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Results for "

auto-phosphorylation

" in MedChemExpress (MCE) Product Catalog:

By Targets:	DYRK (1) Akt (1) Anaplastic lymphoma kinase (ALK) (3) Antibiotic (1) Apoptosis (29) ATM/ATR (1) Autophagy (16) Bcr-Abl (6) BCRP (1) Btk (2) c-Fms (2) c-Kit (3) CaMK (1) Caspase (3) CDK (2) Checkpoint Kinase (Chk) (2) Discoidin Domain Receptor (3) DNA-PK (1) Drug Metabolite (3) EGFR (25) Endogenous Metabolite (1) Ephrin Receptor (1) ERK (2) FAK (5) FGFR (4) FLT3 (13) Fungal (2) GDNF Receptor (4) Hippo (MST) (1) IGF-1R (3) Insulin Receptor (1) IRE1 (10) Isotope-Labeled Compounds (7) JAK (5) Ligands for Target Protein for PROTAC (4) LRRK2 (3) MHC (1) Mitophagy (6) Nucleoside Antimetabolite/Analog (1) Organoid (2) Orthopoxvirus (4) PDGFR (12) Phosphatase (2) Prostaglandin Receptor (1) Reference Standards (9) RET (4) RIP kinase (1) ROS Kinase (1) Src (7) STAT (2) TGF-beta/Smad (1) TGF-β Receptor (5) VEGFR (9) YAP (1)
By Research Areas:	Cancer (89) Cardiovascular Disease (6) Infection (6) Inflammation/Immunology (5) Metabolic Disease (6) Neurological Disease (12)
Click Chemistry:	Alkynes (1)

117

Inhibitors & Agonists

Screening Libraries

Peptides

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: Oxidative Phosphorylation DYRK

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-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-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-162309

CSF1R-IN-20	c-Fms	Cancer
CSF1R-IN-20 (compound 7a) is a CSF-1R Inhibitor with an IC₅₀ value of 467 nM. CSF1R-IN-20 inhibits CSF-1R auto-phosphorylation .

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-101521

CHMFL-BTK-01	Btk	Cancer
CHMFL-BTK-01 (compound 9) is a highly selective irreversible BTK inhibitor, with an IC₅₀ of 7 nM. CHMFL-BTK-01 (compound 9) potently inhibited BTK Y223 auto-phosphorylation .

HY-157996

CSF1R-IN-21	c-Fms	Neurological Disease
CSF1R-IN-21 (compound 7e) is a CSF-1R Inhibitor with an IC₅₀ value of 31 nM. CSF1R-IN-21 inhibits CSF-1R auto-phosphorylation and can be used for the research of neurodegenerative diseases .

HY-162413

(R)-LW-Srci-8	Src	Cancer
(R)-LW-Srci-8 is a selective covalent inhibitor of c-Src (IC₅₀= 35.83 nM) that disrupts the autophosphorylation of c-Src by targeting its autophosphorylation site (Y419) .

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-107594

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

HY-10255A

Sunitinib 60+ 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-101957R

AG 1295 (Standard)	Reference Standards PDGFR	Cardiovascular Disease
AG 1295 (Standard) is the analytical standard of AG 1295. This product is intended for research and analytical applications. 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-10255

Sunitinib Malate 60+ Cited Publications SU 11248 Malate	PDGFR VEGFR IRE1 Mitophagy Autophagy Apoptosis	Cancer
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-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 TPX-0046	RET	Cancer
Enbezotinib, an inhibitor of RET, can inhibit the RET autophosphorylation. Enbezotinib can be used for the research of cancer .

HY-10255AS

Sunitinib-d10 SU 11248-d₁₀	VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis	Cancer
Sunitinib-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-103471

Y11	FAK	Cancer
Y11 inhibits FAK1 autophosphorylation by blocking phosphorylation of Y397 and decreases tumor growth .

