nucleophile

By Targets:	Autophagy (3) Bacterial (3) Biochemical Assay Reagents (2) Endogenous Metabolite (1) FAAH (4) Fluorescent Dye (1) Fungal (1) Glutathione S-transferase (1) Glyoxalase (GLO) (1) HIV (1) Proteasome (1)
By Research Areas:	Cancer (3) Cardiovascular Disease (1) Infection (3) Inflammation/Immunology (2) Metabolic Disease (1) Neurological Disease (2)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-W009177

S-Methylglutathione	Glyoxalase (GLO)	Others
S-Methylglutathione is an S-substitued glutathione and a stronger *nucleophile* than GSH . S-Methylglutathione has inhibitory effect on glyoxalase 1 .

HY-N0548

α-Angelica lactone 2 Publications Verification	Glutathione S-transferase	Cancer
α-Angelica lactone is a naturally occurring anticarcinogen and an vinylogous nucleophile. α-Angelica lactone can give the chiral δ-amino γ,γ-disubstituted butenolide carbonyl derivatives and exhibitselectrophilic trapping at the γ-carbon. α-Angelica lactone exerts strong chemoprotective effects by selective enhancement of glutathione-S-thansferase (GST) and UDP-glucononosyltransferase (UGT) detoxification enzymes .

HY-20556

DBU 1,8-Diazabicyclo[5.4.0]undec-7-ene	Others	Others
DBU acts as a nucleophile and can work as a catalyst .

HY-128429

Trans-2-Hexenal	Endogenous Metabolite	Others
Trans-2-Hexenal can be used for the determination of low-molecular-weight carbonyl compounds which are reactive with biological nucleophiles in biological samples .

HY-18081

PF 750	FAAH Autophagy	Metabolic Disease
PF 750 is a selective and covalent fatty acid amide hydrolase (FAAH) inhibitor, with IC₅₀s varied from 16.2-595 nM in different pre-incubation times. Covalently modifies the enzyme’s active site serine nucleophile .

HY-150226

Enzyme-IN-1	Proteasome	Inflammation/Immunology
Enzyme-IN-1 (compound 1) is a peptide-based inhibitor of N-terminal nucleophile (Ntn) hydrolases. Specifically, Enzyme-IN-1 inhibits the chymotrypsin-like activity (CT-L) of the 20S proteasome. Enzyme-IN-1 may has potential antiinflammatory properties .

HY-14380

PF-3845 1 Publications Verification	FAAH Autophagy	Inflammation/Immunology Cancer
PF-3845 is a potent, selective, irreversible and orally active inhibitor of fatty acid amide hydrolase (FAAH), with a K_i of 0.23 μM. PF-3845 is a covalent inhibitor that carbamylates FAAH's serine nucleophile. PF-3845 can reduce pain sensation, inflammation, and anxiety/depression without substantial effects on motility or cognition .

HY-131846

6-Cl-5'-PuMP 6-Chloropurine 5'-ribonucleotide	Others	Others
6-Cl-5'-PuMP is a reactive analogue of adenosine 5’-O-monophosphate (5’-AMP), and is suitable for modifying position 6 using various nucleophiles .

HY-126944

2-Aminobenzanilide 2-Amino-N-phenylbenzamide	Biochemical Assay Reagents	Cancer
2-Aminobenzamide is a neutral and stable compound used as fluorescent tag, numerously in Glycan analysis. 2-aminobenzamide acts as the starting material for several important reactions like Bargellini reaction as an competent ambident nucleophile. Specifically 2-aminobenzamide and its derivatives are used in the blood coagulation cascade .

HY-112526

Thiofluor 623	Fluorescent Dye	Others
Thiofluor 623 (Compound 3) is a fluorescent turn-on probe that can be used for the selective sensing and bioimaging of thiols. Thiofluor 623 displays excellent immunity to interference from nitrogen and oxygen nucleophiles. Thiofluor 623 is essentially nonfluorescent in the absence of thiols, which cleave the probe and release the red-emissive donor-acceptor fluorophore (Ex=563 nm, Em=623 nm) .

