threonine residue

By Targets:	Ser/Thr Protease (1) Apoptosis (4) Autophagy (4) Bacterial (1) Bcr-Abl (1) Biochemical Assay Reagents (2) Calcium Channel (1) CDK (1) Endogenous Metabolite (1) Ephrin Receptor (1) Isotope-Labeled Compounds (1) LRRK2 (1) NF-κB (4) PKC (1) Proteasome (4) Reference Standards (1) TREM receptor (4) Wnt (1) β-catenin (1)
By Research Areas:	Cancer (8) Metabolic Disease (1) Neurological Disease (1)

Targets Recommended: STK33 Microtubule‐associated serine/threonine kinase (MAST) Ser/Thr Kinase FASTK TSSK MASTL PASK/STK37 Ser/Thr Protease

Cat. No.	Nom du produit	Target	Áreas de investigación	Chemical Structure

HY-10227

Bortezomib 245+ Cited Publications PS-341; LDP-341; NSC 681239	Proteasome NF-κB Apoptosis Autophagy TREM receptor	Cancer
Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (K_i=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Bortezomib can be used for the study of multiple myeloma (MM) . Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs) .

HY-10227R

Bortezomib (Standard) PS-341 (Standard); LDP-341 (Standard); NSC 681239 (Standard)	Reference Standards Proteasome NF-κB Apoptosis Autophagy TREM receptor	Cancer
Bortezomib (Standard) is the analytical standard of Bortezomib. This product is intended for research and analytical applications. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (K_i=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Bortezomib can be used for the study of multiple myeloma (MM) . Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs) .

HY-P5979

LRRKtide	LRRK2	Neurological Disease
LRRKtide is a polypeptide substrate. LRRKtide is a specific phosphorylation substrate of LRRK2, a kinase associated with Parkinson's disease, and its phosphorylation site is a threonine residue. LRRKtide can be used for characterization of the catalytic properties of LRRK2, as well as studies on kinase activity and inhibition. LRRKtide is applicable to research related to Parkinson's disease .

HY-10227S

Bortezomib-d8 PS-341-d₈; LDP-341-d₈; NSC 681239-d₈	Isotope-Labeled Compounds Proteasome NF-κB Apoptosis Autophagy TREM receptor	Cancer
Bortezomib-d₈ is the deuterium labeled Bortezomib. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (K_i=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Bortezomib can be used for the study of multiple myeloma (MM) . Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs) .

HY-E70290

N-Acetylgalactosaminyltransferase 1 GALNT1	Endogenous Metabolite β-catenin Wnt	Cancer
N-Acetylgalactosaminyltransferase 1 (GALNT1) is a glycosyltransferase that initiates mucin-type O-glycosylation by transferring α-GalNAc from UDP-GalNAc to serine (Ser) or threonine (Thr) residues in proteins. Overexpression of N-Acetylgalactosaminyltransferase 1 in gastric cancer can promote abnormal O-glycosylation of CD44, thereby activating the Wnt/β-catenin signaling pathway and regulating the malignant behavior of gastric cancer cells. Additionally, N-Acetylgalactosaminyltransferase 1 plays a crucial role in cancer growth and metastasis by modifying the O-glycosylation of various glycoproteins, such as mucin (MUC1), osteopontin (OPN), matrix metalloproteinase-14 (MMP14), and integrin α3 .

HY-10227G

Bortezomib PS-341; LDP-341; NSC 681239	Proteasome NF-κB Apoptosis Autophagy TREM receptor	Cancer
Bortezomib (GMP) (PS-341 (GMP)) is Bortezomib (HY-10227) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (K_i=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Bortezomib can be used for the study of multiple myeloma (MM) . Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs) .

HY-P5444

Drosocin	Bacterial	Others
Drosocin is a biological active peptide. (Drosocin is a 19-mer cationic antimicrobial peptide from Drosophila melanogaster. In Drosophila native drosocin carries a disaccharide moiety attached to a threonine residue in mid-chain position. This synthetic drosocin peptide of identical amino acid sequence without the disaccharide has an activity several times lower than the native compound.)

HY-160478

GNF-6	Bcr-Abl	Cancer
GNF-6 (Compound 14) inhibits the gatekeeper threonine residue mutation of BCR-ABL-T315I with IC₅₀s of 0.25 μM, 0.09 μM and 0.590 μM for c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants, respectively. GNF-6, an ATP competitive inhibitor, disrupts the assembly of the hydrophobic spine (a network of hydrophobic interactions), thereby locking the kinase in an inactive ‘DFG-out’ conformation .

HY-P5954

PLTX-II	Calcium Channel	Others
PLTX-II is a calcium channel blocker. PLTX-II has a 44-residue peptide containing ten Cys residues and an O-palmitoylated threonine amide at the carboxy-terminus .

