Search Result

Pathways Recommended:	Protein Tyrosine Kinase/RTK

Results for "

tyrosine phosphorylation

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Anaplastic lymphoma kinase (ALK) (4) Btk (2) DYRK (4) FLT3 (1) Syk (2) Akt (3) Apoptosis (9) Autophagy (6) Bcr-Abl (1) c-Kit (2) c-Met/HGFR (5) CDK (1) Cyclic GMP-AMP Synthase (1) DNA/RNA Synthesis (1) EGFR (12) Epigenetic Reader Domain (1) ERK (4) FGFR (2) Fungal (1) GLUT (1) Histone Acetyltransferase (1) Insulin Receptor (4) JAK (2) NF-κB (1) p38 MAPK (2) PDGFR (2) PDHK (1) Phosphatase (2) PKA (1) RET (3) ROS Kinase (4) SHP2 (1) Src (2) STAT (2) Tie (1) Trk Receptor (4) Tyrosinase (2) VEGFR (2)
By Research Areas:	Cancer (37) Cardiovascular Disease (2) Endocrinology (2) Infection (1) Inflammation/Immunology (6) Metabolic Disease (5) Neurological Disease (3)

By Targets:

Anaplastic lymphoma kinase (ALK) (4)

Btk (2)

DYRK (4)

FLT3 (1)

Syk (2)

Akt (3)

Apoptosis (9)

Autophagy (6)

Bcr-Abl (1)

c-Kit (2)

c-Met/HGFR (5)

CDK (1)

Cyclic GMP-AMP Synthase (1)

DNA/RNA Synthesis (1)

EGFR (12)

Epigenetic Reader Domain (1)

ERK (4)

FGFR (2)

Fungal (1)

GLUT (1)

Histone Acetyltransferase (1)

Insulin Receptor (4)

JAK (2)

NF-κB (1)

p38 MAPK (2)

PDGFR (2)

PDHK (1)

Phosphatase (2)

PKA (1)

RET (3)

ROS Kinase (4)

SHP2 (1)

Src (2)

STAT (2)

Tie (1)

Trk Receptor (4)

Tyrosinase (2)

VEGFR (2)

By Research Areas:

Cancer (37)

Cardiovascular Disease (2)

Endocrinology (2)

Infection (1)

Inflammation/Immunology (6)

Metabolic Disease (5)

Neurological Disease (3)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Recombinant Proteins

Isotope-Labeled Compounds

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

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-20878

Tyrphostin AG 879 1 Publications Verification AG 879	Trk Receptor EGFR Apoptosis	Cancer
Tyrphostin AG 879 (AG 879) is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation (IC₅₀ of 10 μM), but not TrKB and TrKC. Tyrphostin AG 879 is also a selective ErbB2 tyrosine kinase inhibitor with an IC₅₀ of 1 μM, and has at least 500-fold higher selectivity to ErbB2 than EGFR. Tyrphostin AG 879 has anticancer activity .

HY-15838

ID-8 4 Publications Verification	DYRK	Cancer
ID-8 is an inhibitor of *dual-specificity tyrosine* phosphorylation-regulated kinase (DYRK)**. ID-8 sustains embryonic stem cell (ESC) self-renewal and pluripotency. ID-8 enhances Wnt-mediated hESC survival and proliferation via inhibition of DYRKs .

HY-N0755

Rhoifolin	Insulin Receptor GLUT NF-κB p38 MAPK Autophagy	Metabolic Disease Endocrinology Cancer
Rhoifolin is a flavone glycoside can be isolated from Rhus succedanea. Rhoifolin has anti-diabetic effect acting through enhanced adiponectin secretion, tyrosine phosphorylation of insulin receptor-β and glucose transporter 4 (GLUT 4) translocation. Rhoifolin has an anti-inflammatory action via multi-level regulation of inflammatory mediators. Rhoifolin ameliorates titanium particle-stimulated osteolysis and attenuates osteoclastogenesis via RANKL-induced NF-κB and MAPK pathways. Rhoifolin also has cytotoxic activity against different cancer cell lines .

