycin is an aminoglycoside antibiotic that inhibits protein synthesis.