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.

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.

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.

CES2A-IN-3 (Compound 9d) is a potent covalent inhibitor targeting human carboxylesterase 2A (hCES2A) with an IC50 value of 0.12 nM. It shows promise for research into diarrhea and ulcerative colitis.

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].

HumanCES2Enzyme is a recombinant CES2 enzyme that hydrolyzes carboxylic ester bonds, thioester bonds, and amide bonds in numerous exogenous and endogenous compounds (including lipids).

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

Cipemastat is a competitive inhibitor of human collagenases 1, 2, and 3 (Kis: 3.0, 4.4, and 3.4 nM).

ES-242-4 is a useful organic compound for research related to life sciences. The catalog number is T125980 and the CAS number is 136565-69-0.

Antibiotic ES 242-3 is a useful organic compound for research related to life sciences. The catalog number is T125981 and the CAS number is 136565-68-9.

Thalidomide-O-amido-C8-NH2 (Cereblon Ligand-Linker Conjugates 2) is a synthesized E3 ligase ligand-linker conjugate containing a Thalidomide-based cereblon ligand and a linker, useful in the synthesis of PROTACs, as per reference [1].

cIAP1 Ligand-Linker Conjugates 2 Hydrochloride is a chemical compound that combines an IAP ligand, targeting the E3 ubiquitin ligase, with a PROTAC linker and is utilized in the creation of SNIPERs[1].

cIAP1 Ligand-Linker Conjugates 2 is a chemical compound that combines an IAP ligand for the E3 ubiquitin ligase with a PROTAC linker. This compound is particularly useful in the design of SNIPERs [1].

(S,R,S)-AHPC-PEG1-OTs is a chemically synthesized conjugate serving as a ligase ligand-linker for E3 ligase, incorporating the VHL ligand derived from (S,R,S)-AHPC and a 1-unit PEG linker. This compound is commonly utilized in PROTAC technology.

Pomalidomide-amido-C4-amido-PEG2-C2-NH-Boc is a novel synthesized conjugate compound functioning as an E3 ligase ligand-linker in PROTAC technology. Incorporating a Pomalidomide-derived cereblon ligand that selectively binds to the E3 ligase cereblon and a 2-unit PEG linker, it provides stability and flexibility to the conjugate.

Pomalidomide-amido-C4-amido-C6-NH-Boc, a synthesized conjugate, is a ligand-linker that incorporates the cereblon ligand based on Pomalidomide and a PROTAC technology linker.

Pomalidomide-PEG4-C2-NH2 (E3 Ligase Ligand-Linker Conjugates 22) is a synthesized E3 ligase ligand-linker conjugate incorporating the Pomalidomide-based cereblon ligand and 4-unit PEG linker.

Thalidomide-O-amido-PEG2-C2-NH2 TFA (E3 Ligase Ligand-Linker Conjugates 24 TFA) is a synthesized E3 ligase ligand-linker conjugate incorporating the Thalidomide-based cereblon ligand and a 2-unit PEG linker, utilized in PROTAC technology.

Thalidomide-O-amido-C6-NH2 TFA (Cereblon Ligand-Linker Conjugates 11 TFA) is a synthesized E3 ligase ligand-linker conjugate comprising a Thalidomide-based cereblon ligand and a linker.

VH032-thiol-C6-NH2, also known as VHL Ligand-Linker Conjugates 14, is a synthesized compound that functions as an E3 ligase ligand-linker conjugate. This compound combines the VH032 based VHL ligand with a linker commonly utilized in PROTAC technology.

(S,R,S)-AHPC-C4-NH2 hydrochloride (E3 ligase Ligand-Linker Conjugates 28) is a synthesized E3 ligase ligand-linker conjugate comprising the (S,R,S)-AHPC-based VHL ligand and a linker.