HY-W728451

URB694	FAAH	Cardiovascular Disease Neurological Disease
URB694 is a carbamate FAAH inhibitor that irreversibly carbamoylate the nucleophile catalytic serine in FAAH active site. URB694 exhibits antidepressant-like activity and cardioprotective effects. URB694 can be used to prepare ¹¹C-Carbonyl-URB694 for in vivo positron emission tomography (PET) imaging studies of the brain FAAH .

HY-W010243

Methylisothiazolinone hydrochloride	Bacterial	Infection
Methylisothiazolinone hydrochloride is the constituent of the biocide Kathon CG. Methylisothiazolinone hydrochloride is an isothiazolone derivative widely used as a preservative. Methylisothiazolinone hydrochloride is also a moderate sensitizer and reacts with GSH .

HY-106991A

Amustaline dihydrochloride S-303 dihydrochloride	HIV Bacterial	Infection
Amustaline (S-303) dihydrochloride, a nucleic acid-targeted alkylator, is an efficient pathogen inactivation agent for blood components containing red blood cells. Amustaline dihydrochloride has three components: an acridine anchor (an intercalator that targets nucleic acids non-covalently), an effector (a bis-alkylator group that reacts with nucleophiles), and a linker (a small flexible carbon chain containing a labile ester bond that hydrolyzes at neutral pH to yield non-reactive breakdown products) .

HY-10865

LY2183240 2 Publications Verification	FAAH Autophagy	Neurological Disease
LY2183240 is a highly potent blocker of anandamide uptake (IC₅₀= 270 pM; K_i=540 nM). LY2183240 is a potent, covalent inhibitor of the endocannabinoid-degrading enzyme fatty acid amide hydrolase (FAAH) with an IC₅₀ of 12.4 nM. LY2183240 inactivates FAAH by carbamylation of the enzyme's serine nucleophile. LY2183240 also inhibits several other brain serine hydrolases with IC₅₀s of 5.3, 0.09, 8.2 nM for MAG lipase, bh6 and KIAA1363, respectively .

HY-W250129

2,3,4,5-Tetrafluorobenzoyl chloride	Biochemical Assay Reagents	Others
2,3,4,5-Tetrafluorobenzoyl chloride is a fluorinated organic compound that belongs to the class of benzoyl chlorides. It is a colorless liquid with a pungent smell and is mainly used as an intermediate in the synthesis of various pharmaceutical and pesticide compounds. 2,3,4,5-Tetrafluorobenzoyl chloride is an acylating agent that can react with a variety of nucleophiles, including amines, alcohols, and thiols, to form amides, esters, or thioesters, respectively. Its unique fluorine-containing structure can impart desired properties to target molecules, such as increased lipophilicity or increased stability against metabolic degradation. However, due to its high reactivity and potential health hazards, proper safety measures and handling procedures must be followed when using this compound.

HY-126637

Marasmic acid	Bacterial Fungal	Infection
Marasmic acid is a sesquiterpenoid with unsaturated dialdehyde functionality, first isolated from the Basidiomycete Marasmus conigenus. Marasmic acid has antibacterial, antifungal, cytotoxic and mutagenic activities, and its broad-spectrum activity is related to the α,β-unsaturated aldehyde group. However, its detailed biological mechanism of action has not been clarified. Previous studies have suggested that marasmic acid may exert its effects by reacting with endogenous nucleophiles or forming pyrrole derivatives. This study found that marasmic acid interferes with the membrane sensor histidine kinase MoSln1p of M. oryzae, superactivates the HOG pathway and causes cell death, indicating that its mechanism of action is different from other unsaturated dialdehyde sesquiterpenoids.

Cat. No.	Product Name

HY-L915

Lysine Focused Covalent Fragment Library	445 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

445 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.

Cat. No.	Product Name	Type

HY-112526

Thiofluor 623	Fluorescent Dyes/Probes
Thiofluor 623 (Compound 3) is a fluorescent turn-on probe that can be used for the selective sensing and bioimaging of thiols. Thiofluor 623 displays excellent immunity to interference from nitrogen and oxygen nucleophiles. Thiofluor 623 is essentially nonfluorescent in the absence of thiols, which cleave the probe and release the red-emissive donor-acceptor fluorophore (Ex=563 nm, Em=623 nm) .