HY-E70691

CLK1 Recombinant Human Active Protein Kinase	CDK	Cancer
CLK1 is one of the dual specificity kinases and is the founding member of the 'LAMMER' family of kinases. CLK1 activity is positively regulated by phosphorylation on either tyrosine residues or serine/threonine residues, and is negatively regulated by steric constraints mediated by the N-terminal domain, as well as, by phosphorylation on a subset of serine/threonine residues within the catalytic domain. CLK1 Recombinant Human Active Protein Kinase is a recombinant CLK1 protein that can be used to study CLK1-related functions .

HY-E70568

Protease (O-glycan Cleaving)	Ser/Thr Protease	Others
Protease (O-glycan Cleaving) is recombinantly expressed from E.coli and contains a His tag. Protease (O-glycan Cleaving) is an O-glycan-dependent protease that digests proteins carrying mucin-type O-glycans, including sialylated substrates, glycosylated Ser and Thr residues at the N terminus. Protease (O-glycan Cleaving) digests a variety of O-glycan structures, including sialylated glycosylated core 1 and core 2 structures and Tn antigen. Protease (O-glycan Cleaving) does not digest terminally modified serine or threonine residues, nor does it digest N-glycosylation sites on glycoproteins.

HY-E70569

α-N-acetylgalactosidase	Biochemical Assay Reagents	Others
α-N-acetylgalactosidase (EC 3.2.1.4) is a highly specific exoglycosidase that efficiently hydrolyzes α-N-acetylgalactosamine (GalNAc) linked to serine or threonine residues in glycoproteins (Tn antigen). α-N-acetylgalactosidase shows activity against α 1-3 linked terminal GalNAc . α-N-acetylgalactosidase is suitable for use in the pH range of 6.0-7.6 and does not require cofactors or special buffer systems.

HY-E71300

β-Galactoside α-2,3-sialyltransferase	Biochemical Assay Reagents	Others
The acceptor for β-galactoside α-2,3-sialyltransferase (EC 2.4.99.4) is Galβ1,3GalNAc-R, where R is H, a threonine or serine residue in a glycoprotein, or a glycolipid. Lactose can also serve as an acceptor.

HY-E70949

Protein Kinase C,Rat	PKC	Metabolic Disease
Protein Kinase C,Rat (EC 2.7.1.37) is a family of protein kinase enzymes that are involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and threonine amino acid residues on these proteins. Protein Kinase C in turn are activated by signals such as increases in the concentration of diacylglycerol (DAG) or calcium ions (Ca ²⁺).

HY-10654

EphB4-IN-2	Ephrin Receptor	Cancer
EphB4-IN-2 is a tyrosine kinase inhibitor targeting the Eph family and Src family. EphB4-IN-2 binds to the ATP-binding site of the kinase domain of EphB4, and exhibits high affinity for tyrosine kinases with threonine as the gatekeeper residue, such as Abl, Lck and Src. EphB4-IN-2 can be used in research related to tumor-associated angiogenesis .

Cat. No.	Nom du produit

HY-L164

Serine/Threonine Kinase Inhibitor Library	2,162 compounds
Protein serine/threonine kinases (PSKs) are protein kinases that use ATP as a high-energy donor molecule to transfer phosphate groups to serine/threonine residues of target protein. As an important signal transduction regulator, serine/threonine kinases can affect the function of target proteins by disrupting enzyme activity or binding of target proteins to other proteins. Serine/threonine kinases are involved in the regulation of immune response, cell proliferation, differentiation, apoptosis and other physiological processes. Serine/threonine kinase inhibitors are an important class of compounds that have been widely studied in cancer, chronic inflammation, autoimmune diseases, aging and other diseases. MCE designs a unique collection of 2,162 serine/threonine kinase inhibitors, mainly targeting the receptor PKA, Akt, PKC, MAPK/ERK, etc, which is an effective tool for development and research of anti-cancer, anti-chronic inflammatory diseases, anti-autoimmune diseases and anti-aging compounds.

Serine/Threonine Kinase Inhibitor Library

2,162 compounds

Protein serine/threonine kinases (PSKs) are protein kinases that use ATP as a high-energy donor molecule to transfer phosphate groups to serine/threonine residues of target protein. As an important signal transduction regulator, serine/threonine kinases can affect the function of target proteins by disrupting enzyme activity or binding of target proteins to other proteins. Serine/threonine kinases are involved in the regulation of immune response, cell proliferation, differentiation, apoptosis and other physiological processes. Serine/threonine kinase inhibitors are an important class of compounds that have been widely studied in cancer, chronic inflammation, autoimmune diseases, aging and other diseases.

MCE designs a unique collection of 2,162 serine/threonine kinase inhibitors, mainly targeting the receptor PKA, Akt, PKC, MAPK/ERK, etc, which is an effective tool for development and research of anti-cancer, anti-chronic inflammatory diseases, anti-autoimmune diseases and anti-aging compounds.