HY-124827

Tec-IN-1	Tyrosinase	Cancer
Tec-IN-1 (Compound 21) is a Tec inhibitor (IC₅₀s of 11.7 μM). Tec-IN-1 inhibits Tec-mediated tyrosine phosphorylation of FGF2, and inhibits FGF2 secretion from cells .

HY-N3550

Catalponol	Others	Cancer
Catalponol is a naphthoquinone derivative. Catalponol enhances dopamine biosynthesis by inducing tyrosine hydroxylase activity. Catalponol also increases the levels of cAMP and tyrosine hydroxylase phosphorylation in PC12 cells .

HY-125260

SHP844	SHP2	Cancer
SHP844 is a SHP2 inhibitor with the IC₅₀ of 18.9 µM. SHP2 is a protein tyrosine phosphatase (PTP) that regulates tyrosine phosphorylation levels and is involved in cell proliferation, differentiation and survival .

HY-147303

Sacibertinib	Trk Receptor EGFR	Cancer
Sacibertinib is a tyrosine kinase (Trk) inhibitor with EC₅₀ value of 110 nM and 244 nM for EGFR-TK phosphorylation and HER2, respectively. Antineoplastic activity .

HY-50878

Crizotinib 60+ Cited Publications PF-02341066	Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy	Cancer
Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .

HY-50878B

Crizotinib acetate PF-02341066 acetate	Anaplastic lymphoma kinase (ALK) ROS Kinase c-Met/HGFR	Cancer
Crizotinib (PF-02341066) acetate is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib acetate inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. Crizotinib acetate is also a ROS1 inhibitor. Crizotinib acetate has effective tumor growth inhibition .

HY-107586

Demethylasterriquinone B1 DAQ B1; L-783281; Dimethylasterriquinone	Insulin Receptor Akt	Endocrinology
Demethylasterriquinone B1 is a selective insulin receptor activator. Demethylasterriquinone B1 stimulates tyrosine phosphorylation of the IR β subunit, and the activation of PIK3 and AKT .

HY-50878S

Crizotinib-d5 PF-02341066-d₅	Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy	Cancer
Crizotinib-d₅ is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .

HY-101246

RPI-1
RPI-1 is a specific, orally available 2-indolinone Ret tyrosine kinase inhibitor. RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT in human medullary thyroid carcinoma TT cells. Antitumor activity .

HY-50878A

Crizotinib hydrochloride 60+ Cited Publications PF-02341066 hydrochloride	Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy	Cancer
Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .

HY-124404A

12(S)-HETE	ERK DNA/RNA Synthesis p38 MAPK	Cancer
12(S)-HETE is the 12-lipoxygenase metabolite of arachidonic acid and has a mitogenic effect on cancer cell proliferation. 12(S)-HETE induces tyrosine phosphorylation of cellular proteins, promotes ERK and P38 MAPK phosphorylation, increases DNA synthesis, and stimulates the proliferation of pancreatic cancer cells .

HY-108330

AG126 2 Publications Verification Tyrphostin AG126	ERK	Inflammation/Immunology
AG126 is a tyrosine kinase inhibitor, can inhibit the phosphorylation of ERK1 and ERK2 at 25-50 μM. AG126 can be used in meiosis, mitosis, and postmitotic research .

HY-N0737A

Harmine 15+ Cited Publications Telepathine
Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT_2A serotonin receptor, with an K_i of 397 nM .

HY-116111

AG 370	PDGFR	Cardiovascular Disease
AG 370, an indole tyrphostin, is a potent PDGF-induced mitogenesis inhibotor (IC₅₀ of 20 μM). AG 370 displays weak inhibition of the EGF receptor .

HY-128758

DYRKs-IN-1	DYRK	Cancer
DYRKs-IN-1 is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC₅₀s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 has antitumor activity .

HY-128758A

DYRKs-IN-1 hydrochloride	DYRK	Cancer
DYRKs-IN-1 hydrochloride is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC₅₀s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 hydrochloride has antitumor activity .

HY-148779

FGFR3-IN-5	FGFR	Cancer
FGFR3-IN-5 is a potent and selective FGFR3 inhibitor with IC₅₀ values of 3, 44, and 289 nM for FGFR3, FGFR2, and FGFR1, respectively. FGFR3-IN-5 can be used in research of cancer .

