lysosomal

ML-SA1 (Mucolipin synthetic agonist 1) is a selective TRPML agonist, inhibits Dengue virus 2 (DENV2) and Zika virus (ZIKV) by promoting lysosomal acidification and protease activity. The IC50 value of ML-SA1 against DENV2 RNA and ZIKV RNA is 8.3 μM and 52.99 μM, respectively[1].

20-DEOXYINGENOL is a natual product.

Vps34-IN-4 is a potent and selective inhibitor of VPS34 (IC50: 15 nM).

Naphthazarin (5,8-Dihydroxy-1,4-naphthoquinone) is effective by various cellular mechanisms including oxidative stress, activation of mitochondrial apoptosis-inducing factor (AIF), depolymerization of microtubules, interference with lysosomal function and p53-dependent p21 activation. It triggers apoptosis and has anti-tumor effects

Lysosomal P-gp targeted agent 1 (Compound 14) is an antitumor drug that targets lysosomal P-glycoprotein (Pgp). It is selectively transported to lysosomes via overexpressed Pgp, releasing nitric oxide that generates reactive oxygen species (ROS), causing lysosomal membrane permeabilization (LMP) and inducing apoptosis. This compound can overcome resistance mediated by P-glycoprotein, leading to cell cycle arrest while maintaining relatively low toxicity to normal cells. It exhibits antitumor activity by significantly inhibiting tumor growth.

Lysosomal α-Glucosidase (EC:3.2.1.20) is a gamma-amylase specifically acting on glycogen as well as various natural and synthetic oligosaccharides.

Lysosomal α-mannosidase (EC:3.2.1.24; MAN2B1; LAMAN) is an exoglycosidase that hydrolyzes the α-mannosidic linkages in mannose-containing glycans. It is utilized in research related to α-mannosidosis.

Esomeprazole is the S-isomer of omeprazole, inhibits the lysosomal cysteine protease legumain to prevent cancer metastasis. Esomeprazole is a proton pump inhibitors (PPI).

Siramesine hydrochloride (Lu 28-179 hydrochloride) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of Y cells and to exhibit a potent anticancer activity in vivo.

Lys05, or Lys01 trihydrochloride, is a potent, water soluble lysosomal autophagy inhibitor. Lys05 is a previously undescribed dimeric chloroquine which more potently accumulates in the lysosome and blocks autophagy compared with HCQ. Lys05 produced more p

Lalistat 2 is a selective inhibitor of lysosomal acid lipase with IC50 of 152 nM and exhibits no inhibition of human pancreatic lipase or bovine milk lipoprotein lipase (up to 10 μM).

Allixin is a phytoallexin found in garlic (Allium sativum) bulbs. Allixin has weak antimicrobial activity and exerts an anti-promoting activity against skin tumors induced by the chemical 12-O-tetradecanoylphorbol-13-acetate (TPA). Allixin also demonstrates an inhibitory effect on aflatoxin B1-induced mutagenesis.

L-Leucyl-L-Leucine methyl ester hydrochloride (Leu-Leu-ome hydrochloride) is a dipeptide condensation product of L-leucine methyl ester produced by human monocytes or polymorphonuclear leukocytes. L-Leucyl-L-Leucine methyl ester hydrochloride selectively eliminates lymphocytes with cytotoxic potential and also induces lysosomal stress.

Swainsonine (Tridolgosir) is an alkaloid isolated from Astragalus membranaceus and is a potent and reversible inhibitor of alpha-mannosidase. swainsonine has antitumour activity and induces apoptosis and cell cycle arrest in the G2/M phase.

PFB-FDGlu belongs to fluorescent dyes and is a lysosomal β-glucocerebrosidase (GCase) substrate that releases fluorescein upon hydrolysis by GCase, possessing cell permeability. This compound can be used for flow cytometric detection of GCase activity in live cells.

AZD0780 (EX-A6975, PCSK9-IN-12) is an orally active PCSK9 inhibitor with high affinity for PCSK9 (Kd < 200 nM). It binds to a specific pocket in the C-terminal domain of PCSK9 without affecting the PCSK9–LDLR interaction. AZD0780 blocks the lysosomal trafficking of the PCSK9–LDLR complex and prevents PCSK9-induced LDLR degradation, making it useful for studies related to hypercholesterolemia.

Tri-GalNAc-COOH is a ligand for the asialoglycoprotein receptor (ASGPR) and is commonly used in lysosomal targeting chimera (LYTAC) investigations.

Sinbaglustat (OGT2378) (OGT2378) is a dual inhibitor of glucose ceramide synthetase (GCS) and non-lysosomal glucose ceramidase (GBA2).Sinbaglustat is an orally administered N-alkyl iminosugar that crosses the blood-brain barrier.Sinbaglustat is used for the treatment of lysosomal storage disorders and for the study of central neurodegenerative disorders associated with lysosomal dysfunction. Sinbaglustat is used for the treatment of lysosomal storage disorders and for the study of lysosomal dysfunction-related central neurodegenerative diseases.

Ezurpimtrostat hydrochloride (GNS561 hydrochloride) is an orally available palmitoyl protein thioesterase-1 inhibitor with antifibrotic, antiviral, and anticancer effects that blocks cancer cell proliferation by interacting with palmitoyl protein thioesterase to inhibit late autophagy and dose-dependently increase lysosomal accumulation.

Chloroquine phosphate (Aralen phosphate) is an antimalarial and anti-inflammatory agent widely used for malaria and rheumatoid arthritis. Chloroquine phosphate acts as an inhibitor of autophagy and toll-like receptors, effectively suppressing SARS-CoV-2 (COVID-19) infection (EC50 = 1.13 μM). Chloroquine phosphate can be utilized in research on autophagy, lysosomal function, and tumor diseases.

1-Dodecylimidazole (N-Dodecylimidazole) is a chemical compound that acts as a cytotoxic agent and lysosomotropic detergent, inducing cell death through acid-dependent lysosomal accumulation, disrupting the lysosomal membrane, and releasing cysteine proteases into the cytoplasm. It also exhibits hypocholesterolemic and broad-spectrum antifungal activities.

DNJNAc, also known as 2-Acetamido-1,2-dideoxynojirimycin, is a highly potent and specific inhibitor of β-hexosaminidase (HEX). HEX enzymes catalyze the hydrolysis of terminal non-reducing N-acetyl-β-D-glucosamine (GlcNAc) and N-acetyl-β-D-galactosamine (GalNAc) residues from glycoconjugates such as glycoproteins, gangliosides, and glycosaminoglycans. HEX secreted by chondrocytes into the extracellular space contributes to cartilage matrix degradation, and HEX activity is elevated in the synovial fluid of osteoarthritis patients.

Gcase activator 2 is a β-glucocerebrosidase activator that induces dimerization of GCase at the endoplasmic reticulum (ER) and lysosomal pHs, increases lysosomal substrate metabolism, and has therapeutic potential for the treatment of Parkinson's and Gosheimer's diseases.

AC1115 is a highly effective and selective antiviral compound targeting SARS-CoV-2 Mpro and the host lysosomal cysteine protease cathepsin L (CTSL), exhibiting potent antiviral activity.