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Results for "

auto-phosphorylation

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (6) Anaplastic lymphoma kinase (ALK) (5) Antibiotic (1) Apoptosis (39) ATM/ATR (1) Aurora Kinase (4) Autophagy (18) Bacterial (3) Bcl-2 Family (3) Bcr-Abl (7) BCRP (1) BMX Kinase (1) Btk (3) c-Fms (2) c-Kit (8) Cadherin (2) CaMK (1) Caspase (4) Cdc42-binding kinase (1) CDK (2) Checkpoint Kinase (Chk) (2) Discoidin Domain Receptor (4) DNA-PK (1) Drug Derivative (1) Drug Metabolite (3) DYRK (2) EGFR (33) Endogenous Metabolite (1) Ephrin Receptor (3) ERK (7) FAK (6) FGFR (6) FLT3 (17) Fluorescent Dye (1) Fungal (3) GDNF Receptor (4) Hippo (MST) (1) IGF-1R (4) IKK (1) Insulin Receptor (2) Interleukin Related (4) IRE1 (11) Isotope-Labeled Compounds (8) JAK (5) Leukotriene Receptor (1) LRRK2 (3) MAP3K (3) MDM-2/p53 (1) MEK (2) MHC (1) Mitophagy (7) MMP (3) mRNA (2) NF-κB (1) Nucleoside Antimetabolite/Analog (1) Organoid (2) Orthopoxvirus (4) P2X Receptor (1) p38 MAPK (2) PAK (1) PARP (3) PDGFR (19) Phosphatase (2) PI3K (2) PKC (1) Prostaglandin Receptor (1) Raf (2) Reference Standards (14) RET (6) RIP kinase (2) ROS Kinase (1) Src (8) STAT (5) TGF-beta/Smad (1) TGF-β Receptor (7) TNF Receptor (1) VEGFR (14) YAP (1)
By Research Areas:	Cancer (120) Cardiovascular Disease (7) Endocrinology (5) Infection (12) Inflammation/Immunology (17) Metabolic Disease (9) Neurological Disease (18)
Click Chemistry:	Alkynes (1)
Oligonucleotides:	mRNA (2)

160

Inhibitors & Agonists

Screening Libraries

Peptides

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Oligonucleotides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10255A

Sunitinib 90+ Cited Publications SU 11248	VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis	Cancer
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC₅₀s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .

HY-13012

RepSox 20+ Cited Publications E-616452; SJN 2511	Organoid TGF-β Receptor	Metabolic Disease
RepSox (E-616452) is a potent and selective transforming growth factor-beta receptor I/activin like kinase 5 (TGF-β-RI/ALK5) inhibitor. RepSox inhibits ALK5 autophosphorylation with an IC₅₀ value of 4 nM. RepSox can be used for the research of obesity and associated metabolic diseases such as type 2 diabetes .

HY-50895

Gefitinib 195+ Cited Publications ZD1839	EGFR Autophagy Apoptosis	Cancer
Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC₅₀ of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC₅₀ of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .

HY-50896

Erlotinib 130+ Cited Publications CP-358774; NSC 718781; OSI-774	EGFR Autophagy	Cancer
Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC₅₀ of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC₅₀ of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer . Erlotinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-10255

Sunitinib Malate 90+ Cited Publications SU 11248 Malate	PDGFR VEGFR IRE1 Mitophagy Autophagy Apoptosis	Infection Inflammation/Immunology Cancer
Sunitinib (SU 11248) Malat is a multi-targeted receptor tyrosine kinase inhibitor with IC₅₀s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib Malat, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .

HY-13001

Quizartinib 40+ Cited Publications AC220	FLT3 Apoptosis PDGFR c-Kit	Cancer
Quizartinib (AC220) is an orally active, potent and selective FLT3 inhibitor. Quizartinib inhibits kinase activity of mutant-FLT3, -PDGFRA and -KIT isoforms and inhibits autophosphorylation. Quizartinib inhibits cellular proliferation, induces apoptosis in cancer cells. Quizartinib can be used for the research of cancer .

