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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
8 Results for "
selectivity cleft
" in MedChemExpress (MCE) Product Catalog:
Products (8)
8 Results for "selectivity 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-W380450
CAS No.: 46817-91-8
Synonyms: Viloxazin; Emovit
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Research Areas:
Viloxazine is a non-brain-penetrant, selective norepinephrine transporter (NET) inhibitor (IC50= 0.26 μM) and 5-HT receptor modulator. Viloxazine antagonizes 5-HT2B receptors (Ki=4.2 μM) and agonizes 5-HT2C receptors (EC50= 32 μM), respectively, and enhances 5-HT neurotransmission by modulating 5-HT2B/C receptors. Viloxazine also competitively inhibits NET from increasing NE and DA levels in the synaptic cleft, and can be used in the study of attention deficit hyperactivity disorder (ADHD) .
Synonyms: Viloxazin hydrochloride; Emovit hydrochloride
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Research Areas:
Viloxazine hydrochloride is a non-brain-penetrant, selective norepinephrine transporter (NET) inhibitor (IC50=0.26 μM) and 5-HT receptor modulator. Viloxazine antagonizes 5-HT2B receptors (Ki=4.2 μM) and agonizes 5-HT2C receptors (EC50=32 μM), respectively, and enhances 5-HT neurotransmission by modulating 5-HT2B/C receptors. Viloxazine also competitively inhibits NET from increasing NE and DA levels in the synaptic cleft, and can be used in the study of attention deficit hyperactivity disorder (ADHD) .
Cat. No.: HY-174462
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Research Areas:
AChE-IN-90 (Compound 5b) is an orally active, brain-penetrant and potent acetylcholinesterase (AChE) inhibitor with an IC50 value of 0.023 μM against human AChE and lower selectivity for butyrylcholinesterase (BuChE) (IC50 1.8 μM). AChE-IN-90 increases acetylcholine levels in the synaptic cleft. AChE-IN-90 is promising for research of neurodegenerative diseases such as Alzheimer's disease .
Cat. No.: HY-W380450R
CAS No.: 46817-91-8
Synonyms: Viloxazin (Standard); Emovit (Standard)
Target:
Research Areas:
Viloxazine is a non-brain-penetrant, selective norepinephrine transporter (NET) inhibitor (IC50= 0.26 μM) and 5-HT receptor modulator. Viloxazine antagonizes 5-HT2B receptors (Ki=4.2 μM) and agonizes 5-HT2C receptors (EC50= 32 μM), respectively, and enhances 5-HT neurotransmission by modulating 5-HT2B/C receptors. Viloxazine also competitively inhibits NET from increasing NE and DA levels in the synaptic cleft, and can be used in the study of attention deficit hyperactivity disorder (ADHD) .
Cat. No.: HY-W723158
CAS No.: 100992-60-7
Research Areas:
Epibestatin hydrochloride is an epimer of Bestatin (HY-B0134), a DPP4 inhibitor and protease inhibitor, with an IC50 of 17 μM against DPP4. As a stabilizer, Epibestatin hydrochloride binds to the cleft between 14-3-3 protein and plant proton pump PMA2, selectively stabilizing their interaction without affecting other 14-3-3 client proteins. Epibestatin hydrochloride triggers stomatal opening in leaf epidermis of Commelina communis. Epibestatin hydrochloride can be used in studies related to type 2 diabetes .
Cat. No.: HY-P0112
CAS No.: 1027141-02-1
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Z-VAE (OMe)-FMK is a selective inhibitor of UCHL1, with better selectivity over UCHL3 and UCHL5. Z-VAE (OMe)-FMK binds to the active site cleft, covalently modifies the active site cysteine C90 to form a thioether bond, binds to inactive UCHL1 with a misaligned catalytic triad, and acts via a two-step addition-folding/migration/displacement mechanism. Z-VAE (OMe)-FMK stabilizes interactions through hydrogen bonding with oxyanion hole residues and van der Waals interactions with surrounding residues. Z-VAE (OMe)-FMK can be used in research related to colorectal cancer, lung cancer, pancreatic cancer, and Alzheimer's disease .
Cat. No.: HY-182927
KLHL12 ligand-1 is a KLHL12 Kelch domain ligand with a Ki of 0.33 μM, Ka of 0.33 μM, submicromolar binding affinity, and selective binding over KEAP1/KLHL19. KLHL12 ligand-1 binds in the substrate cleft of KLHL12, with its 4-methyl group forming a CH-π interaction with Tyr334. KLHL12 ligand-1 binds to cellular KLHL12 in permeabilized and intact cells, and has solvent-exposed positions suitable for modification to create PROTACs. KLHL12 ligand-1 can be used for the research of cancer .
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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
