Search Result

Pathways Recommended:	Protein Tyrosine Kinase/RTK

Results for "

tyrosine residue

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Btk (1) Amino Acid Derivatives (2) EGFR (3) Fluorescent Dye (1) Isotope-Labeled Compounds (2) Kinesin (1) Microtubule/Tubulin (1) p38 MAPK (3) Parasite (1)
By Research Areas:	Cancer (4) Endocrinology (4) Infection (1) Neurological Disease (6)

Inhibitors & Agonists

Screening Libraries

Peptides

Isotope-Labeled Compounds

Targets Recommended: Btk Syk DYRK Pyk2 BRK FAK FLT3 Anaplastic lymphoma kinase (ALK)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-141898

Biotin-4-aminophenol	Fluorescent Dye	Others
Biotin-4-aminophenol is a biotin-phenol analog. Biotin-4-aminophenol generates free radicals and conjugates to tyrosine residues in proteins more efficiently and selectively than the previously reported BP1 .

HY-103441

JNJ28871063 hydrochloride	EGFR	Cancer
JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC₅₀ values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2 .

HY-19730

Olmutinib Maximum Cited Publications 9 Publications Verification HM61713; BI 1482694	EGFR	Cancer
Olmutinib (HM61713; BI-1482694) is an orally active and irreversible third *EGFR tyrosine* kinase** inhibitor that binds to a cysteine residue near the kinase domain. Olmutinib is used for NSCLC .

HY-P4106A

Tat-GluR23Y, scrambled TFA 1 Publications Verification	Amino Acid Derivatives	Neurological Disease
Tat-GluR23Y, scrambled TFA is the scrambled peptide of Tat-GluR23Y (HY-P2259). Tat-GluR23Y is a synthetic peptide containing tyrosine residues that inhibit AMPAR endocytosis and is effective in the research of long-term depression (LTD) .

HY-B0558

Carbimazole	p38 MAPK	Neurological Disease Endocrinology
Carbimazole is an orally active antithyroid agent which rapidly converts to Methimazole after absorption and prevents thyroid peroxidase enzyme from iodinating and coupling the tyrosine residues on thyroglobulin, hence reducing the production of thyroxine. Carbimazole also displays anti-inflammatory and neuronal-protective activities, suggesting its application for hyperthyroidism and neurological research .

HY-P10609

Btk substrate peptide	Btk	Others
Btk substrate peptide is a peptide substrate corresponding to residues 217-229 of human Bruton’s tyrosine kinase (Btk), of which the tyrosine at residue 223 is the major autophosphorylation site of Btk. Btk substrate peptide is used as a substrate in in vitro kinase assays to evaluate the activity of Btk or other tyrosine kinases .

HY-19730A

Olmutinib hydrochloride HM61713 hydrochloride; BI 1482694 hydrochloride	EGFR	Cancer
Olmutinib hydrochloride is an orally active and irreversible third *EGFR tyrosine* kinase** inhibitor that binds to a cysteine residue near the kinase domain. Olmutinib hydrochloride is used for NSCLC .

HY-P4106

Tat-GluR23Y, scrambled	Amino Acid Derivatives	Neurological Disease
Tat-GluR23Y, scrambled is the scrambled peptide of Tat-GluR23Y (HY-P2259). Tat-GluR23Y is a synthetic peptide containing tyrosine residues that inhibit AMPAR endocytosis and is effective in the research of long-term depression (LTD) .

HY-116870

Vamidothion	Parasite	Infection
Vamidothion is a polar organophosphorus insecticide and acaricide with biological activity against insects and mites. Vamidothion is degraded by human serum albumin (HSA) and promotes adduct formation with tyrosine residues. The phosphate amino acid adducts formed after the reaction of vamidothion with HSA are detected by liquid chromatography quadrupole-Orbitrap mass spectrometry. The metabolites of vamidothion can be used in forensic toxicology to help determine deaths caused by organophosphorus poisoning .

HY-B0558S

Carbimazole-d5	Isotope-Labeled Compounds	Neurological Disease Endocrinology
Carbimazole-d₅ is deuterium labeled Carbimazole. Carbimazole is an orally active antithyroid agent which rapidly converts to Methimazole after absorption and prevents thyroid peroxidase enzyme from iodinating and coupling the tyrosine residues on thyroglobulin, hence reducing the production of thyroxine. Carbimazole also displays anti-inflammatory and neuronal-protective activities, suggesting its application for hyperthyroidism and neurological research .

