autophagic flux

ML-SA5 is an MCOLN1 agonist and arrests autophagic flux by perturbing fusion between autophagosomes and lysosomes.

Indomethacin farnesil (Infree) is a prodrug of indomethacin. It acts as a nonsteroidal anti-inflammatory drug (NSAID) and disease-modifying anti-rheumatic drug (DMARD).

EACC, a reversible autophagy inhibitor, selectively impedes Stx17, an autophagosome-specific SNARE, from translocating, hence obstructing the fusion between autophagosomes and lysosomes. This compound effectively halts autophagic flux.

Clarithromycin (A-56268) is a Macrolide Antimicrobial. The mechanism of action of clarithromycin is as a Cytochrome P450 3A4 Inhibitor, and Cytochrome P450 3A Inhibitor, and P-Glycoprotein Inhibitor. The chemical classification of clarithromycin is Macrolides.

CTB (Cholera Toxin B subunit) is an activator of p300 histone acetyltransferase and induces apoptosis in MCF-7 cells.

LV-320 is a potent and uncompetitive ATG4B inhibitor with an IC 50 of 24.5 μM and a K d of 16 μM. LV-320 inhibits ATG4B enzymatic activity, blocks autophagic flux in cells, and is stable, non-toxic and active in vivo. These findings suggest that LV-320 will serve as a relevant chemical tool to study the various roles of ATG4B in cancer and other contexts [1].

PIK5-12d, a potent PROTAC PIKfyve degrader (DC50: 1.48 nM), effectively induces cytoplasmic vacuolization and inhibits autophagic flux in various prostate cancer cell lines, concurrently halting their proliferation. This compound has demonstrated significant anti-tumor activity [1].

DCAP, a broad-spectrum antibiotic, disrupts the membranes of both Gram-positive and Gram-negative bacteria. Additionally, it inhibits late-stage autophagy by blocking autophagolysosome maturation and interrupting autophagic flux [1].

Autophagy-IN-1 is a potent inhibitor of autophagy/mitophagy, blocking autophagosomal-lysosomal fusion in cancer cells while selectively increasing autophagic flux. Autophagy-IN-1 significantly inhibits tumour growth in the HCT116 mouse xenograft tumour model with low toxicity.Autophagy-IN-1 can be used to study colorectal cancer.

Nicotinic acid adenine dinucleotide phosphate (NAADP) is a secondary messenger that induces calcium mobilization. It induces calcium release from endosomes and lysosomes via two-pore channel 2 (TPC2) and TPC1, which then stimulates large-scale calcium release from granules and the endoplasmic reticulum mediated by type 1 ryanodine receptors (RyR2s), RyR3s, and inositol-(1,4,5)-triphosphate receptors (IP3Rs). NAADP induces calcium mobilization in sea urchin and starfish eggs post fertilization to block polyspermy and activate embryogenesis. NAADP-induced calcium mobilization induces VEGF-mediated angiogenesis in human umbilical vein endothelial cells (HUVECs). It also alkalizes lysosomal pH thereby inhibiting fusion between autophagosomes and lysosomes and arresting autophagic flux in mouse embryonic stem cells.

GW406108X (GW108X) is a Kif15 inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X is also an ULK1 kinase inhibitor with pIC50 values of 6.37 (427 nM) and block autophagic flux.

Autophagy-IN-2 (Compound 7h) is an inhibitor of autophagic flux which induces cancer cell apoptosis and can be used for the research of triple-negative breast cancer [1].

Gypenoside L inhibits autophagic flux and induces cell death in human esophageal cancer cells through endoplasm reticulum stress-mediated Ca2+ release. It also inhibit non-small cell lung carcinoma A549 cell inhibitory activity.

Lup-20(29)-en-28-oic acid exhibits anticancer activities in various cancer types, it Inhibits autophagic flux and synergistically enhances the anticancer activity of chemotherapeutic agents against HeLa cells.Pulsatilla saponin D has strong haemolytic act

N6-Isopentenyladenosine, an end product of the mevalonate pathway, is an autophagy inhibitor with anti-melanoma activity. N6-Isopentenyladenosine, an RNA modification found in cytokinins, regulates plant growth/differentiation and improves the efficiency