autophosphorylation

By Targets:	Amino Acid Derivatives (1) Amyloid-β (1) Anaplastic lymphoma kinase (ALK) (1) Antibiotic (1) Apoptosis (26) Autophagy (10) Bcr-Abl (5) Btk (3) c-Fms (2) c-Kit (6) CaMK (1) Caspase (2) CDK (2) Checkpoint Kinase (Chk) (6) Dengue virus (1) Discoidin Domain Receptor (3) DNA/RNA Synthesis (1) Drug Metabolite (2) DYRK (1) EGFR (20) Ephrin Receptor (1) FAK (5) FGFR (3) Flavivirus (1) FLT3 (9) Fungal (2) GDNF Receptor (1) IGF-1R (2) Insulin Receptor (1) IRE1 (7) Isotope-Labeled Compounds (3) JAK (3) Ligands for Target Protein for PROTAC (1) LRRK2 (3) Mitophagy (3) Mps1 (1) Organoid (1) Orthopoxvirus (2) P2X Receptor (1) PDGFR (10) Phosphatase (2) Pim (1) Prostaglandin Receptor (1) RET (3) SARS-CoV (1) Src (6) TGF-β Receptor (5) VEGFR (5)
By Research Areas:	Cancer (75) Cardiovascular Disease (2) Infection (5) Inflammation/Immunology (3) Metabolic Disease (5) Neurological Disease (9)
Click Chemistry:	Alkynes (2)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-101957

AG 1295 2 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.

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

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-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-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-125203

PV-1019 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-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-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-14674

CP-724714 3 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-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-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-144437

ALK5-IN-9	TGF-β Receptor	Cancer
ALK5-IN-9 (Compound 8h) is a potent and orally active inhibitor of TGFβRI (ALK5). ALK5-IN-9 inhibits ALK5 autophosphorylation and NIH3T3 cell activity with IC₅₀ values of 25 nM and 74.6 nM, respectively. ALK5-IN-9 also shows favorable pharmacokinetic profile and ameliorated hERG inhibition. ALK5-IN-9 has the potential for the research of cancer disease .

HY-13686

PQ401 2 Publications Verification	IGF-1R Apoptosis	Cancer
PQ401 is a potent inhibitor of IGF-IR signaling. PQ401 inhibits IGF-I-stimulated IGF-IR autophosphorylation with an IC₅₀ of 12.0 μM in a series of studies in MCF-7 cells. PQ401 is effective at inhibiting IGF-I-stimulated growth of MCF-7 cells (IC₅₀, 6 μM). PQ401 is a potential agent for breast and other IGF-I-sensitive cancers. PQ401 induces caspase-mediated apoptosis .

HY-101042

AG-494 Tyrphostin AG 494	EGFR CDK	Cancer
AG-494 (Tyrphostin AG 494) is a potent and selective EGFR tyrosine kinase inhibitor (IC₅₀=0.7 μM). AG-494 inhibits the autophosphorylation of EGFR, ErbB2, HER1-2 and PDGF-R with IC₅₀s 1.1, 39, 45 and 6 μM, respectively. AG-494 blocks Cdk2 activation and inhibits EGF-dependent DNA synthesis .

HY-50896

Erlotinib 70+ 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-136735

IRE1α kinase-IN-1	IRE1	Neurological Disease Cancer
IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC₅₀ of 77 nM. IRE1α kinase-IN-1 displays 100-fold selectivity for IRE1α over the IRE1β isoform. IRE1α kinase-IN-1 inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC₅₀=80 nM) .

HY-101544

ARQ 069	FGFR	Cancer
ARQ 069, an analog of ARQ 523, inhibits FGFR in an enantiospecific manner. ARQ 069 targets the unphosphorylated, inactive forms of FGFR1/FGFR2 kinases (IC₅₀s of 0.84 μM and 1.23 μM, respectively). ARQ 069 inhibits FGFR1/FGFR2 autophosphorylation (IC₅₀s of 2.8 and 1.9 μM, respectively) through a mechanism in a non-ATP competitive dependent manner .

HY-118304

AKN-028	FLT3 Apoptosis Caspase	Cancer
AKN-028, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC₅₀ value of 6 nM. AKN-028 inhibits FLT3 autophosphorylation. AKN-028 induces dose-dependent cytotoxic response (mean IC₅₀=1 μM). AKN-028 induces apoptosisby activation of caspase 3. AKN-028 can be used in research of acute myeloid leukemia (AML) .

HY-118304B

AKN-028 acetate	FLT3 Apoptosis Caspase	Cancer
AKN-028 acetate, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6 nM. AKN-028 acetate inhibits FLT3 autophosphorylation. AKN-028 acetate induces dose-dependent cytotoxic response (mean IC50=1 μM). AKN-028 acetate induces apoptosisby activation of caspase 3. AKN-028 acetate can be used in research of acute myeloid leukemia (AML).

HY-151441

LRRK2-IN-5	LRRK2	Neurological Disease
LRRK2-IN-5 (compound 25) is a potent, orally active, selective leucine rich repeat protein kinase 2 gene (LRRK2) inhibitor with IC₅₀ values of 1.2 and 16 μM for GS LRRK2 and WT LRRK2, respectively. LRRK2-IN-5 inhibits LRRK2 Ser1292 and Ser925 autophosphorylation. LRRK2-IN-5 can cross the blood-brain barrier .