HY-12444

Y15 25+ Cited Publications FAK Inhibitor 14	FAK	Cancer
Y15 is a potent and specific inhibitor of focal adhesion kinase (FAK) that inhibits its autophosphorylation activity, decreases the viability of cancer cells, and blocks tumor growth.

HY-114258

LY3295668 3 Publications Verification AK-01	Aurora Kinase Apoptosis	Cancer
LY3295668 (AK-01) is a highly specific and orally active inhibitor of Aurora-A kinase with a K_i values for AurA and AurB of 0.8 nM and 1038 nM respectively. LY3295668 can effectively inhibit the autophosphorylation of AurA, induce mitotic arrest and apoptosis. LY3295668 avoids the formation of polyploids related to AurB inhibition. LY3295668 can be used for the study of small cell lung cancer .

HY-103248

Toyocamycin 5+ Cited Publications Vengicide	IRE1 Fungal Antibiotic Apoptosis CDK	Infection Cancer
Toyocamycin (Vengicide) is an adenosine analog produced by Streptomyces diastatochromogenes, acts as an XBP1 inhibitor. Toyocamycin blocks RNA synthesis and ribosome function, and induces apoptosis. Toyocamycin affects IRE1α-XBP1 pathway, and inhibits XBP1 mRNA cleavage with an IC₅₀ value of 80 nM with affecting IRE1α auto-phosphorylation. Toyocamycin specifically inhibits CDK9 with an IC₅₀ value of 79 nM .

HY-10367

Canertinib 5+ Cited Publications CI-1033; PD-183805	EGFR Orthopoxvirus	Infection Cancer
Canertinib (CI-1033;PD-183805) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC₅₀s of 7.4 and 9 nM. Canertinib is active against vaccinia virus respiratory infection in mice .

HY-13258A

NVP-BHG712 5+ Cited Publications BHG712	Ephrin Receptor	Cancer
NVP-BHG712 is an oral active EphB4 kinase autophosphorylation inhibitor, with IC₅₀ values of 3.3 nM and 3.0 nM for EphA2 and EphB4, respectively .

HY-122727

STL127705 5+ Cited Publications	DNA-PK Apoptosis	Cancer
STL127705 (Compound L) is a potent Ku 70/80 heterodimer protein inhibitor with an IC₅₀ of 3.5 μM. STL127705 interferes the binding of Ku70/80 to DNA and by inhibits the activation of the DNA-PKCS kinase. STL127705 shows antiproliferative and anticancer activity. STL127705 induces apoptosis .

HY-50895A

Gefitinib hydrochloride 195+ Cited Publications ZD-1839 hydrochloride	EGFR	Cancer
Gefitinib hydrochloride (ZD1839 hydrochloride) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC₅₀ of 33 nM. Gefitinib hydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC₅₀ of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib hydrochloride also induces autophagy. Gefitinib hydrochloride has antitumour activity .

HY-156618

Irpagratinib ABSK011	FGFR	Cancer
Irpagratinib (ABSK011) is an orally active FGFR4 inhibitor (IC₅₀<10 nM). Irpagratinib inhibits FGFR4 autophosphorylation and blocks signaling from FGFR4 to downstream pathway activation. Irpagratinib has shown high exposure in PK studies in mice, rats, and dogs, and also demonstrated antitumor activity in a subcutaneous xenograft tumor model .

HY-101957

AG 1295 4 Publications Verification	PDGFR	Cardiovascular Disease
AG 1295 is a selective platelet-derived growth factor receptor (PDGFR) tyrosine-kinase inhibitor. AG1295 abolishes autophosphorylation of the PDGFR whereas not affects the autophosphorylation of the EGF receptor .