Cat. No.	Product Name	Type

HY-126944

2-Aminobenzanilide 2-Amino-N-phenylbenzamide	Indicators
2-Aminobenzamide is a neutral and stable compound used as fluorescent tag, numerously in Glycan analysis. 2-aminobenzamide acts as the starting material for several important reactions like Bargellini reaction as an competent ambident nucleophile. Specifically 2-aminobenzamide and its derivatives are used in the blood coagulation cascade .

HY-W250129

2,3,4,5-Tetrafluorobenzoyl chloride	Biochemical Assay Reagents
2,3,4,5-Tetrafluorobenzoyl chloride is a fluorinated organic compound that belongs to the class of benzoyl chlorides. It is a colorless liquid with a pungent smell and is mainly used as an intermediate in the synthesis of various pharmaceutical and pesticide compounds. 2,3,4,5-Tetrafluorobenzoyl chloride is an acylating agent that can react with a variety of nucleophiles, including amines, alcohols, and thiols, to form amides, esters, or thioesters, respectively. Its unique fluorine-containing structure can impart desired properties to target molecules, such as increased lipophilicity or increased stability against metabolic degradation. However, due to its high reactivity and potential health hazards, proper safety measures and handling procedures must be followed when using this compound.

2,3,4,5-Tetrafluorobenzoyl chloride

Biochemical Assay Reagents

2,3,4,5-Tetrafluorobenzoyl chloride is a fluorinated organic compound that belongs to the class of benzoyl chlorides. It is a colorless liquid with a pungent smell and is mainly used as an intermediate in the synthesis of various pharmaceutical and pesticide compounds. 2,3,4,5-Tetrafluorobenzoyl chloride is an acylating agent that can react with a variety of nucleophiles, including amines, alcohols, and thiols, to form amides, esters, or thioesters, respectively. Its unique fluorine-containing structure can impart desired properties to target molecules, such as increased lipophilicity or increased stability against metabolic degradation. However, due to its high reactivity and potential health hazards, proper safety measures and handling procedures must be followed when using this compound.

Cat. No.	Product Name	Target	Research Area

HY-W009177

S-Methylglutathione	Glyoxalase (GLO)	Others
S-Methylglutathione is an S-substitued glutathione and a stronger *nucleophile* than GSH . S-Methylglutathione has inhibitory effect on glyoxalase 1 .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0548

α-Angelica lactone 2 Publications Verification	Natural Products Classification of Application Fields Source classification Dicerothamnus rhinocerotis Plants Umbelliferae Disease Research Fields Cancer	Glutathione S-transferase
α-Angelica lactone is a naturally occurring anticarcinogen and an vinylogous nucleophile. α-Angelica lactone can give the chiral δ-amino γ,γ-disubstituted butenolide carbonyl derivatives and exhibitselectrophilic trapping at the γ-carbon. α-Angelica lactone exerts strong chemoprotective effects by selective enhancement of glutathione-S-thansferase (GST) and UDP-glucononosyltransferase (UGT) detoxification enzymes .

HY-128429

Trans-2-Hexenal	Structural Classification Classification of Application Fields Leguminosae Ketones, Aldehydes, Acids Source classification Other Diseases Plants Phaseolus vulgaris Linn. Disease Research Fields	Endogenous Metabolite
Trans-2-Hexenal can be used for the determination of low-molecular-weight carbonyl compounds which are reactive with biological nucleophiles in biological samples .

HY-126637

Marasmic acid	Structural Classification Microorganisms Antibiotics Source classification Other Antibiotics	Bacterial Fungal
Marasmic acid is a sesquiterpenoid with unsaturated dialdehyde functionality, first isolated from the Basidiomycete Marasmus conigenus. Marasmic acid has antibacterial, antifungal, cytotoxic and mutagenic activities, and its broad-spectrum activity is related to the α,β-unsaturated aldehyde group. However, its detailed biological mechanism of action has not been clarified. Previous studies have suggested that marasmic acid may exert its effects by reacting with endogenous nucleophiles or forming pyrrole derivatives. This study found that marasmic acid interferes with the membrane sensor histidine kinase MoSln1p of M. oryzae, superactivates the HOG pathway and causes cell death, indicating that its mechanism of action is different from other unsaturated dialdehyde sesquiterpenoids.

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