lysosome

Perphenazine (Trilafon) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.

MK6-83 is the transient receptor potential channel ML3 agonist.

1. Liensinine, a kind of isoquinoline alkaloid, can antagonize the ventricular arrhythmias.

Autophagy-lysosome Activator-1 (Compound F1) is an autophagy-lysosome stimulator that effectively induces the degradation of PD-L1 or VISTA in tumor cells.

HEPES is a zwitterionic sulfonic acid buffering agent, commonly used to uphold a neutral pH of basal medium within cell cultures.HEPES is a potent inducer of lysosome biogenesis.

Fosfomycin calcium (Phosphomycin calcium salt) is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis.

An antibiotic produced by Streptomyces fradiae.

Fosfomycin sodium is a bactericidal, low-molecular weight, broad-spectrum antibiotic, with putative activity against several bacteria, including multidrug-resistant Gram-negative bacteria, by irreversibly inhibiting an early stage in cell wall synthesis.

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.

ROC-325 is an effective and orally active inhibitor of autophagy with anticancer activity. ROC-325 induces renal cell carcinoma apoptosis and exhibits favorable selectivity.

Siramesine (Lu 28-179)(Lu 28-179) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo.lysosome-destabilizing agent siramesine can induce rapid cell death in a number of cell lines at concentrations above 20 μM. In HaCaT cells, cell death was accompanied by caspase activation, rapid loss of mitochondrial membrane potential (MMP), cytochrome c release, cardiolipin peroxidation and typical apoptotic morphology, whereas in U-87MG cells most apoptotic hallmarks were not notable, although MMP was rapidly lost

MHY1485 is an mTOR activator that is cell-permeable. MHY1485 inhibits autophagosome and lysosome fusion, leading to accumulation of LC3II proteins and increased autophagosomes, thereby inhibiting cellular autophagy.

H1k is an eudistomin Y fluorescent derivative and lysosome-targeted antiproliferative agent that dose-dependently increases autophagy signalling and down-regulates the expression of cyclin-dependent kinase (CDK1) and cyclin B1.

HEPES Sodium salt is a nonvolatile zwitterionic chemical buffering agent. HEPES Sodium salt is broadly applied in cell culture. HEPES Sodium salt is effective at pH 6.8 to 8.2. HEPES Sodium salt also induces of lysosome biogenesis.

EN6-mediated ATP6V1A modification decouples the v-ATPase from the Rags, leading to inhibition of mTORC1 signaling, increased lysosomal acidification and activation of autophagy. EN6 clears TDP-43 aggregates, a causative agent in frontotemporal dementia, in a lysosome-dependent manner. EN6 is a small-molecule in vivo activator of autophagy that covalently targets cysteine 277 in the ATP6V1A subunit of the lysosomal the vacuolar H+ ATPase (v-ATPase).

IFB-088 acetate, a benzyl guanidine derivative, is used to treat diseases and cancers associated with the PPP1R15A pathway and associated with protein misfolding stress, Examples include tau disease, synaptic riboprotein disease, polyglutamine and polyalanine diseases, leukodystrophy, cystic fibrosis, multiple sclerosis, lysosome storage disorders, amyloidosis diseases, inflammation, metabolic disorders, cardiovascular diseases, osteoporosis, neurological trauma, and more.

Migalastat hydrochloride (GR181413A) is an orally available, potent and competitive inhibitor of alpha-galactosidase A. It promotes the transport of alpha-galactosidase A to the lysosome and can be used in the study of Fabry disease.

ZX782 acts as a GPX4 protein degrader and an inducer of ferroptosis (Ferroptosis), targeting GPX4 for destruction via both the ubiquitin-proteasome system and the autophagy-lysosome pathway. Following the degradation of GPX4 induced by ZX782, there is a significant increase in the accumulation of lipid reactive oxygen species (ROS) in HT1080 cells.

ZX703 (compound 5I) is a GPX4-targeting PROTAC that induces efficient, dose- and time-dependent degradation of GPX4 through both ubiquitin–proteasome and autophagy–lysosome pathways, ZX703 results in reactive oxygen species accumulation, ferroptosis induction, and strong mechanistic relevance for cancer biology and ferroptosis-focused therapeutic research.

PD-L1degrader-2 (Compound B3) is an orally effective AUTAC degrader that degrades PD-L1 via the autophagy-lysosome pathway with a DC50 of 0.5 μM. It inhibits the interaction between PD-1 and PD-L1, with an IC50 of 22.8 nM. PD-L1degrader-2 upregulates the expression of Atg9b, Lamp1, and Mitf, activating the autophagy-lysosome system. It exhibits antitumor activity in the CT26 mouse model.

LYMTAC-2 is a lysosome-targeting chimera (LYMTAC) developed to degrade membrane-associated proteins through lysosomal membrane proteins (LMP) such as RNF152, LAPTM4a, and LAPTM5. It forms a ternary complex with target proteins like KRASG12D, facilitating their relocation to lysosomes and resulting in ubiquitin-dependent degradation. This compound has potential for studying membrane protein regulation and devising strategies to counter resistance in KRAS-driven signaling pathways.

TrxR/EGFR-IN-1 (Compound L1Au2) is a TrxR/EGFR inhibitor with activity against both gefitinib-sensitive and -resistant lung cancer, effectively suppressing tumor proliferation and promoting apoptosis. It enhances GPX4 degradation through autophagosome-lysosome and proteasome pathways, leading to ferroptosis. Additionally, it induces endoplasmic reticulum stress and triggers immunogenic cell death, making it applicable for studies on gefitinib-resistant lung cancer.

BRD4 degrader-5 (Compound 23) is a protein degrader utilizing a hydrophobic tag (HyTag) that targets BRD4 for degradation through endoplasmic reticulum stress and the autophagy-lysosome pathway (DC50 = 24.7 μM). It also inhibits the proliferation of 4T1 cancer cells, with an IC50 of 20.6 μM.

LC3B recruiter 2 (34R) is an LC3B recruiting agent incorporated into the autophagy-lysosome pathway degradation system (ATTEC, Autophagy-Tethering Compounds), with a direct binding affinity for LC3B. It connects via a linker to the CDK9 inhibitor SNS-032, creating an ATTEC capable of targeting and degrading the CDK9 and Cyclin T1 complex, while also inhibiting them. Consequently, LC3B recruiter 2 exerts its function through an LC3B-dependent autophagy-lysosome pathway, interfering with the cancer cell cycle progression, thereby demonstrating antitumor activity.