HY-15002

AST 487 5 Publications Verification NVP-AST 487	RET FLT3 VEGFR c-Kit Bcr-Abl	Cancer
AST 487 is a RET kinase inhibitor with IC₅₀ of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC₅₀ of 520 nM.

HY-17537

APY29 10+ Cited Publications	IRE1	Cancer
APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC₅₀ of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain .

HY-15841

CEP-37440	Anaplastic lymphoma kinase (ALK) FAK	Cancer
CEP-37440 is a potent, orally active dual FAK/ALK inhibitor with IC₅₀ values of 2.3 nM and 3.5 nM for FAK and ALK, respectively. CEP-37440 decreases the cell proliferation by blocking the autophosphorylation kinase activity of FAK1 (Tyr 397) .

HY-10367A

Canertinib dihydrochloride 5+ Cited Publications CI-1033 dihydrochloride; PD-183805 dihydrochloride	EGFR Orthopoxvirus	Infection Cancer
Canertinib dihydrochloride (CI-1033 dihydrochloride) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC₅₀s of 7.4 and 9 nM. Canertinib dihydrochloride is active against vaccinia virus respiratory infection in mice .

HY-15480

NSC 42834 3 Publications Verification JAK2 Inhibitor V; Z3	JAK	Cancer
NSC 42834 (JAK2 Inhibitor V), a novel specific inhibitor of Jak2, inhibits Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner but was not cytotoxic to cells at concentrations that inhibited kinase activity.

HY-12282

GNE-9605	LRRK2	Neurological Disease
GNE-9605 is a potent, orally active, selective Leucine-rich repeat kinase 2 (LRRK2) inhibitor with an IC₅₀ value of 18.7 nM. GNE-9605 inhibits LRRK2 Ser1292 autophosphorylation. GNE-9605 can be used in research of Parkinson's disease (PD) .

HY-W062835

CGP77675	Src	Cancer
CGP77675 is an orally active and potent inhibitor of Src family kinases. CGP77675 inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC₅₀s of 5-20 and 40 nM, respectively), and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC₅₀s of 5-20, 40, 20, 150, 1000, 310, and 290 nM, respectively. Anticancer activity .

HY-145574

Iruplinalkib WX-0593	Anaplastic lymphoma kinase (ALK) ROS Kinase BCRP Akt ERK STAT	Cancer
Iruplinalkib (WX-0593) is an orally active and selective ALK/ROS1 inhibitor. Iruplinalkib can effectively inhibit tyrosine autophosphorylation of ALK and mutant ALK, EGFR, with the IC₅₀ between 5.38 and 16.74 nM. Iruplinalkib is also a suppressive agent of the transporter MATE1, MATE2K, P-gp and BCRP. Iruplinalkib can be used in the study of non-small cell lung cancer .

HY-10327

GW-6604	TGF-β Receptor	Metabolic Disease
GW-6604 is an ALK5 inhibitor with an IC₅₀ value of 140 nM for inhibiting its autophosphorylation, and can be used in the study of liver fibrosis .

HY-112198

AZ31	ATM/ATR	Cancer
AZ31 is a a potent, highly selective, and orally active ATM inhibitor with an IC₅₀ of <1.2 nM for ATM enzyme, and an IC₅₀ of 46 nM for ATM in cell. AZ31 shows excellent selectivity over ATR (>500-fold) and excellent PIKK-family selectivity and pan-kinase selectivity. AZ31 is a potent radiosensitizer in vitro, it can be used for the research of cancer .

HY-125203

PV-1019 2 Publications Verification NSC 744039	Checkpoint Kinase (Chk)	Cancer
PV-1019 (NSC 744039) is a potent, selective Chk2 inhibitor with an IC₅₀ value of 24 nM. PV-1019 inhibits the Topotecan (HY-13768)-induced Chk2 autophosphorylation. PV-1019 inhibits IR-induced apoptosis .