HY-101084

NSC 228155 5+ Cited Publications	EGFR Histone Acetyltransferase Epigenetic Reader Domain	Cancer
NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR . NSC 228155 is also a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP, with an IC₅₀ of 0.36 μM .

HY-138961

ER-27319	Syk	Inflammation/Immunology
ER-27319, an acridone derivative, is a potent and selective SYK inhibitor, and inhibits the tyrosine phosphorylation of SYK and its activity. ER-27319 inhibits the release of antigen-induced allergic mediators from human and rat mast cells with an IC₅₀ of 10 μM and can be used for study in allergic diseases .

HY-108489

ER-27319 maleate	Syk	Inflammation/Immunology
ER-27319 (maleate), an acridone derivative, is a potent and selective SKY inhibitor, and inhibits the tyrosine phosphorylation of SYK and its activity. ER-27319 (maleate) inhibits the release of antigen-induced allergic mediators from human and rat mast cells with an IC₅₀ of 10 μM and can be used for study in allergic diseases ^[1] ^[2].

HY-119152

CMX-2043	Insulin Receptor Tyrosinase Akt	Others
CMX-2043 is a novel analogue of α-Lipoic Acid (HY-N0492). CMX-2043 is effective in antioxidant effect, activation of insulin receptor kinase, soluble tyrosine kinase, and Akt phosphorylation. CMX-2043 shows protection against ischemia-reperfusion injury (IRI) in rat model .

HY-149007

STAT3-IN-11 1 Publications Verification	STAT Apoptosis	Cancer
STAT3-IN-11 (7a) is a selective STAT3 inhibitor that inhibits the phosphorylation of STAT3 at site pTyr705. STAT3-IN-11 inhibits the phosphorylation of downstream genes (Survivin and Mcl-1) without affecting its upstream tyrosine kinases (Src and JAK2) levels and p-STAT1 expression. STAT3-IN-11 can induce cancer cell apoptosis, which is potential for the discovery of effective STAT3 inhibitors and antitumor agents against cancers .

HY-111489

LMPTP inhibitor 1	Phosphatase	Metabolic Disease
LMPTP inhibitor 1 is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC₅₀ of 0.8 μM LMPTP-A.

HY-101960A

Tyrphostin A51 AG-183	EGFR	Others
Tyrphostin A51 is a potent *protein tyrosine* kinase (PTK)** inhibitor. Tyrphostin A51 inhibits the volume-dependent release of [ ³H]taurine in a dose-dependent manner. Tyrphostin A51 markedly reduces cellular tyrosyl phosphorylation level. Tyrphostin A51 inhibits both basal and EGF-induced human bone cell proliferation .

HY-50683

JNJ-38877605 3 Publications Verification	c-Met/HGFR	Metabolic Disease Cancer
JNJ-38877605 is an orally active ATP-competitive inhibitor of c-Met with an IC₅₀ of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases . JNJ-38877605 inhibits c-Met phosphorylation and regulates lipid accumulation. JNJ-38877605 can be used for tumor and metabolic disease reseach .

HY-15844

AG-825 Tyrphostin AG-825	EGFR Apoptosis	Neurological Disease Inflammation/Immunology Cancer
AG-825 (Tyrphostin AG-825) is a selective and ATP-competitive ErbB2 inhibitor which suppresses tyrosine phosphorylation, with an IC₅₀ of 0.35 μM. AG-825 displays anti-cancer activity . AG825 significantly accelerates apoptosis of human neutrophils . AG-825 is a potential agent for overcoming Mn-induced neurotoxicity or AD development .

HY-130616

EGFR-IN-11	EGFR Apoptosis	Cancer
EGFR-IN-11 is a fourth-generation *EGFR*-tyrosine kinase inhibitor (EGFR-TKI) with an IC₅₀ of 18 nM for triple mutant EGFR ^{L858R/T790M/C797S}. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1 .

HY-50867

Lestaurtinib 3 Publications Verification CEP-701; KT-5555	JAK FLT3 Trk Receptor Apoptosis STAT	Cancer
Lestaurtinib (CEP-701) is an orally active and selective *RPTKs (receptor protein tyrosine* kinase) inhibitor, competitively inhibits ATP binding to the TrkA/B/C** domain. Lestaurtinib inhibits RPTKs phosphorylation, with IC₅₀s of 2, 25 and 0.9 nM for FLT3, TrkA and JAK2, respectively. Lestaurtinib induces apoptosis and cycle arrest, also can inhibit growth of tumor .

