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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
2 Results for "
substrate/catalytic cleft
" in MedChemExpress (MCE) Product Catalog:
Products (2)
2 Results for "substrate/catalytic cleft" in MCE Product Catalog:
26
26 Cited Publications
Target:
Research Areas:
Cardiovascular Disease Neurological Disease Endocrinology Cancer
IU1 is a selective, reversible USP14 inhibitor with an IC50 of 4-5 μM. IU1 binds USP14’s catalytic cleft to block deubiquitinase activity. IU1 induces calpain-dependent Tau cleavage, causes ATP deficits, reduces E1~Ub thioester levels and 26S proteasome assembly. IU1 enhances 26S proteasome chymotrypsin-like activity, modulates LC3B-dependent autophagy flux, reduces cancer cell proliferation and migration, and blocks G0/G1 to S phase cell cycle transition in follicular thyroid cancer cells. IU1 activates autophagy-lysosomal and ubiquitin-proteasome pathways, triggers apoptosis, and reduces cervical cancer cell growth. IU1 enhances degradation of proteasome substrates linked to neurodegenerative disease, accelerates oxidized protein degradation, and increases oxidative stress resistance. IU1 can be used for the research of Alzheimer’s disease, follicular thyroid cancer, ischemic stroke, cervical cancer, and neurodegenerative disease .
Cat. No.: HY-114611
CAS No.: 2011754-00-8
Target:
Research Areas:
BDM44768 is an insulin-degrading enzyme (IDE) inhibitor (human IC50 = 0.06 μM; Ki = 60 nM). BDM44768 impairs D-Glucose (HY-B0389) tolerance, enhances Insulin (HY-P0035) signaling, and increases Amyloid-β concentration in an IDE-dependent manner by chelating the catalytic zinc, stabilizing the closed conformation, and binding the substrate/catalytic cleft. BDM44768 can be used in research on diabetes and metabolic dysfunction-associated steatotic liver disease (MASLD) .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
