histidine residues

By Targets:	Biochemical Assay Reagents (4) Endogenous Metabolite (2) PACAP Receptor (1)
By Research Areas:	Cancer (1) Cardiovascular Disease (1) Inflammation/Immunology (1) Metabolic Disease (2) Neurological Disease (2)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-P0294

Hexa-His 6X His Tag	Biochemical Assay Reagents	Others
Hexa-His (6X His Tag) is a commonly used affinity tag made up of six histidine residues. HEXA-HIS can bind to affinity chromatography media containing transition metal ions like nickel (Ni ²⁺) or cobalt (Co ²⁺), making it useful for protein purification .

HY-D0846

Diethyl pyrocarbonate	Biochemical Assay Reagents	Neurological Disease
Diethyl pyrocarbonate is a potent, orally active, non-specific chemical inhibitor of RNase. Diethyl pyrocarbonate has been useful in vitro as an agent relatively specific for binding to imidazole of histidine. Diethyl pyrocarbonate inhibits central chemosensitivity in rabbits. Diethyl pyrocarbonate can modify Ser, Thr, His and Tyr residues. Diethyl pyrocarbonate can be used for modeling .

HY-P11421

Cys-His Tag	Biochemical Assay Reagents	Others
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 .

HY-P1767

Prepro VIP (81-122), human	PACAP Receptor	Cardiovascular Disease
Prepro VIP (81-122), human is a prepro-vasoactive intestinal polypeptide (VIP) derived peptide, corresponding to residues 81-122. Peptide histidine valine 42 (PHV-42) has been designated to correspond exactly to Prepro VIP (81-122), which reduces both the force and frequency of spontaneous contractions of isolated rat uterus .

HY-E70933

Protease, Streptomyces griseus	Endogenous Metabolite	Metabolic Disease
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.

HY-P4599B

H-His-His-OH acetate	Biochemical Assay Reagents	Others
H-His-His-OH acetate is an oligopeptide. H-His-His-OH acetate can chelate with Ruthenium (II). H-His-His-OH inhibits the hydrolysis of metal ions at pH 7.4 .

HY-P2782A

Chloramphenicol Acetyltransferase, Escherichia coli	Endogenous Metabolite	Metabolic Disease
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.	Product Name

HY-L908

Lead-like Covalent Screening Library	1,248 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.

Lead-like Covalent Screening Library

1,248 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.

HY-L945

Sulfonyl Fluoride Fragment Library	1162 compounds
Sulfonyl fluoride (-SO₂F) overcomes the bottleneck of target selectivity in traditional covalent warheads through its unique chemical and biological properties, which rely heavily on cysteine (Cys) residues. Featuring high stability and tunable electrophilicity under physiological conditions, it can target a wide range of nucleophilic residues including lysine (Lys), tyrosine (Tyr), serine (Ser), and histidine (His). It offers the advantages of a broader druggable space, lower off-target risks, and long-lasting efficacy, with numerous reported cases in the research of covalent inhibitors, Molecular glue, PROTACs, and chemical biology probe development. MCE constructs a highly diverse sulfonyl fluoride fragment library based on the reactivity, stability and physiological compatibility of sulfonyl fluoride. The library contains 1000 efficiently synthesized and stable sulfonyl fluoride fragments, which ensure precise reactivity of the warhead and retain sufficient derivatization space for subsequent optimization. Combined with the modular strategy of SuFEx click chemistry, it enables versatile modification of compounds and functionalization of complex molecules, improves the efficiency of structural optimization and rapidly expands druggability, making it suitable for high-throughput probe and custom covalent library construction. It provides an efficient research tool for the development of broad-spectrum covalent inhibitors targeting Lys/Tyr/Ser/His, covalent PROTACs for E3 ligases and chemical biology probe development, meeting the requirements of modern drug research for high throughput, high success rate and high derivatization potential. This library contains 1,162 sulfonyl fluoride fragments with high structural diversity, favorable drug-like properties and tunable electrophilicity. It is well suited for precise targeting of non-Cys residues and meets the criteria of simple structure and high derivatization potential. It effectively improves

Sulfonyl Fluoride Fragment Library

1162 compounds

Sulfonyl fluoride (-SO₂F) overcomes the bottleneck of target selectivity in traditional covalent warheads through its unique chemical and biological properties, which rely heavily on cysteine (Cys) residues. Featuring high stability and tunable electrophilicity under physiological conditions, it can target a wide range of nucleophilic residues including lysine (Lys), tyrosine (Tyr), serine (Ser), and histidine (His). It offers the advantages of a broader druggable space, lower off-target risks, and long-lasting efficacy, with numerous reported cases in the research of covalent inhibitors, Molecular glue, PROTACs, and chemical biology probe development.