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-101960

(Z)-Tyrphostin A51 (Z)-AG-183	EGFR	Others
(Z)-Tyrphostin A51 is the Z configuration of Lanoconazole A51. Tyrphostin A51 is a potent *protein tyrosine* kinase (PTK)** inhibitor. Tyrphostin A51 inhibits the volume-dependent release of [ ³H]taurine in a dose-dependent manner. Tyrphostin A51 markedly reduces cellular tyrosyl phosphorylation level. Tyrphostin A51 inhibits both basal and EGF-induced human bone cell proliferation .

HY-156618

Irpagratinib ABSK011	FGFR	Cancer
Irpagratinib (ABSK011) is an orally active inhibitor of fibroblast growth factor receptor (FGFR) tyrosine kinase, targeting to FGFR4 (IC50<10 nM). Irpagratinib inhibits the auto-phosphorylation of FGFR4 and blocks signal transduction from FGFR4 to downstream pathway activation. Irpagratinib exhibits high exposure in PK study in mouse, rat and dog, and also shows antineoplastic/anti-tumor activity in subcutaneous xenograft tumor models .

HY-116116

Tafetinib SIM010603	c-Kit RET VEGFR	Cancer
Tafetinib (SIM010603) is an oral multi-targets receptor tyrosine kinases inhibitor. Tafetinib inhibitsstem cell factor receptor (Kit),vascular endothelial growth factor receptor-2 (VEGFR-2),platelet-derived growth factor receptor-β (PDGFR-β),glial cell line-derived neurotrophic factor receptor (Rearranged during Transfection; RET), andFms-like tyrosine kinase-3 (FLT3)withIC₅₀values between 5.0 and 68.1 nmol/l. Tafetinib inhibits the phosphorylation ofPDGFR-βandVEGFR-2. Tafetinib inhibits endothelial cell proliferation, endothelial cells chemotaxis, and corneal angiogenesis .

HY-108485

Damnacanthal	Src Apoptosis Fungal	Infection Inflammation/Immunology Cancer
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* .

HY-124097

HNMPA-(AM)3	Insulin Receptor	Metabolic Disease
HNMPA-(AM)3 is a cell-permeable and selective *insulin receptor tyrosine* kinase** inhibitor analog of HNMPA. HNMPA-(AM)3 greatly inhibits the ability of prothoracicotropic hormone (PTTH) to activate ERK phosphorylation and stimulate ecdysteroidogenesis. HNMPA-(AM)3 is also effective in inhibiting ecdysteroid production (IC₅₀=14.2 μM) and insulin receptor activity (IC₅₀ is 14.2 μM and 200 μM in mosquitoes and mammals, respectively) .

HY-123468

HA-1004	Cyclic GMP-AMP Synthase PKA ERK	Cardiovascular Disease Metabolic Disease
HA-1004 is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .

HY-121833

Gambogic amide	Trk Receptor Akt ERK	Neurological Disease Cancer
Gambogic amide is a potent and selective agonist of TrkA and also induces its tyrosine phosphorylation and activation of downstream signaling, including Akt and MAPK. Gambogic amide specifically interacts with the cytoplasmic juxtamembrane domain of the TrkA receptor and triggers its dimerization, leading to activation. Gambogic amide has neuroprotective activity preventing glutamate-induced neuronal cell death. Gambogic amide has improved efficacy in a transient middle cerebral artery occlusion model of stroke and could be used to study neurodegenerative diseases and stroke .

HY-100434

PD-161570
PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC₅₀ of 39.9 nM and a K_i of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and *c-Src tyrosine* kinases with IC₅₀ values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor** phosphorylation with IC₅₀s of 450 nM and 622 nM, respectively . PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor .

HY-17600

Acalabrutinib 15+ Cited Publications ACP-196	Btk	Cancer
Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL) . Acalabrutinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-17600S

Acalabrutinib-d4 ACP-196-d₄	Btk	Cancer
Acalabrutinib-d₄ is a deuterium labeled Acalabrutinib. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor[1]. Acalabrutinib-d4 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-110193

SPP-86 1 Publications Verification	RET	Cancer
SPP-86 is a potent and selective cell permeable inhibitor of *RET tyrosine* kinase, with an IC₅₀** of 8 nM. SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells . SPP-86 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-13775

XL019 4 Publications Verification	JAK Apoptosis	Cancer
XL019 is a potent, orally active, and selective JAK2 inhibitor, with IC₅₀s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2 .

HY-123450

S116836	Bcr-Abl Apoptosis PDGFR	Cancer
S116836, a potent, orally active BCR-ABL tyrosine kinase inhibitor, blocks both wild-type as well as T315I Bcr-Abl. S116836 arrests the cells in the G0/G1 phase of cell cycle, induces apoptosis, increases ROS production, and decreases GSH production in BaF3/WT and BaF3/T315I cells. S116836 also inhibits SRC, LYN, HCK, LCK and BLK, and receptor tyrosine kinases such as FLT3, TIE2, KIT, PDGFR-β. Antitumor activies . S116836 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-109041

Razuprotafib 1 Publications Verification AKB-9778	Phosphatase Tie	Inflammation/Immunology
Razuprotafib (AKB-9778) is a potent and selective inhibitor of the catalytic activity of *VE-PTP (vascular endothelial protein tyrosine* phosphatase) with an IC₅₀*of 17 pM. Razuprotafib promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation* of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib inhibits the structurally related phosphatase PTP1B with an IC₅₀ of 780 nM. Razuprotafib shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC₅₀=36 pM) and HPTPγ (100 pM) .

HY-50895

Gefitinib Maximum Cited Publications 112 Publications Verification 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-117049

Leucettine L41	CDK DYRK	Neurological Disease
Leucettine L41 is a potent inhibitor of *dual-specificity tyrosine* phosphorylation-regulated kinase 1A (DYRK1A), DYRK2, CDC-like kinase 1 (CLK1), and CLK3 (IC₅₀**s = 0.04, 0.035, 0.015, and 4.5 µM, respectively) . Leucettine L41 prevents lipid peroxidation and the accumulation of reactive oxygen species (ROS) induced by Aβ_25-35 in the hippocampus in a mouse model of Alzheimer’s disease-like toxicity. Leucettine L41 also prevents memory deficits induced by Aβ_25-35 in the same model .

HY-13342AS

Apatinib-d8 free base YN968D1-d₈ free base	Src VEGFR Autophagy c-Kit RET	Cancer
Apatinib-d₈ (free base) is the deuterium labeled Apatinib free base[1]. Apatinib free base (YN968D1 free base) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 (IC50=1 nM). Apatinib free base (YN968D1 free base) is an anti-angiogenic drug for the research of advanced or metastatic gastric cancer. Apatinib free base (YN968D1 free base) potently inhibits Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. It also inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ[2][3][4].

HY-136882

TM-1	PDHK	Cancer
TM-1 is a potent inhibitor of pyruvate dehydrogenase kinase (PDHK1). TM-1 inhibits PDHK1 and PDHK2 with IC₅₀s of 2.97 μM and 5.2 μM, respectively. TM-1 blocks pyruvate dehydrogenase complex (PDHC) phosphorylation, and inhibits cell proliferation .

Cat. No.	Product Name

HY-L081

Phosphatase Inhibitor Library

132 compounds

Protein phosphorylation is a key post-translational modification underlying the regulation of many cellular processes. Phosphatases and kinases contribute to the regulation of protein phosphorylation homeostasis in the cell. This reversible regulation of protein phosphorylation is critical for the proper control of a wide range of cellular activities, including cell cycle, proliferation and differentiation, metabolism, cell-cell interactions, etc.

Protein phosphatases have evolved in separate families that are structurally and mechanistically distinct. Based on substrate specificity and functional diversity, protein phosphatases are classified into two superfamilies: Protein serine/threonine phosphatases and Protein tyrosine phosphatases. Ser/Thr phosphatases are metalloenzymes belonging to two major gene families termed PPP (phosphoprotein phosphatase) and PPM (metal-dependent protein phosphatases), whereas protein tyrosine phosphatases (PTPs) belong to distinct classes of enzymes that utilize a phospho-cysteine enzyme intermediate as a part of their catalytic action.