HY-14217

Quizartinib dihydrochloride 40+ Cited Publications AC220 dihydrochloride	FLT3 Apoptosis PDGFR c-Kit	Cancer
Quizartinib (AC220) dihydrochloride is an orally active, potent and selective FLT3 inhibitor. Quizartinib dihydrochloride inhibits kinase activity of mutant-FLT3, -PDGFRA and -KIT isoforms and inhibits autophosphorylation. Quizartinib dihydrochloride inhibits cellular proliferation, induces apoptosis in cancer cells. Quizartinib dihydrochloride can be used for the research of cancer .

HY-13905

Flumatinib mesylate 3 Publications Verification HHGV678 mesylate	Bcr-Abl c-Kit PDGFR	Cancer
Flumatinib (HHGV678) mesylate is an orally active and selective inhibitor of Bcr-Abl. Flumatinib mesylate inhibits c-Abl, PDGFRβ and c-Kit with IC₅₀ values of 1.2, 307.6 and 665.5 nM, respectively. Flumatinib mesylate inhibits Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation. Flumatinib mesylate inhibits tumor growth in chronic myelogenous leukemia model .

HY-133669

DDR1-IN-5	Discoidin Domain Receptor	Cancer
DDR1-IN-5 is a selective Discoidin Domain Receptor family, member 1 (DDR1) inhibitor with an IC₅₀ of 7.36 nM. DDR1-IN-5 inhibits auto-phosphorylation DDR1b (Y513) with an IC₅₀ of 4.1 nM. DDR1-IN-5 has anti-cancer activity . DDR1-IN-5 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-133670

DDR1-IN-6	Discoidin Domain Receptor	Cancer
DDR1-IN-6 is a selective Discoidin Domain Receptor family, member 1 (DDR1) inhibitor with an IC₅₀ of 9.72 nM. DDR1-IN-6 inhibits auto-phosphorylation DDR1b (Y513) with an IC₅₀ of 9.7 nM. DDR1-IN-6 has anti-cancer activity . DDR1-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-139481

TL-895 1 Publications Verification	Btk BMX Kinase Interleukin Related TNF Receptor	Neurological Disease Inflammation/Immunology Cancer
TL-895 is a potent, orally active, ATP-competitive, and highly selective irreversible BTK inhibitor. TL-895 is active against recombinant BTK (average IC₅₀: 1.5 nM) and inhibits only three additional kinases BLK, BMX (IC₅₀ = 1.6 nM) and TXK with IC₅₀ within tenfold of BTK activity. TL-895 inhibits BTK auto-phosphorylation at the Y223 phosphorylation site (IC₅₀: 1-10 nM). The TL-895 effectively inhibits the production of inflammatory factors such as IL-8, IL-1β, MCP-1 and TNF-α by monocytes or macrophages, and reduces the chemotactic migration of MF cells towards SDF-1. TL-895 is used be for studies of chronic lymphocytic leukemia (CLL), myelofibrosis (MF), and B-cell malignancies .

HY-103443

HKI-357	EGFR	Cancer
HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 with IC₅₀s of 34 nM and 33 nM, respectively. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation .

HY-114173

DDR1-IN-4	Discoidin Domain Receptor	Inflammation/Immunology
DDR1-IN-4 (Compound 2.45) is a selective and potent Discoidin Domain Receptor 1 (DDR1) autophosphorylation inhibitor, with IC₅₀ values of 29 nM and 1.9 μM for DDR1 and DDR2, respectively .

HY-144448

FAK-IN-2 1 Publications Verification	FAK Apoptosis	Cancer
FAK-IN-2 is a potent and orally active focal adhesion kinase (FAK) inhibitor, with anticancer activity (FAK IC₅₀= 35 nM). FAK-IN-2 covalently inhibits the autophosphorylation of FAK in a dose-dependent manner, and inhibits the clone formation and migration of tumor cells, inducing apoptosis .