HY-151444

LRRK2-IN-6	LRRK2	Neurological Disease
LRRK2-IN-6 (compound 22) is a potent, orally active, selective leucine rich repeat protein kinase 2 gene (LRRK2) inhibitor with IC₅₀ values of 4.6 and 49 μM for GS LRRK2 and WT LRRK2, respectively. LRRK2-IN-6 inhibits LRRK2 Ser1292 and Ser925 autophosphorylation. LRRK2-IN-6 can cross the blood-brain barrier .

HY-112345

PD-089828	FGFR PDGFR EGFR Src	Cancer
PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC₅₀s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC₅₀=0.18 µM). PD-089828 also inhibits MAPK with an IC₅₀ of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity .

HY-13012

RepSox 15+ 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-10255A

Sunitinib 45+ 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-10255

Sunitinib Malate 45+ 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

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-103471

Y11

FAK Cancer

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

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

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

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

HY-10255AS

Sunitinib-d10 SU 11248-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[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].

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[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].

HY-147414

Vamotinib PF-114	Bcr-Abl	Cancer
Vamotinib (PF-114) is a potent, selective and orally active tyrosine kinase inhibitor. Vamotinib inhibits the autophosphorylation of BCR/ABL and BCR/ABL-T315I. Vamotinib induces apoptosis. Vamotinib shows anti-proliferative and anti-tumor activity. Vamotinib has the potential for the research of resistant philadelphia chromosome-positive (Ph+) leukemia. Vamotinib inhibits ABL series kinases with IC₅₀s of 0.49 nM (ABL), 0.78 nM (ABL ^T315I), 9.5 nM (ABL ^E255K), 2.0 nM (ABL ^F317I), 7.4 nM (ABL ^G250E), 1.0 nM (ABL ^H396P), 2.8 nM (ABL ^M351T), 12 nM (ABL ^Q252H), and 4.1 nM (ABL ^Y253F), respectively . Vamotinib 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-15002

AST 487 4 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 15+ 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-13258A

NVP-BHG712 4 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-149413

FHND5071	RET	Others
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-15003

ATH686	FLT3 Apoptosis	Cancer
ATH686 is a potent, selective and ATP-competitive FLT3 inhibitor. ATH686 target mutant FLT3 protein kinase activity and inhibit the proliferation of cells harboring FLT3 mutants via induction of apoptosis and cell cycle inhibition. ATH686 has antileukemic effects .

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-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-18899

Nec-3a

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 .

Nec-3a
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-112162

BOS-172722	Mps1	Cancer
BOS-172722 is an inhibitor of monopolar spindle 1 (MPS1) checkpoint with an IC₅₀ of 11 nM and 63 nM for MPS1 (1 mM ATP) and P-MPS1, respectively. BOS-172722 also has potential for the study of various forms of breast cancer .

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 .

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-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-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-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-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-15480

NSC 42834 1 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-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-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) .

Cat. No.	Product Name

HY-L016

Protein Tyrosine Kinase Compound Library

1045 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 1045 compounds that act as a useful tool for PTKs-related drug screening and disease research.

Cat. No.	Product Name	Type

HY-13012G

RepSox (GMP) E-616452 (GMP); SJN 2511 (GMP)	Fluorescent Dye
RepSox (E-616452) (GMP) is a RepSox (HY-13012) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. RepSox is a potent and selective TGF-β-RI/ALK5 inhibitor .

Cat. No.	Product Name	Type

HY-13012G

RepSox (GMP) E-616452 (GMP); SJN 2511 (GMP)	Biochemical Assay Reagents
RepSox (E-616452) (GMP) is a RepSox (HY-13012) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. RepSox is a potent and selective TGF-β-RI/ALK5 inhibitor .

Cat. No.	Product Name	Target	Research Area

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

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-P2385

Fmoc-Val-Ser(psi(Me,Me)pro)-OH

Amino Acid Derivatives Others

Fmoc-Val-Ser(psi(Me,Me)pro)-OH is a dipeptide.

Cat. No.	Product Name	Target	Research Area

HY-P99284

Dalotuzumab 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 4 Publications Verification 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 Rubiaceae Morinda citrifolia Linn. 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-15463S1

Imatinib-d4
Imatinib-d₄ is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity[1][2].

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[1][2].

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[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].

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[1].

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[1][2].

HY-50896S

Erlotinib-d6
Erlotinib-d₆ (CP-358774 D6) is a deuterium labeled Erlotinib (CP-358774). Erlotinib is a directly acting inhibitor EGFR tyrosine kinase inhibitor with an IC50 of 2 nM for human EGFR[1]. Erlotinib-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Cat. No.	Product Name		Classification

HY-50896

Erlotinib 70+ 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.

HY-50896S

Erlotinib-d6 CP-358774-d₆; NSC 718781-d₆; OSI-774-d₆		Alkynes
Erlotinib-d₆ (CP-358774 D6) is a deuterium labeled Erlotinib (CP-358774). Erlotinib is a directly acting inhibitor EGFR tyrosine kinase inhibitor with an IC50 of 2 nM for human EGFR[1]. Erlotinib-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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