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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
172 Results for "
Ppi
" in MedChemExpress (MCE) Product Catalog:
Products (172)
172 Results for "Ppi" in MCE Product Catalog:
Cat. No.: HY-B0656AR
CAS No.: 117976-90-6
Synonyms: LY307640 sodium (Standard)
Research Areas:
Rabeprazole (sodium) (Standard) is the analytical standard of Rabeprazole (sodium). This product is intended for research and analytical applications. Rabeprazole sodium (LY307640 sodium) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H +/K +-ATPase. Rabeprazole sodium induces apoptosis. Rabeprazole sodium acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole sodium can be used for the research of gastric ulcerations and gastroesophageal reflux .
Cat. No.: HY-B0656R
CAS No.: 117976-89-3
Synonyms: LY307640 (Standard)
Research Areas:
Rabeprazole (Standard) is the analytical standard of Rabeprazole. This product is intended for research and analytical applications. Rabeprazole (LY307640) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H +/K +-ATPase. Rabeprazole induces apoptosis. Rabeprazole acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole can be used for the research of gastric ulcerations and gastroesophageal reflux .
Cat. No.: HY-L913
105 compounds
Recently, significant advancements in tyrosine-targeting electrophiles have primarily occurred in the field of protein-protein interactions (PPIs), where cysteine residues are often underrepresented and novel chemistries are needed to address these interfaces. In this context, tyrosines are frequently more accessible compared to more buried binding sites. Moreover, they are commonly found at "hot spots," which are functional epitopes of PPIs, with 12.3% of the residues consisting of tyrosines. This prevalence is likely due to the hydrophobic nature of tyrosine, its ability to participate in aromatic π-interactions, and its capacity for hydrogen bonding. Beyond PPIs, some progress has also been made in covalent tyrosine targeting in other areas where more commonly addressed side chains are lacking. Even though tyrosine has a slightly lower pKa value compared to the protonated lysine side chain (approximately 10 vs. 10.5 for the unprotected amino acid side chains), significantly less progress has been made in the development of tyrosine-targeted covalent ligands compared to lysine. This is likely due to the reduced flexibility of the tyrosine side chain and the greater steric hindrance of its hydroxy group, which makes it more challenging to adopt suitable reaction geometries.
Through careful selection, we constructed a structural filter containing over 110 electrophilic groups. By analyzing the electrophilic fragments selected by the structural filter, we removed any molecules with trivial or undesirable structural features. Ultimately, we obtained 124 fragment molecules which can target tyrosine residue and can be used for fragment-based covalent drug discovery.
Cat. No.: HY-L943
37030 compounds
MCE-18 stands for Medicinal Chemistry Evolution 2018, which was first published in Journal of Medicinal Chemistry in 2019 for assessing molecular novelty and three-dimensional complexity. Developed based on Clarivate global pharmaceutical patent database, this descriptor was constructed via big-data analysis covering 28,161 patented lead compounds, 1,370 approved drugs and nearly 30,000 preclinical-to-phase III drug candidates from 23 top pharmaceutical companies worldwide between 1950 and 2018, followed by structural clustering and removal of redundant outdated scaffolds for data denoising. Its scoring system integrates five core structural features including aromatic ring (AR), aliphatic heterocycle (NAR), chiral center (CHIRAL), spiro atom (SPIRO), cyclic and acyclic sp³ carbon ratio together with a quadratic topological correction factor. Breaking the limitations of the single Fsp³ parameter, MCE-18 effectively distinguishes conventional flat aromatic scaffolds from modern 3D-enriched novel chemotypes, overcoming typical drawbacks of traditional compound libraries such as scaffold redundancy, low screening hit rates and poor compatibility with allosteric and PPI-related difficult targets.
This library contains over 37,000 structurally diverse compounds with favorable overall drug-likeness, suitable for high-throughput screening against canonical targets including kinases, GPCRs and proteases as well as challenging allosteric and PPI targets. Compounds comply with the developmental trend of modern novel drug discovery, supporting routine primary screening as well as early hit identification of allosteric modulators and PPI inhibitors, serving as an efficient screening resource for early-stage innovative drug discovery.
Cat. No.: HY-100341R
CAS No.: 312271-03-7
Research Areas:
M2I-1 (Standard) is the analytical standard of M2I-1 (HY-100341). This product is intended for research and analytical applications. M2I-1 is a Mad2 inhibitor targeting the binding of Mad2 to Cdc20, an essential protein-protein interaction (PPI) within the spindle assembly checkpoint (SAC) .