HY-14674

CP-724714 4 Publications Verification	EGFR Apoptosis	Cancer
CP-724714 is a potent, selective and orally active ErbB2 (HER2) tyrosine kinase inhibitor, with an IC₅₀ of 10 nM. CP-724714 displays a marked selectivity against EGFR kinase (IC₅₀=6400 nM). CP-724714 potently inhibits ErbB2 receptor autophosphorylation in intact cells. Antitumor activities .

HY-18509

IRE1α kinase-IN-2 1 Publications Verification	IRE1	Cancer
IRE1α kinase-IN-2 is a potent IRE1α kinase inhibitor, with an EC₅₀ of 0.82 μM. IRE1α kinase-IN-2 inhibits IRE1α kinase autophosphorylation (IC₅₀=3.12 μM). IRE1α kinase-IN-2 inhibits XBP1 mRNA splicing in the WT cell lines .

HY-103274

PD180970	Bcr-Abl Src c-Kit Apoptosis	Neurological Disease Cancer
PD180970 is a highly potent and ATP-competitive p210 ^Bcr-Abl kinase inhibitor, with an IC₅₀ of 5 nM for inhibiting the autophosphorylation of p210 ^Bcr-Abl. PD180970 also inhibits Src and KIT kinase with IC₅₀s of 0.8 nM and 50 nM, respectively. PD180970 indcues apoptosis of K562 leukemic cells, and can be used for chronic myelogenous leukemia research .

HY-103471

Y11	FAK Interleukin Related	Cancer
Y11 inhibits the autophosphorylation of FAK1 by blocking the phosphorylation of Y397. Y11 increases the expression level of IL-6. Y11 is applicable for cancer research .

HY-108263

3-Hydroxy Midostaurin CGP52421	FLT3	Cancer
3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC₅₀s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively. 3-Hydroxy Midostaurin is less selective but more cytotoxic than PKC412 .

HY-101429

RG13022 1 Publications Verification Tyrphostin RG13022	EGFR	Cancer
RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor with an IC₅₀ of 4 μM.

HY-145565

Enbezotinib 1 Publications Verification TPX-0046	RET	Cancer
Enbezotinib, an inhibitor of RET, can inhibit the RET autophosphorylation. Enbezotinib can be used for the research of cancer .

HY-10255R

Sunitinib Malate (Standard) SU 11248 Malate (Standard)	Reference Standards PDGFR VEGFR IRE1 Mitophagy Autophagy Apoptosis	Cancer
Sunitinib (Malate) (Standard) is the analytical standard of Sunitinib (Malate). This product is intended for research and analytical applications. Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC₅₀s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .

HY-119910

(E)-Aminoquinol XIB4035	GDNF Receptor	Neurological Disease
(E)-Aminoquinol (XIB4035) is a GFRα-1 agonist. (E)-Aminoquinol has mimic neurotrophic effects of GDNF, and induces Ret autophosphorylation in Neuro-2A cells. (E)-Aminoquinol can be used for research of Parkinson’s disease .

HY-136895

AZ12672857	Prostaglandin Receptor	Cancer
AZ12672857 is an orally active inhibitor of EphB4 (IC₅₀=1.3 nM) and Src kinases. AZ12672857 shows good inhibition of proliferation of c-Src transfected 3T3 cells (IC₅₀=2 nM) as well as autophosphorylation of EphB4 in transfected CHO-K1 cells (IC₅₀=9 nM) .

HY-123779

RWJ-49815	Bacterial Fungal	Infection
RWJ-49815 is a histidine kinase inhibitor. RWJ-49815 inhibits the autokinase activity of purified GST-Sln1 and the autophosphorylation of KinA in vitro. RWJ-49815 acts as a fungal growth inhibitor . RWJ-49815 serves as a bactericide against Gram-positive pathogenic bacteria. RWJ-49815 is applicable to research related to fungal infections and Gram-positive bacterial infections .