HY-W744953

Carbimazole-d3	Isotope-Labeled Compounds p38 MAPK	Neurological Disease Endocrinology
Carbimazole-d₃ is deuterium labeled Carbimazole. Carbimazole is an orally active antithyroid agent which rapidly converts to Methimazole after absorption and prevents thyroid peroxidase enzyme from iodinating and coupling the tyrosine residues on thyroglobulin, hence reducing the production of thyroxine. Carbimazole also displays anti-inflammatory and neuronal-protective activities, suggesting its application for hyperthyroidism and neurological research .

HY-B0558R

Carbimazole (Standard)	p38 MAPK	Neurological Disease Endocrinology
Carbimazole (Standard) is the analytical standard of Carbimazole. This product is intended for research and analytical applications. Carbimazole is an orally active antithyroid agent which rapidly converts to Methimazole after absorption and prevents thyroid peroxidase enzyme from iodinating and coupling the tyrosine residues on thyroglobulin, hence reducing the production of thyroxine. Carbimazole also displays anti-inflammatory and neuronal-protective activities, suggesting its application for hyperthyroidism and neurological research .

HY-110208

BRD9876 1 Publications Verification	Kinesin Microtubule/Tubulin	Cancer
BRD9876 is the “rigor” inhibitor that locks kinesin-5 (Eg5) in a state with enhanced microtubules (MTs) binding, leading to bundling and stabilization of MTs. BRD9876 interacts with the tyrosine 104 residue that is part of the α4-α6 allosteric binding pocket. BRD9876 specifically targets microtubule-bound Eg5 and selectively inhibits myeloma over CD34 cells. BRD9876 has the potential for multiple myeloma (MM) research .

Cat. No.	Product Name

HY-L913

Tyrosine Focused Covalent Fragment Library	124 compounds
Recently, significant advancements in tyrosine-targeting electrophiles have primarily occurred in the field of protein-protein interactions (PPIs), where cysteine residues are often underrepresented and novel chemistries are needed to address these interfaces. In this context, tyrosines are frequently more accessible compared to more buried binding sites. Moreover, they are commonly found at "hot spots," which are functional epitopes of PPIs, with 12.3% of the residues consisting of tyrosines. This prevalence is likely due to the hydrophobic nature of tyrosine, its ability to participate in aromatic π-interactions, and its capacity for hydrogen bonding. Beyond PPIs, some progress has also been made in covalent tyrosine targeting in other areas where more commonly addressed side chains are lacking. Even though tyrosine has a slightly lower pKa value compared to the protonated lysine side chain (approximately 10 vs. 10.5 for the unprotected amino acid side chains), significantly less progress has been made in the development of tyrosine-targeted covalent ligands compared to lysine. This is likely due to the reduced flexibility of the tyrosine side chain and the greater steric hindrance of its hydroxy group, which makes it more challenging to adopt suitable reaction geometries. 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 124 fragment molecules which can target tyrosine residue and can be used for fragment-based covalent drug discovery.

Tyrosine Focused Covalent Fragment Library

124 compounds

Recently, significant advancements in tyrosine-targeting electrophiles have primarily occurred in the field of protein-protein interactions (PPIs), where cysteine residues are often underrepresented and novel chemistries are needed to address these interfaces. In this context, tyrosines are frequently more accessible compared to more buried binding sites. Moreover, they are commonly found at "hot spots," which are functional epitopes of PPIs, with 12.3% of the residues consisting of tyrosines. This prevalence is likely due to the hydrophobic nature of tyrosine, its ability to participate in aromatic π-interactions, and its capacity for hydrogen bonding. Beyond PPIs, some progress has also been made in covalent tyrosine targeting in other areas where more commonly addressed side chains are lacking. Even though tyrosine has a slightly lower pKa value compared to the protonated lysine side chain (approximately 10 vs. 10.5 for the unprotected amino acid side chains), significantly less progress has been made in the development of tyrosine-targeted covalent ligands compared to lysine. This is likely due to the reduced flexibility of the tyrosine side chain and the greater steric hindrance of its hydroxy group, which makes it more challenging to adopt suitable reaction geometries.

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

HY-L016

Protein Tyrosine Kinase Compound Library	1,193 compounds
Protein tyrosine kinases (PTKs) are key signaling molecules and important drug targets. Two classes of PTKs are present in cells: the transmembrane receptor PTKs (RTKs) and the nonreceptor PTKs. The RTK family includes the receptors for insulin and for many growth factors, such as EGFR, FGFR, PDGFR, VEGFR, and NGFR. RTKs are transmembrane glycoproteins that are activated by the binding of their ligands, and they transduce the extracellular signal to the cytoplasm by phosphorylating tyrosine residues on the receptors themselves (autophosphorylation) and on downstream signaling proteins. Their principal functions of PTKs involve the regulation of multicellular aspects of the organism. Cell to cell signals concerning growth, differentiation, adhesion, motility, and death are frequently transmitted through tyrosine kinases. In humans, tyrosine kinases have been demonstrated to play significant roles in the development of many disease states, including diabetes and cancers. MCE designs a unique collection of 1,193 compounds that act as a useful tool for PTKs-related drug screening and disease research.