Cat. No.: HY-150958
RAD51-IN-8, a new RAD51 binder, is a RAD51-BRCA2 inhibitor that inhibits the RAD51 BRCA2 protein protein interaction. RAD51-IN-8 also is a protein−protein interaction (PPI) inhibitor. RAD51-IN-8 has inhibitory activity for H4A4 with an EC50 value of 19 μM .
Cat. No.: HY-157929
Target:
Research Areas:
Keap1-Nrf2-IN-19 (compound 33) is an oral active Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with the Kd value of 0.0014 μM. Keap1-Nrf2-IN-19 exhibits less than 50% inhibition at 30 μM against hERG and 10 μM against CYPs .
Cat. No.: HY-168161
CAS No.: 2771115-65-0
Target:
Research Areas:
Keap1-Nrf2-IN-23 (compound 56) is an inhibitor of the Keap1–Nrf2 PPI (IC50=16.0 nM). Keap1-Nrf2-IN-23 binds to Keap1 with a Kd value of 3.07 nM. Keap1-Nrf2-IN-23 has oral activity .
Cat. No.: HY-17507S
CAS No.: 922727-65-9
Synonyms: BY1023-d6; SKF96022-d6
Cat. No.: HY-17507S1
CAS No.: 922727-37-5
Synonyms: BY1023-d3; SKF96022-d3
Cat. No.: HY-B0656AS1
CAS No.: 1216494-11-9
Synonyms: LY307640-d3 sodium
Cat. No.: HY-B0656S1
CAS No.: 1261392-48-6
Synonyms: LY307640-13C,d3
Cat. No.: HY-N19296
CAS No.: 861145-00-8
Category:
Target:
Cat. No.: HY-149092
CAS No.: 2097497-16-8
Target:
Research Areas:
Anticancer agent 109 (compound 6-15) is an inhibitor of the Gas6-Axl axis with anti-cancer activity. Anticancer agent 109 inhibits the expression of Gas6 and Axl, and the expression p-PI3K and p-AKT in cancer cells, leads to G1 phase arrest and promotes cancer cells apoptosis, and inhibits tumor growth significantly in nude mouse tumor bearing models .
Cat. No.: HY-100862R
CAS No.: 1622262-55-8
Target:
Research Areas:
BRCA1-IN-2 (Standard) is the analytical standard of BRCA1-IN-2 (HY-100862). This product is intended for research and analytical applications. BRCA1-IN-2 (compound 15) is a cell-permeable protein-protein interaction (PPI) inhibitor for BRCA1 with an IC50 of 0.31 μM and a Kd of 0.3 μM, which shows antitumor activities via the disruption of BRCA1 (BRCT)2/protein interactions .
Cat. No.: HY-113371R
CAS No.: 6061-96-7
Synonyms: Methylcitric acid (Standard)
Cat. No.: HY-123746
CAS No.: 332132-39-5
Target:
Research Areas:
E5700 is an orally active squalene synthase inhibitor, antimalarial agent and antifungal agent with an IC50 of 0.49 nM (without PPi) against squalene synthase from T. cruzi epimastigotes. E5700 shows antiparasitic activities against Trypanosoma cruzi. E5700 inhibits the growth and alters the lipid prolife and the ultrastructure of a multiple agent-resistant C. tropicalis strain. E5700 is a potent and selective inhibitor of the growth of Leishmania amazonensis .
Cat. No.: HY-15295R
CAS No.: 881681-01-2
Synonyms: TAK-438 (Standard)
Target:
Research Areas:
Vonoprazan (Fumarate) (Standard) is the analytical standard of Vonoprazan (Fumarate). This product is intended for research and analytical applications. Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H+,K+-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease .
Cat. No.: HY-157928
Target:
Research Areas:
Keap1-Nrf2-IN-18 (Compound 22) is an orally active Keap1-Nrf2 protein-protein interaction (PPI) inhibitor with good pharmacokinetics (PK) profiles and more potent in vivo activities in rats. Keap1-Nrf2-IN-18 has the strongest inhibitory activity in structure−activity relationship (SAR) study (KD = 0.0029 μM) .
Cat. No.: HY-173187
Target:
Research Areas:
Keap1-Nrf2-IN-27 (compound 1C) is a inhibitor of Keap1-Nrf2 protein-protein interaction (PPI) with KD2 value of 0.119 μM. Keap1-Nrf2-IN-27 suppresses the expression of pro-inflammatory cytokine TNF-α and IL-6 in the LPS-induced RAW264.7 cell model .
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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
