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protein nucleophiles

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By Targets:	Biochemical Assay Reagents (2) Dipeptidyl Peptidase (1) Drug Derivative (1) Ligands for E3 Ligase (2) Reactive Oxygen Species (ROS) (1) Transmembrane Glycoprotein (1)
By Research Areas:	Cancer (2) Inflammation/Immunology (1)

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-137383

Sulfo-SANPAH	Biochemical Assay Reagents Reactive Oxygen Species (ROS)	Others
Sulfo-SANPAH is a primary amine-nitrobenzene azide cross-linker. Sulfo-SANPAH improves the functionalization process of PDMS surfaces, is covalently bound to the PAAm gel surface. Sulfo-SANPAH is widely used to crosslink ECM proteins to various substrates, including acrylic-based hydrogels, such as polyacrylamide hydrogels. Sulfo-SANPAH facilitates covalent binding through its negatively charged sulfonate group on its N-hydroxysuccinimide ester ring and a photoactivated phenyl azide group that is highly reactive with nucleophiles and free radicals .

HY-101974

Biotin-PEG3-Bromide	Biochemical Assay Reagents	Others
Biotin-PEG3-Bromide is a short PEG linker featuring a biotin group and a bromide. The bromide is a halogen which is easily displaced by nucleophiles such as alcohols or amines. Alternatively, bromide can be applied in a number of cross-coupling reactions such as in a Suzuki reaction. Biotin is useful for affinity-based applications such as pull-down assays or for ligating with streptavidin proteins.

HY-W586329

Thalidomide-4-carbaldehyde	Ligands for E3 Ligase	Others
Thalidomide-4-carbaldehyde is a Thalidomide analogue with an aldehyde. Thalidomide recruiits E3 ligase for the ubiquitinylation and subsequent proteolysis of target proteins. The aldehyde is highly reactive towards amine nucleophiles through reductive amination among other reactions.

HY-W451211

Thalidomide-5-carbaldehyde	Ligands for E3 Ligase	Cancer
Thalidomide-5-carbaldehyde is a Thalidomide analogue with an aldehyde. Thalidomide recruiits E3 ligase for the ubiquitinylation and subsequent proteolysis of target proteins. The aldehyde is highly reactive towards amine nucleophiles through reductive amination among other reactions.

HY-N19808

2-Deacetyl-4-tigloylchamissionolide	Drug Derivative	Cancer
2-Deacetyl-4-tigloylchamissionolide is a heliangolide-type sesquiterpene lactone, a derivative of Chamissonolide (HY-N19727), and a cytotoxic agent. 2-Deacetyl-4-tigloylchamissionolide exerts cytotoxicity via alkylating biological nucleophiles, targeting free thiol groups in proteins to interfere with their functions. 2-Deacetyl-4-tigloylchamissionolide exhibits different chromatographic behaviors in TLC and HPLC. 2-Deacetyl-4-tigloylchamissionolide can be used for the research of Ehrlich ascites carcinoma .

HY-W121887

Zomepirac acyl-O-β-D-glucuronide Zomepirac glucuronide	Dipeptidyl Peptidase Transmembrane Glycoprotein	Inflammation/Immunology
Zomepirac acyl-O-β-D-glucuronide (Zomepirac glucuronide) is a dipeptidyl peptidase IV Inhibitor. Zomepirac acyl-O-β-D-glucuronide is an unstable and chemically reactive metabolite of Zomepirac (HY-B0890A). Zomepirac acyl-O-β-D-glucuronide forms covalent adducts with cell membrane glycoproteins. Zomepirac acyl-O-β-D-glucuronide can be used for research on immunotoxicity .

Cat. No.	Product Name

HY-L915

Lysine Focused Covalent Fragment Library	421 compounds
Lysine is the second most common target residue used in the design of TCIs and related covalent ligands. Its appeal lies in its abundance in human proteins, which is approximately three times higher than that of cysteine (5.8% vs. 1.9%). This significantly increases the number of proteins suitable for covalent targeting, especially given that many human proteins lack ligandable cysteine residues. Moreover, it has been suggested that functional lysines have a lower probability of being replaced by mutation, as they often play a crucial role in catalysis by acting as bases or nucleophiles. Additionally, lysines are essential for maintaining the structural integrity of proteins and for regulating post-translational modifications (PTMs). Consequently, targeting lysine has garnered significant interest in recent years. 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 445 fragment molecules which can target lysine residue and can be used for fragment-based covalent drug discovery.

Lysine Focused Covalent Fragment Library

421 compounds

Lysine is the second most common target residue used in the design of TCIs and related covalent ligands. Its appeal lies in its abundance in human proteins, which is approximately three times higher than that of cysteine (5.8% vs. 1.9%). This significantly increases the number of proteins suitable for covalent targeting, especially given that many human proteins lack ligandable cysteine residues. Moreover, it has been suggested that functional lysines have a lower probability of being replaced by mutation, as they often play a crucial role in catalysis by acting as bases or nucleophiles. Additionally, lysines are essential for maintaining the structural integrity of proteins and for regulating post-translational modifications (PTMs). Consequently, targeting lysine has garnered significant interest in recent years.

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 445 fragment molecules which can target lysine residue and can be used for fragment-based covalent drug discovery.

Biotin-PEG3-Bromide	Fluorescent Dyes
Biotin-PEG3-Bromide is a short PEG linker featuring a biotin group and a bromide. The bromide is a halogen which is easily displaced by nucleophiles such as alcohols or amines. Alternatively, bromide can be applied in a number of cross-coupling reactions such as in a Suzuki reaction. Biotin is useful for affinity-based applications such as pull-down assays or for ligating with streptavidin proteins.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N19808

2-Deacetyl-4-tigloylchamissionolide	Structural Classification Terpenoids Sesquiterpenes Plants Compositae Source Classification	Drug Derivative
2-Deacetyl-4-tigloylchamissionolide is a heliangolide-type sesquiterpene lactone, a derivative of Chamissonolide (HY-N19727), and a cytotoxic agent. 2-Deacetyl-4-tigloylchamissionolide exerts cytotoxicity via alkylating biological nucleophiles, targeting free thiol groups in proteins to interfere with their functions. 2-Deacetyl-4-tigloylchamissionolide exhibits different chromatographic behaviors in TLC and HPLC. 2-Deacetyl-4-tigloylchamissionolide can be used for the research of Ehrlich ascites carcinoma .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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