Protein Tyrosine Kinase Compound Library

1,193 compounds

Protein tyrosine kinases (PTKs) are key signaling molecules and important drug targets. Two classes of PTKs are present in cells: the transmembrane receptor PTKs (RTKs) and the nonreceptor PTKs. The RTK family includes the receptors for insulin and for many growth factors, such as EGFR, FGFR, PDGFR, VEGFR, and NGFR. RTKs are transmembrane glycoproteins that are activated by the binding of their ligands, and they transduce the extracellular signal to the cytoplasm by phosphorylating tyrosine residues on the receptors themselves (autophosphorylation) and on downstream signaling proteins. Their principal functions of PTKs involve the regulation of multicellular aspects of the organism. Cell to cell signals concerning growth, differentiation, adhesion, motility, and death are frequently transmitted through tyrosine kinases. In humans, tyrosine kinases have been demonstrated to play significant roles in the development of many disease states, including diabetes and cancers.

MCE designs a unique collection of 1,193 compounds that act as a useful tool for PTKs-related drug screening and disease research.

Cat. No.	Product Name	Target	Research Area

HY-P4106A

Tat-GluR23Y, scrambled TFA 1 Publications Verification	Amino Acid Derivatives	Neurological Disease
Tat-GluR23Y, scrambled TFA is the scrambled peptide of Tat-GluR23Y (HY-P2259). Tat-GluR23Y is a synthetic peptide containing tyrosine residues that inhibit AMPAR endocytosis and is effective in the research of long-term depression (LTD) .

HY-P10609

Btk substrate peptide	Btk	Others
Btk substrate peptide is a peptide substrate corresponding to residues 217-229 of human Bruton’s tyrosine kinase (Btk), of which the tyrosine at residue 223 is the major autophosphorylation site of Btk. Btk substrate peptide is used as a substrate in in vitro kinase assays to evaluate the activity of Btk or other tyrosine kinases .

HY-P4106

Tat-GluR23Y, scrambled	Amino Acid Derivatives	Neurological Disease
Tat-GluR23Y, scrambled is the scrambled peptide of Tat-GluR23Y (HY-P2259). Tat-GluR23Y is a synthetic peptide containing tyrosine residues that inhibit AMPAR endocytosis and is effective in the research of long-term depression (LTD) .

Cat. No.	Product Name	Chemical Structure

HY-B0558S

Carbimazole-d5
Carbimazole-d₅ is deuterium labeled Carbimazole. Carbimazole is an orally active antithyroid agent which rapidly converts to Methimazole after absorption and prevents thyroid peroxidase enzyme from iodinating and coupling the tyrosine residues on thyroglobulin, hence reducing the production of thyroxine. Carbimazole also displays anti-inflammatory and neuronal-protective activities, suggesting its application for hyperthyroidism and neurological research .

Carbimazole-d5

Carbimazole-d₅ is deuterium labeled Carbimazole. Carbimazole is an orally active antithyroid agent which rapidly converts to Methimazole after absorption and prevents thyroid peroxidase enzyme from iodinating and coupling the tyrosine residues on thyroglobulin, hence reducing the production of thyroxine. Carbimazole also displays anti-inflammatory and neuronal-protective activities, suggesting its application for hyperthyroidism and neurological research .

HY-W744953

Carbimazole-d3
Carbimazole-d₃ is deuterium labeled Carbimazole. Carbimazole is an orally active antithyroid agent which rapidly converts to Methimazole after absorption and prevents thyroid peroxidase enzyme from iodinating and coupling the tyrosine residues on thyroglobulin, hence reducing the production of thyroxine. Carbimazole also displays anti-inflammatory and neuronal-protective activities, suggesting its application for hyperthyroidism and neurological research .

Carbimazole-d3

Carbimazole-d₃ is deuterium labeled Carbimazole. Carbimazole is an orally active antithyroid agent which rapidly converts to Methimazole after absorption and prevents thyroid peroxidase enzyme from iodinating and coupling the tyrosine residues on thyroglobulin, hence reducing the production of thyroxine. Carbimazole also displays anti-inflammatory and neuronal-protective activities, suggesting its application for hyperthyroidism and neurological research .

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