MCE constructs a highly diverse sulfonyl fluoride fragment library based on the reactivity, stability and physiological compatibility of sulfonyl fluoride. The library contains 1000 efficiently synthesized and stable sulfonyl fluoride fragments, which ensure precise reactivity of the warhead and retain sufficient derivatization space for subsequent optimization. Combined with the modular strategy of SuFEx click chemistry, it enables versatile modification of compounds and functionalization of complex molecules, improves the efficiency of structural optimization and rapidly expands druggability, making it suitable for high-throughput probe and custom covalent library construction. It provides an efficient research tool for the development of broad-spectrum covalent inhibitors targeting Lys/Tyr/Ser/His, covalent PROTACs for E3 ligases and chemical biology probe development, meeting the requirements of modern drug research for high throughput, high success rate and high derivatization potential.

This library contains 1,162 sulfonyl fluoride fragments with high structural diversity, favorable drug-like properties and tunable electrophilicity. It is well suited for precise targeting of non-Cys residues and meets the criteria of simple structure and high derivatization potential. It effectively improves

HY-L924

Boronic acid/boronic ester fragment library	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.

Boronic acid/boronic ester fragment library

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.

Cat. No.	Product Name	Type

HY-D0846

Diethyl pyrocarbonate	Biochemical Assay Reagents
Diethyl pyrocarbonate is a potent, orally active, non-specific chemical inhibitor of RNase. Diethyl pyrocarbonate has been useful in vitro as an agent relatively specific for binding to imidazole of histidine. Diethyl pyrocarbonate inhibits central chemosensitivity in rabbits. Diethyl pyrocarbonate can modify Ser, Thr, His and Tyr residues. Diethyl pyrocarbonate can be used for modeling .

Cat. No.	Product Name	Target	Research Area

HY-P0294

Hexa-His 6X His Tag	Biochemical Assay Reagents	Others
Hexa-His (6X His Tag) is a commonly used affinity tag made up of six histidine residues. HEXA-HIS can bind to affinity chromatography media containing transition metal ions like nickel (Ni ²⁺) or cobalt (Co ²⁺), making it useful for protein purification .

HY-P0046

Glycyl-L-histidyl-L-lysine 2 Publications Verification GHK; Tripeptide-1	Peptides	Neurological Disease Inflammation/Immunology
Glycyl-L-histidyl-L-lysine is a tripeptide consisting of glycine, L-histidine and L-lysine residues joined in sequence. Glycyl-L-histidyl-L-lysine is a hepatotropic immunosuppressor and shows anxiolytic effect. Glycyl-L-histidyl-L-lysine and its copper complexes show good skin tolerance .

HY-P11421

Cys-His Tag	Biochemical Assay Reagents	Others
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 .

HY-P1767

Prepro VIP (81-122), human	PACAP Receptor	Cardiovascular Disease
Prepro VIP (81-122), human is a prepro-vasoactive intestinal polypeptide (VIP) derived peptide, corresponding to residues 81-122. Peptide histidine valine 42 (PHV-42) has been designated to correspond exactly to Prepro VIP (81-122), which reduces both the force and frequency of spontaneous contractions of isolated rat uterus .

HY-P4599B

H-His-His-OH acetate	Biochemical Assay Reagents	Others
H-His-His-OH acetate is an oligopeptide. H-His-His-OH acetate can chelate with Ruthenium (II). H-His-His-OH inhibits the hydrolysis of metal ions at pH 7.4 .

HY-P10794

LH2 peptide	Peptides	Cancer
LH2 peptide is a pH-responsive cell-penetrating peptide dimer with the amino acid sequence LHHLCHLLHHLCHLAG. It can increase its uptake in tumor cells under weakly acidic conditions (such as the tumor microenvironment) through the protonation of histidine residues (pK_a approximately 6). When conjugated with the anticancer drug Paclitaxel (HY-B0015), the PTX-LH2 conjugate showed superior tumor suppression effects compared to paclitaxel alone in a subcutaneous breast tumor model. The LH2 peptide holds potential as a drug delivery vehicle in cancer research .

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

Name
Email *

	Sorry, but the email address you supplied was invalid.