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-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-10255AR

Sunitinib (Standard) SU 11248 (Standard)	Reference Standards VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis	Cancer
Sunitinib (Standard) is the analytical standard of Sunitinib. This product is intended for research and analytical applications. 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-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-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-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-12444

Y15 20+ 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-149413

FHND5071	RET	Others Cancer
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-13258A

NVP-BHG712 5 Publications Verification 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-144131

RET-IN-11	Apoptosis RET	Cancer
RET-IN-11 is a potent and selective RET inhibitor with IC₅₀s of 6.20 nM, 18.68 nM for RET and RET ^V804M, respectively. RET-IN-11 shows anti-proliferation and migration activity in CCDC6-RET-driven LC-2/ad cells. RET-IN-11 induces cell apoptosis .

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-103443A

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

HY-119910A

Aminoquinol (E/Z)-XIB4035	GDNF Receptor	Neurological Disease
Aminoquinol is a GFRα-1 agonist. Aminoquinol exhibits neurotrophic effects similar to GDNF and induces Ret autophosphorylation in Neuro-2A cells. Aminoquinol can be used in research related to Parkinson's disease .

HY-101962

HNMPA	Insulin Receptor	Metabolic Disease
HNMPA is a membrane impermeable insulin receptor tyrosine kinase inhibitor. HNMPA inhibits serine and tyrosine autophosphorylation by the human insulin receptor. HNMPA has no effect on protein kinase C or cyclic AMP-dependent protein kinase activities

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-18899

Nec-3a	RIP kinase	Cancer
Nec-3a is a Necrostatin-3 analogue. Nec-3a is a RIP1 inhibitor (IC₅₀: 0.44 μM). Nec-3a inhibits the autophosphorylation activity of the RIP1 kinase domain .

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-125203

PV-1019 1 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-17537

APY29 5+ 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-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-119910B

Aminoquinol phosphate (E/Z)-XIB4035 phosphate	GDNF Receptor	Neurological Disease
Aminoquinol ((E/Z)-XIB4035) phosphate is a GFRα-1 agonist. Aminoquinol phosphate exhibits neurotrophic effects similar to GDNF and induces Ret autophosphorylation in Neuro-2A cells. Aminoquinol phosphate can be used in research related to Parkinson's disease .

HY-144448

FAK-IN-2	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-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-119910C

Aminoquinol triphosphate (E/Z)-XIB4035 triphosphate	GDNF Receptor	Neurological Disease
Aminoquinol ((E/Z)-XIB4035) phosphate is a GFRα-1 agonist. Aminoquinol phosphate exhibits neurotrophic effects similar to GDNF and induces Ret autophosphorylation in Neuro-2A cells. Aminoquinol phosphate can be used in research related to Parkinson's disease .

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-15480

NSC 42834 2 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-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-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 .

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) .

Cat. No.	Product Name

HY-L016

Protein Tyrosine Kinase Compound Library

1,330 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 1,330 compounds that act as a useful tool for PTKs-related drug screening and disease research.

Cat. No.	Product Name	Target	Research Area

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-P3226

JB-1	IGF-1R	Metabolic Disease
JB-1, an IGF-1 peptide analog, is a selective and potent IGF-1R antagonist. JB-1 competes with IGF-1 by binding the IGF-1 receptor. JB-1 prevents the autophosphorylation of IGF-1R, and has no activity in IGF-II .

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-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

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 .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-103248

Toyocamycin 5+ Cited Publications Vengicide	Infection Structural Classification Microorganisms Classification of Application Fields Antibiotics Source classification Antibacterial Disease Research Disease Research Fields Other Antibiotics	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-108485

Damnacanthal	Structural Classification Classification of Application Fields Source classification Plants Infection Quinones Monophenols Anthraquinones Morinda citrifolia Linn. Rubiaceae Phenols Inflammation/Immunology Disease Research Fields	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-10255AS

Sunitinib-d10
Sunitinib-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-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-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-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-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-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-13001S

Quizartinib-d8

Quizartinib-d₈ (AC220-d₈) is deuterium labeled Quizartinib. Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a K_d of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC₅₀s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis .

Cat. No.	Product Name		Classification

HY-50896

Erlotinib 100+ 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.

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