HY-152183

FINDY	DYRK	Neurological Disease
FINDY is a folding intermediate-selective inhibitor of DYRK1A. FINDY can inhibit Ser97 autophosphorylation with an IC₅₀ value of 35 μM. FINDY can be used for the research of neurological disorder . FINDY is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-133779

Gefitinib impurity 5	Drug Metabolite	Cancer
Gefitinib impurity 5 is the impurity of Gefitinib (HY-133779). Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC₅₀ of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC₅₀ of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces Autophagy. Gefitinib has antitumour activity .

HY-107594

Benzene hexabromide 1 Publications Verification	JAK	Cancer
Benzene hexabromide, a bromohydrocarbon, is a potent inhibitor of JAK2 tyrosine kinase autophosphorylation.

HY-10255AS1

Sunitinib-d4	Isotope-Labeled Compounds VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis	Cancer
Sunitinib-d₄ is the deuterium labeled Sunitinib. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC₅₀s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .

HY-10255AS

Sunitinib-d10 SU 11248-d₁₀	VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis	Cancer
Sunitinib-d₁₀ (SU 11248-d₁₀) is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC₅₀s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .

Cat. No.	Product Name

HY-L016

Protein Tyrosine Kinase Compound Library

1,578 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 1,578 compounds that act as a useful tool for PTKs-related drug screening and disease research.

Cat. No.	Product Name	Target	Research Area

HY-P11056

REF1 peptide	MDM-2/p53	Others
REF1 peptide is a PORK1 agonist with an EC₅₀ of 0.028 nM in tomato. REF1 peptide binds to the extracellular domain of PORK1, triggers receptor autophosphorylation, and drives downstream MPK3/MPK6 activation, thereby initiating defense and regeneration signaling cascades. REF1 peptide induces callus formation, inhibits shoot regeneration upon continuous exposure, and enhances the regeneration and transformation efficiency of recalcitrant dicotyledonous and monocotyledonous crops .

HY-P3226

JB-1	IGF-1R VEGFR Drug Derivative	Cardiovascular Disease Neurological Disease
JB-1, an IGF-I analog, is a selective IGF-I receptor inhibitor that does not interact with IGF-II. JB-1 competes with IGF-I for binding to IGF-1R and blocks receptor autophosphorylation. JB-1 increases the level of sVEGFR-1. JB-1 normalizes retinal abnormalities, including reducing retinal neovascularization. JB-1 is applicable to studies related to oxygen-induced retinopathy .

HY-P2548

*pp60 (v-SRC) Autophosphorylation* Site, Phosphorylated**	EGFR	Others
pp60 (v-SRC) Autophosphorylation Site, Phosphorylated is the phosphorylated peptide of an EGFR substrate. pp60 (v-SRC) Autophosphorylation Site, Phosphorylated can be used for the screening of EGFR Kinase inhibitors via phosphorylated-substrate quantification .

HY-P3744

*pp60v-src Autophosphorylation* site**	EGFR	Others
pp60v-src Autophosphorylation site is a synthetic peptide. pp60v-src Autophosphorylation site can be used for various biochemical studies .

HY-P10840

Tkip	JAK MHC	Inflammation/Immunology
Tkip is a JAK2 specific inhibitor. Tkip can bind the JAK2 autophosphorylation site, inhibit the JAK2 autophosphorylation and the phosphorylation of the IFN-γ receptor subunit IFNGR-1. Tkip inhibits the antiviral activity of IFN-γ and the expression of MHC Class I molecules. Tkip can be used to study the IFN-γ signaling pathway .

HY-P1799

[pTyr5] EGFR (988-993)	Phosphatase	Others
[pTyr5] EGFR (988-993) is derived from the autophosphorylation site (Tyr992) of epidermal growth factor receptor (EGFR 988-993). [pTyr5] EGFR (988-993) is often complexed with the catalytically inactive protein-tyrosine phosphate 1B (PTP1B) .

