es2

Endosidin-2 is an exocyst inhibitor, a cell-permeable benzylidene benzoylhydrazine, that binds to the exocyst component of the 70 kDa (EXO70) subunit of the exocyst complex (Kd = 253 μM, EXO70A1).Endosidin-2 disrupts protein translocation between the endosomes and plasma membrane, thereby facilitating translocation of proteins to the vesicle for degradation. It also inhibits recirculation of endocytosed transferrin to the plasma membrane in HeLa cells and targets multiple isoforms of mammalian EXO70, leading to dysregulation of exocytosis.Endosidin2 can be used as a tool molecule to study cytosolization.

Compound LE-77, known as FXR CES2 modulator 1, functions as a dual regulator that activates FXR and inhibits CES2. It effectively mitigates the intestinal toxicity of irinotecan.

OES2-0017 exhibits strong synergistic effects and growth inhibition in collaboration with polyamines within a low micromolar range. At low concentrations, OES2-0017 inhibits spermidine spermine N1-acetyltransferase (SpeG) (IC50: 34.82 μM) and other polyamine detoxifying enzymes, while at higher concentrations, it disrupts bacterial membranes.

hCES2A-IN-2 (compound 14n) is an orally active, highly specific, irreversible, covalent inhibitor of hCES2A with an IC50 of 0.04 nM. It targets and covalently binds to the catalytic serine residue (Ser-228) of hCES2A. hCES2A-IN-2 can significantly mitigate irinotecan-induced gastrointestinal toxicity (ITGT) without diminishing the antitumor efficacy of irinotecan in tumor-bearing mice.

hCES2-IN-1 (Compound 24) is a reversible and selective inhibitor of the human carboxylesterase 2 (hCES2) enzyme, with an IC50 of 6.72 μM. This compound reduces hCES2 levels in vivo and is effective in treating irinotecan-induced delayed diarrhea and DSS-induced ulcerative colitis [1].

hCES2A-IN-1 (compound 20w), a potent hCES2A inhibitor derived from bysspectin A, exhibits an IC50 value of 1.6 nM, demonstrating an approximately 1000-fold potency enhancement compared to its lead compound, bysspectin A [1].

BTYNB (MDK6620) is an inhibitor of the oncofetal mRNA-binding protein IMP1 (IC50 = 5 μM for IMP1 binding to c-Myc mRNA). MDK6620 downregulates β-TrCP1 mRNA and reduces activation of nuclear transcriptional factors-kappa B (NF-κB). It disrupts this enhancer function by impairing IGF2 mRNA-binding protein 1 (IGF2BP1)-RNA association

NSC348884 is a nucleophosmin inhibitor disrupts oligomer formation and induces apoptosis, inhibits cell proliferation at an IC50 of 1.7-4.0 μM in distinct cancer cell lines.

Coumestrol that existed in soybean products suppresses the proliferation of ES2 cells (IC50: 50 μM). It exhibits activities against neurological disorders, cancers and autoimmune diseases.