MCE supplies a unique collection of 132 phosphatase inhibitors that mainly targeting protein tyrosine phosphatases (PTPs) and serine/threonine-specific protein phosphatases. MCE Phosphatase Inhibitor Library is a useful tool for phosphatase drug discovery and related research.

HY-L024

Histone Modification Research Compound Library

614 compounds

A histone modification, a covalent post-translational modification (PTM) to histone proteins, includes methylation, phosphorylation, acetylation, ubiquitylation, and sumoylation, etc. In general, histone modifications are catalyzed by specific enzymes that act predominantly at the histone N-terminal tails involving amino acids such as lysine or arginine, as well as serine, threonine, tyrosine, etc. The PTMs made to histones can impact gene expression by altering chromatin structure or recruiting histone modifiers. Histone modifications act in diverse biological processes such as transcriptional activation/inactivation, chromosome packaging, and DNA damage/repair. Deregulation of histone modification contributes to many diseases, including cancer and autoimmune diseases.

MCE owns a unique collection of 614 bioactive compounds targeting Epigenetic Reader Domain, HDAC, Histone Acetyltransferase, Histone Demethylase, Histone Methyltransferase, Sirtuin, etc. Histone Modification Research Compound Library is a useful tool for histone modification research and drug screening.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0755

Rhoifolin	Structural Classification Rhus succedanea Flavonoids Classification of Application Fields Flavones Plants Disease Research Fields Endocrinology Cancer Anacardiaceae	Insulin Receptor GLUT NF-κB p38 MAPK Autophagy
Rhoifolin is a flavone glycoside can be isolated from Rhus succedanea. Rhoifolin has anti-diabetic effect acting through enhanced adiponectin secretion, tyrosine phosphorylation of insulin receptor-β and glucose transporter 4 (GLUT 4) translocation. Rhoifolin has an anti-inflammatory action via multi-level regulation of inflammatory mediators. Rhoifolin ameliorates titanium particle-stimulated osteolysis and attenuates osteoclastogenesis via RANKL-induced NF-κB and MAPK pathways. Rhoifolin also has cytotoxic activity against different cancer cell lines .

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* .

HY-N3550

Catalponol	Other Terpenoids Catalpa ovata G. Don Classification of Application Fields Terpenoids Source classification Plants Bignoniaceae Disease Research Fields Cancer	Others
Catalponol is a naphthoquinone derivative. Catalponol enhances dopamine biosynthesis by inducing tyrosine hydroxylase activity. Catalponol also increases the levels of cAMP and tyrosine hydroxylase phosphorylation in PC12 cells .

HY-124404A

12(S)-HETE	Structural Classification Ketones, Aldehydes, Acids Source classification Endogenous metabolite	ERK DNA/RNA Synthesis p38 MAPK
12(S)-HETE is the 12-lipoxygenase metabolite of arachidonic acid and has a mitogenic effect on cancer cell proliferation. 12(S)-HETE induces tyrosine phosphorylation of cellular proteins, promotes ERK and P38 MAPK phosphorylation, increases DNA synthesis, and stimulates the proliferation of pancreatic cancer cells .

Species:	Human (7)
Tag:	His (3) Tag Free (1) GST (4) Flag (1)
Source:	Sf9 insect cells (4) E. coli (3)

Cat. No.	Compare	Product Name	Species	Source

HY-P701672

	DYRK2 Protein, Human (GST) DYRK2; Dual specificity tyrosine-phosphorylation-regulated kinase 2	Human	E. coli
	DYRK2 is a multifunctional serine/threonine protein kinase that complexly controls multiple cellular processes, including the mitotic cell cycle, cell proliferation, apoptosis, cytoskeletal organization, and neurite outgrowth. DYRK2 operates downstream of ATM to phosphorylate p53/TP53 at the “Ser-46” site, leading to DNA damage-induced apoptosis. DYRK2 Protein, Human (GST) is the recombinant human-derived DYRK2 protein, expressed by E. coli , with N-GST labeled tag. The total length of DYRK2 Protein, Human (GST) is 600 a.a., .