HY-P1799A

[pTyr5] EGFR (988-993) TFA	Phosphatase	Others
[pTyr5] EGFR (988-993) TFA is derived from the autophosphorylation site (Tyr992) of epidermal growth factor receptor (EGFR 988-993). [pTyr5] EGFR (988-993) TFA is often complexed with the catalytically inactive protein-tyrosine phosphate 1B (PTP1B) .

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 .

Cat. No.	Product Name	Target	Research Area	Image

HY-P99284

Dalotuzumab 1 Publications Verification MK-0646; h7C10	IGF-1R Apoptosis	Cancer
Dalotuzumab (MK-0646) is a recombinant humanized monoclonal antibody (IgG1 type) targeting IGF-1R. Dalotuzumab acts by inhibiting IGF-1- and IGF-2-mediated tumor cell proliferation, IGF-1R autophosphorylation, and Akt phosphorylation. Dalotuzumab also induces apoptosis and cycle arrest. Dalotuzumab in combination with other anticancer agents such as statins can enhance the antitumor activity of Dalotuzumab in vitro and in vivo .

HY-P991979

Erbicin	EGFR	Cancer
Erbicin is a single-chain antibody against the human ErbB2 receptor . Erbicin specifically binds to ErbB2-positive cells, inhibits receptor autophosphorylation, and is internalized by target cells. Erbicin can be used in breast cancer-related research .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-103248

Toyocamycin 5+ Cited Publications Vengicide	Infection Microorganisms Classification of Application Fields Antibiotics Antibacterial Disease Research Disease Research Fields Other Antibiotics Source Classification	IRE1 Fungal Antibiotic Apoptosis CDK
Toyocamycin (Vengicide) is an adenosine analog produced by Streptomyces diastatochromogenes, acts as an XBP1 inhibitor. Toyocamycin blocks RNA synthesis and ribosome function, and induces apoptosis. Toyocamycin affects IRE1α-XBP1 pathway, and inhibits XBP1 mRNA cleavage with an IC₅₀ value of 80 nM with affecting IRE1α auto-phosphorylation. Toyocamycin specifically inhibits CDK9 with an IC₅₀ value of 79 nM .

HY-N4322

Decursinol angelate 1 Publications Verification	Structural Classification Pseudognaphalium affine (D. Don) Anderberg Classification of Application Fields Coumarins Phenylpropanoids Umbelliferae Plants Inflammation/Immunology Disease Research Fields Source Classification Cancer	PKC
Decursinol angelate acts as a PKC activator and GDH inhibitor, with an IC₅₀ of 1.432 μM against human GDH. Decursinol angelate activates PKC, downregulates PKCα and PKCβII isoforms, and exerts cytotoxic activity against cancer cells. Decursinol angelate binds to GDH and inhibits its enzymatic activity. Decursinol angelate inhibits VEGF-induced autophosphorylation of VEGFR2, downstream p42/44 ERK and JNK-MAPK signaling pathways, as well as the angiogenesis process. Decursinol angelate is applicable to research related to cancer and leukemia .

HY-108485

Damnacanthal	Infection Quinones Monophenols Classification of Application Fields Anthraquinones Morinda citrifolia Linn. Rubiaceae Phenols Plants Inflammation/Immunology Disease Research Fields Source Classification	Src Apoptosis Fungal
Damnacanthal is an anthraquinone isolated from the root of Morinda citrifolia. Damnacanthal is a highly potent, selective inhibitor of p56 ^lck tyrosine kinase activity. Natural Damnacanthal inhibits p56 ^lck autophosphorylation and phosphorylation of exogenous substrates with IC₅₀s of 46 nM and 220 nM, respectively. Damnacanthal is a potent inducer of apoptosis with anticancer activity. Damnacanthal also has antinociceptive, anti-inflammatory effects in mice and anti-fungal activity against *Candida albicans* .