HY-L914

Serine/Threonine Focused Covalent Fragment Library	3,208 compounds
In the research of covalent inhibitors targeting serine and threonine, scientists have found that the nucleophilicity of these hydroxyl groups is significantly enhanced due to the influence of their surrounding environment. This results in higher activity during catalytic reactions. Aspirin, which targets the non-catalytic domain serine (Ser529 in human COX1) of cyclooxygenase, exerts its anti-inflammatory effect through covalent binding. β-lactam antibiotics, which targets the catalytic domain serine of penicillin-binding proteins, interferes with bacterial cell wall synthesis. 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 3,300 fragment molecules which can target serine and threonine residues and can be used for fragment-based covalent drug discovery.

Serine/Threonine Focused Covalent Fragment Library

3,208 compounds

In the research of covalent inhibitors targeting serine and threonine, scientists have found that the nucleophilicity of these hydroxyl groups is significantly enhanced due to the influence of their surrounding environment. This results in higher activity during catalytic reactions. Aspirin, which targets the non-catalytic domain serine (Ser529 in human COX1) of cyclooxygenase, exerts its anti-inflammatory effect through covalent binding. β-lactam antibiotics, which targets the catalytic domain serine of penicillin-binding proteins, interferes with bacterial cell wall synthesis.

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 3,300 fragment molecules which can target serine and threonine residues and can be used for fragment-based covalent drug discovery.

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.	Nom du produit	Type

HY-10227G

Bortezomib PS-341; LDP-341; NSC 681239	Fluorescent Dyes
Bortezomib (GMP) (PS-341 (GMP)) is Bortezomib (HY-10227) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (K_i=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Bortezomib can be used for the study of multiple myeloma (MM) . Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs) .

Bortezomib

PS-341; LDP-341; NSC 681239

Fluorescent Dyes

Bortezomib (GMP) (PS-341 (GMP)) is Bortezomib (HY-10227) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (K_i=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Bortezomib can be used for the study of multiple myeloma (MM) . Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs) .

Cat. No.	Nom du produit	Type

HY-10227G

Bortezomib PS-341; LDP-341; NSC 681239	Biochemical Assay Reagents
Bortezomib (GMP) (PS-341 (GMP)) is Bortezomib (HY-10227) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (K_i=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Bortezomib can be used for the study of multiple myeloma (MM) . Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs) .

Bortezomib

PS-341; LDP-341; NSC 681239

Biochemical Assay Reagents

Bortezomib (GMP) (PS-341 (GMP)) is Bortezomib (HY-10227) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (K_i=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Bortezomib can be used for the study of multiple myeloma (MM) . Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs) .

Cat. No.	Nom du produit	Target	Research Area

HY-P5979

LRRKtide	LRRK2	Neurological Disease
LRRKtide is a polypeptide substrate. LRRKtide is a specific phosphorylation substrate of LRRK2, a kinase associated with Parkinson's disease, and its phosphorylation site is a threonine residue. LRRKtide can be used for characterization of the catalytic properties of LRRK2, as well as studies on kinase activity and inhibition. LRRKtide is applicable to research related to Parkinson's disease .

HY-P5444

Drosocin	Bacterial	Others
Drosocin is a biological active peptide. (Drosocin is a 19-mer cationic antimicrobial peptide from Drosophila melanogaster. In Drosophila native drosocin carries a disaccharide moiety attached to a threonine residue in mid-chain position. This synthetic drosocin peptide of identical amino acid sequence without the disaccharide has an activity several times lower than the native compound.)

HY-P5954

PLTX-II	Calcium Channel	Others
PLTX-II is a calcium channel blocker. PLTX-II has a 44-residue peptide containing ten Cys residues and an O-palmitoylated threonine amide at the carboxy-terminus .

Cat. No.	Nom du produit

HY-KE7057

O-Glycosidase
O-Glycosidase is highly specific and can release Galβ1-3GalNAc from serine, threonine residues or as part of a glycopeptide or glycoprotein. Applied to glycoprotein biosynthesis analysis, O-glycan bioactive protein O-glycosylation detection and binding site analysis.

Cat. No.	Nom du produit	Chemical Structure

HY-10227S

Bortezomib-d8
Bortezomib-d₈ is the deuterium labeled Bortezomib. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (K_i=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Bortezomib can be used for the study of multiple myeloma (MM) . Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs) .

Bortezomib-d8

Bortezomib-d₈ is the deuterium labeled Bortezomib. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (K_i=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Bortezomib can be used for the study of multiple myeloma (MM) . Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs) .

Targets Recommended: STK33 Microtubule‐associated serine/threonine kinase (MAST) Ser/Thr Kinase FASTK TSSK MASTL PASK/STK37 Ser/Thr Protease

Cat. No.	Nom du produit	Target	Áreas de investigación	Chemical Structure

HY-10227G

Bortezomib PS-341; LDP-341; NSC 681239	Proteasome NF-κB Apoptosis Autophagy TREM receptor	Cancer
Bortezomib (GMP) (PS-341 (GMP)) is Bortezomib (HY-10227) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (K_i=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Bortezomib can be used for the study of multiple myeloma (MM) . Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs) .

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
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