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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
16 Results for "
histidine residues
" in MedChemExpress (MCE) Product Catalog:
Products (16)
16 Results for "histidine residues" in MCE Product Catalog:
3
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Cat. No.: HY-P0294
CAS No.: 64134-30-1
Synonyms: 6X His Tag
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Cat. No.: HY-P11421
CAS No.: 1051859-63-2
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Cys-His Tag is a dual-purpose protein tag combining a cysteine residue and a Histidine tag. Cys-His Tag can be used to improve marker specificity or introduce covalent binding sites .
Cat. No.: HY-P1767
CAS No.: 111366-38-2
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Cat. No.: HY-103538
CAS No.: 62252-26-0
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JLK-6 is a rhomboid protease GlpG inhibitor. JLK-6 reduces the production of Amyloid β-peptide by altering the cleavage of β-amyloid precursor protein by γ-secretase, with no effect on the cleavage of Notch receptors. JLK-6 can be used in research related to Alzheimer's disease .
Cat. No.: HY-E70933
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Protease, Streptomyces griseus, exhibits broad substrate specificity. Its active site consists of one aspartic acid residue, one histidine residue, and one serine residue. Protease tends to hydrolyze the peptide bond on the carboxyl side of glutamate or aspartate.
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Cat. No.: HY-180690A
CAS No.: 3069873-81-7
Synonyms: Imidazolepyruvic acid TFA
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Cat. No.: HY-E71402
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2-(3-Amino-3-carboxypropyl)histidine synthase (EC 2.5.1.108) is a [4Fe-4S] enzyme that modifies a histidine residue of translation elongation factor 2 (EF2) via a 3-amino-3-carboxypropyl radical. 2-(3-Amino-3-carboxypropyl)histidine synthase (EC 2.5.1.108) is involved in the biosynthesis of diphthamide.
Cat. No.: HY-P4599B
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Cat. No.: HY-187411A
Synonyms: DOPE-PEG2000-Mal-Cys-RRRRRRHHHH
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DOPE-PEG2000-R6H4 (DOPE-PEG2000-Mal-Cys-RRRRRRHHHH) is an amphiphilic lipid-PEG-peptide conjugate consisting of DOPE (1,2-dioleoyl-sn-glycero-3-phosphoethanolamine), PEG2000, and the R6H4 peptide, a histidine-rich cell-penetrating peptide containing arginine and histidine residues. DOPE-PEG2000-R6H4 is used for intracellular delivery of drugs and nucleic acids.
Cat. No.: HY-P2782A
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Chloramphenicol Acetyltransferase, Escherichia coli is a bacterial enzyme that detoxifies the antibiotic chloramphenicol and is responsible for chloramphenicol resistance in bacteria. Chloramphenicol Acetyltransferase, Escherichia coli covalently attaches an acetyl group from acetyl-CoA to chloramphenicol, which prevents chloramphenicol from binding to ribosomes. A histidine residue, located in the C-terminal section of Chloramphenicol Acetyltransferase, Escherichia coli, plays a central role in its catalytic mechanism.
Cat. No.: HY-P10794
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Cat. No.: HY-L908
1,244 compounds
Small molecule covalent inhibitors, or irreversible inhibitors, are a type of inhibitors that exert their biological functions by irreversibly binding to target through covalent bonds. Compared with non-covalent inhibitors, covalent inhibitors have obvious advantages in bioactivity, such that covalent warheads can target rare residues of a particular target protein, thus leading to the development of highly selective inhibitors and achieving a more complete and continued target occupancy in living systems. In recent years, the distinct strengths of covalent inhibitors in overcoming drug resistance had been recognized. However, toxicity can be a real challenge related to this class of therapeutics due to their potential for off-target reactivity and has led to these drugs being disfavored as a drug class. The drug design and optimization of covalent inhibitors has become a hot spot in drug discovery.
MCE Lead-like Covalent Screening Library offers a valuable resource of 1,049 lead-like compounds with commonly used covalent warheads. These warheads, such as acrylamide, activated terminal alkyne, acyloxymethyl ketone, and boronic acid, are capable of reacting with specific amino acid residues, including cysteine, lysine, serine, and histidine. The inclusion of these reactive warheads in the library allows researchers to explore the potential of covalent inhibition, a powerful approach in drug discovery.
Cat. No.: HY-L924
1,488 compounds
Boronic acid and boronic ester represent a relatively novel and promising chemical structure in drug design. Boronic acid exists in an sp²-hybridized state, possessing an empty p-orbital that can act as a Lewis acid to accept lone pairs from heteroatoms (O, N, or S). This Lewis acidity enables it to form reversible covalent bonds with amino acid residues such as lysine, serine, threonine, and histidine. Currently, five FDA-approved drugs containing boronic acid or boronic ester predominantly involve such covalent binding mechanisms in their interactions with target proteins. Furthermore, boronic acid can serve as a bioisostere for carboxylic acids, phosphates, and phenolic groups, utilized to improve pharmacokinetic properties and enhance drug efficacy.
To date, five boron-containing drugs have been approved by the FDA. The unique properties of boronic acids and boronic esters confer significant potential in drug design, with applications spanning cancer therapy (e.g., multiple myeloma), anti-infectives (e.g., fungal infections, tuberculosis), anti-inflammatory treatments (e.g., atopic dermatitis), antibacterial agents (e.g., carbapenem-resistant bacterial infections), and Reactive Oxygen Species (ROS)-responsive prodrugs, among others. The MCE Boronic Acid/Boronic Ester Fragment Library, which contains 1,488 compounds, serves as a valuable tool for the development of boron-containing drugs.
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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