Cat. No.	Product Name	Chemical Structure

HY-50895S2

Gefitinib-d3

Gefitinib-d₃ (ZD1839-d₃) is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC₅₀ of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC₅₀ of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity .

HY-10255AS1

Sunitinib-d4
Sunitinib-d₄ is the deuterium labeled Sunitinib. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC₅₀s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .

HY-10255AS

Sunitinib-d10
Sunitinib-d₁₀ (SU 11248-d₁₀) is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC₅₀s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .

HY-149413

FHND5071
FHND5071 is a potent and selective RET kinase inhibitor, FHND5071 can exert antitumor effects by inhibiting RET autophosphorylation. FHND5071 can be used for tumor diseases research .

HY-50895S1

Gefitinib-d6

Gefitinib-d₆ is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC₅₀ of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC₅₀ of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity .

HY-108263S

3-Hydroxy Midostaurin-d5
3-Hydroxy Midostaurin-d₅ is a deuterium labeled 3-Hydroxy Midostaurin. 3-Hydroxy Midostaurin is a metabolite of PKC412, which effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC₅₀s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively .

HY-13001S

Quizartinib-d8

Quizartinib (AC220)-d₈ is deuterium labeled Quizartinib (HY-13001). Quizartinib is an orally active, potent and selective FLT3 inhibitor. Quizartinib inhibits kinase activity of mutant-FLT3, -PDGFRA and -KIT isoforms and inhibits autophosphorylation. Quizartinib inhibits cellular proliferation, induces apoptosis in cancer cells. Quizartinib can be used for the research of cancer .

HY-W751180

3-Hydroxy Midostaurin-13C6

3-Hydroxy Midostaurin- ¹³C₆ (CGP52421- ¹³C₆) is the ¹³C-labeled 3-Hydroxy Midostaurin (HY-108263). 3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC₅₀s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively. 3-Hydroxy Midostaurin is less selective but more cytotoxic than PKC412 .

HY-50896S3

Erlotinib-d8

Erlotinib-d₈ (CP-358774-d₈) is deuterium labeled Erlotinib. Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC₅₀ of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC₅₀ of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer . Erlotinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-50896S2

Erlotinib-d4

Erlotinib-d₄ (CP-358774-d₄) is deuterium labeled Erlotinib. Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC₅₀ of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC₅₀ of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer . Erlotinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-13012S

RepSox-d5
RepSox-d₅ (E-616452-d₅) is the deuterium labeled RepSox (HY-13012). RepSox (E-616452) is a potent and selective transforming growth factor-beta receptor I/activin like kinase 5 (TGF-β-RI/ALK5) inhibitor. RepSox inhibits ALK5 autophosphorylation with an IC₅₀ value of 4 nM. RepSox can be used for the research of obesity and associated metabolic diseases such as type 2 diabetes .

Cat. No.	Product Name		Classification

HY-50896

Erlotinib 130+ Cited Publications CP-358774; NSC 718781; OSI-774		Alkynes
Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC₅₀ of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC₅₀ of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer . Erlotinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Cat. No.	Product Name		Classification

HY-174720

Human EIF2AK2 mRNA		mRNA
Human EIF2AK2 mRNA encodes the human eukaryotic translation initiation factor 2 alpha kinase 2 (EIF2AK2) protein, a serine/threonine protein kinase that is activated by autophosphorylation after binding to dsRNA. EIF2AK2 plays a key role in the innate immune response to viral infection and is also involved in the regulation of signal transduction, apoptosis, cell proliferation and differentiation.

HY-174721

Human EGFR mRNA		mRNA
Human EGFR mRNA encodes the human epidermal growth factor receptor (EGFR) protein, a member of the protein kinase superfamily. IGF1R plays a critical role in transformation events. EGFR is a cell surface protein that binds to epidermal growth factor, thus inducing receptor dimerization and tyrosine autophosphorylation leading to cell proliferation.

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