AMXT-1501

AMXT-1501 is a Bacterial agent and polyamine transport system inhibitor. AMXT-1501 targets membrane phospholipids and exhibits antibacterial activity against a variety of Gram-positive and Gram-negative multidrug-resistant bacteria. AMXT-1501 inhibits capsular biosynthesis in Streptococcus pneumoniae. AMXT-1501 targets ornithine decarboxylase and polyamines to inhibit the proliferation of neuroblastoma cells. AMXT-1501 in combination with DFMO (HY-B0744) induces Apoptosis in neuroblastoma cells. AMXT-1501 is applicable to research related to multidrug-resistant bacterial infections, pneumococcal infections, Streptococcus pneumoniae infections, and neuroblastoma^[1][2][3][4]. IC50 & Target:Polyamine transport^[1] In Vitro:AMXT-1501 (1.56-50 μM) exhibits dose-dependent antibacterial activity against a variety of Gram-positive and Gram-negative multidrug-resistant (MDR) bacterial isolates, with MIC₅₀/MIC₉₀ values ranging from 3.13 to 12.5 μM^[1].
AMXT-1501 (8× MIC; 0-24 h) exhibits rapid and potent bactericidal activity against planktonic MRSA, ESBL-producing E. coli, and CR E. coli^[1].
AMXT-1501 (1-4× MIC; 0.5-24 h) reduces biofilm formation in a dose-dependent manner in most tested Staphylococcus aureus (MSSA and MRSA) and Enterococcus faecalis strains, causes severe damage to the cell membranes of MRSA and CR E. coli, increases membrane permeability and depolarizes them, thereby leading to bacterial cell death^[1].
AMXT-1501 (3.125-50 μg/mL; 90 s) binds directly to the bacterial membrane phospholipids CL and PG^[1].
AMXT-1501 (7.4 μM; cultured until OD₆₀₀ reaches 0.2-0.5) inhibits capsular polysaccharide biosynthesis by 61% in Streptococcus pneumoniae serotype 2 (strain D39), depletes intracellular polyamines and glucuronic acid, and simultaneously increases intracellular glucose levels^[2].
AMXT-1501 (7.4 μM) regulates gene expression in Streptococcus pneumoniae D39, thereby enhancing the biosynthesis of polyamines and glucose, inhibiting ATP production and fatty acid synthesis, and upregulating stress response pathways^[3].
AMXT-1501 (0.39-50 μM; 48 h) potently inhibits the viability of human neuroblastoma cell lines BE (2)-C, SMS-KCNR and SH-SY5Y in vitro, with IC₅₀ values of 17.69 μM, 17.72 μM and 14.13 μM, respectively^[4].
AMXT-1501 (2.5 μM; 96 h) induced apoptosis in BE (2)-C, SMS-KCNR and SH-SY5Y human neuroblastoma cells when used in combination with DFMO^[4]. In Vivo:AMXT-1501 (20 mg/kg; i.p.; every 12 h; 3 days) significantly reduces the size of skin abscesses and decreases MRSA loads in BALB/c mice^[1].
AMXT-1501 (20 mg/kg; i.p.; every 12 h; 3 days) significantly improves the survival rate of BALB/c mice with bacterial abdominal infection and reduces the bacterial load of CRE E. coli in their lung and liver tissues^[1].