HY-P701673

	DYRK4 Protein, Human (Sf9, GST) DYRK4; Dual specificity tyrosine-phosphorylation-regulated kinase 4	Human	Sf9 insect cells
	The DYRK4 protein may play a non-essential role in spermatogenesis, suggesting involvement in sperm cell development. Although specific functions and molecular mechanisms are unknown, its association with spermatogenesis suggests that it plays a role in complex pathways controlling male germ cell maturation. DYRK4 Protein, Human (Sf9, GST) is the recombinant human-derived DYRK4 protein, expressed by Sf9 insect cells , with GST tagged.

HY-P701674

	DYRK4 Protein, Human (Sf9, His, FLAG) DYRK4; Dual specificity tyrosine-phosphorylation-regulated kinase 4	Human	Sf9 insect cells
	The DYRK4 protein may play a non-essential role in spermatogenesis, suggesting involvement in sperm cell development. Although specific functions and molecular mechanisms are unknown, its association with spermatogenesis suggests that it plays a role in complex pathways controlling male germ cell maturation. DYRK4 Protein, Human (Sf9, His, FLAG) is the recombinant human-derived DYRK4 protein, expressed by Sf9 insect cells , with N-Flag, N-8*His labeled tag. The total length of DYRK4 Protein, Human (Sf9, His, FLAG) is 520 a.a., .

HY-P76308

	DYRK3 Protein, Human (sf9, His-GST) Dual specificity tyrosine-phosphorylation-regulated kinase 3; REDK; DYRK3	Human	Sf9 insect cells
	DYRK3 is a dual-specificity protein kinase that dissociates membraneless organelles such as stress granules and nuclear speckles in mitosis. DYRK3 Protein, Human (sf9, His-GST) is the recombinant human-derived DYRK3 protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag. The total length of DYRK3 Protein, Human (sf9, His-GST) is 588 a.a., with molecular weight of ~80 KDa.

HY-P701670

	DYRK1B Protein, Human (Sf9, GST) DYRK1B; Dual specificity tyrosine-phosphorylation-regulated kinase 1B; Minibrain-related kinase; Mirk protein kinase	Human	Sf9 insect cells
	DYRK1B protein has dual serine/threonine and tyrosine kinase activities. DYRK1B Protein, Human (Sf9, GST) is the recombinant human-derived DYRK1B protein, expressed by Sf9 insect cells , with N-GST labeled tag. The total length of DYRK1B Protein, Human (Sf9, GST) is 628 a.a., .

HY-P701667

	DYRK1A Protein, Human DYRK1A; Dual specificity tyrosine-phosphorylation-regulated kinase 1A; Dual specificity YAK1-related kinase; HP86; Protein kinase minibrain homolog; MNBH; hMNB	Human	E. coli
	DYRK1A protein has dual serine/threonine and tyrosine kinase activities. DYRK1A Protein, Human is the recombinant human-derived DYRK1A protein, expressed by E. coli , with tag free. The total length of DYRK1A Protein, Human is 359 a.a., .

HY-P701668

	DYRK1A Protein, Human (His) DYRK1A; Dual specificity tyrosine-phosphorylation-regulated kinase 1A; Dual specificity YAK1-related kinase; HP86; Protein kinase minibrain homolog; MNBH; hMNB	Human	E. coli
	DYRK1A protein has dual serine/threonine and tyrosine kinase activities. DYRK1A Protein, Human (His) is the recombinant human-derived DYRK1A protein, expressed by E. coli , with N-6*His labeled tag. The total length of DYRK1A Protein, Human (His) is 359 a.a., .

Cat. No.	Product Name	Chemical Structure

HY-50878S

Crizotinib-d5

Crizotinib-d₅ is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .

HY-17600S

Acalabrutinib-d4
Acalabrutinib-d₄ is a deuterium labeled Acalabrutinib. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor[1]. Acalabrutinib-d4 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-13342AS

Apatinib-d8 free base

Apatinib-d₈ (free base) is the deuterium labeled Apatinib free base[1]. Apatinib free base (YN968D1 free base) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 (IC50=1 nM). Apatinib free base (YN968D1 free base) is an anti-angiogenic drug for the research of advanced or metastatic gastric cancer. Apatinib free base (YN968D1 free base) potently inhibits Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. It also inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ[2][3][4].

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