Search Result

Pathways Recommended:	Protein Tyrosine Kinase/RTK

Results for "

tyrosine phosphorylation

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Anaplastic lymphoma kinase (ALK) (8) Btk (3) DYRK (10) FLT3 (2) Syk (2) 5-HT Receptor (2) Adrenergic Receptor (1) Akt (4) Apoptosis (14) Autophagy (11) Bcl-2 Family (1) Bcr-Abl (1) c-Kit (2) c-Met/HGFR (9) Calcium Channel (3) CDK (3) Cyclic GMP-AMP Synthase (3) DNA/RNA Synthesis (1) Drug Metabolite (1) EGFR (20) Enterovirus (1) Epigenetic Reader Domain (1) ERK (8) FGFR (2) Fungal (1) GLUT (2) GSK-3 (1) Histone Acetyltransferase (1) Insulin Receptor (5) Isotope-Labeled Compounds (4) JAK (5) MAP3K (1) MAP4K (1) Mitosis (4) NF-κB (3) p38 MAPK (4) PDGFR (4) PDHK (1) PERK (1) Phosphatase (5) PI3K (1) PKA (3) Reference Standards (5) RET (6) ROS Kinase (7) SHP2 (1) Src (3) STAT (5) TGF-β Receptor (1) Tie (1) Trk Receptor (4) Tyrosinase (2) VEGFR (3) Wnt (1)
By Research Areas:	Cancer (64) Cardiovascular Disease (8) Endocrinology (3) Infection (2) Inflammation/Immunology (10) Metabolic Disease (8) Neurological Disease (9)
Click Chemistry:	Alkynes (1)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Recombinant Proteins

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: Oxidative Phosphorylation Tyrosine Hydroxylase DYRK Btk Syk Pyk2 TNK1 BRK FAK FLT3 Anaplastic lymphoma kinase (ALK)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-101246

RPI-1	RET	Cancer
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-20878

Tyrphostin AG 879 2 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 5 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-124152

3,4-Dephostatin Methyl-3,4-dephostatin	MAP3K MAP4K Phosphatase	Neurological Disease
3,4-Dephostatin (Methyl-3,4-dephostatin) is an inhibitor of protein-tyrosine phosphatase (PTPase). 3,4-Dephostatin accelerates nerve growth factor (NGF)-induced neurite formation in PC12h cells. 3,4-Dephostatin sustains the NGF-induced tyrosine phosphorylation of proteins, most prominently that of mitogen-activated protein (MAP) kinase. 3,4-Dephostatin also prolongs epidermal growth factor (EGF)-induced tyrosine phosphorylation and activation of MAP kinase .

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-N0755R

Rhoifolin (Standard)	Reference Standards Insulin Receptor GLUT NF-κB p38 MAPK Autophagy	Metabolic Disease Endocrinology Cancer
Rhoifolin (Standard) is the analytical standard of Rhoifolin. This product is intended for research and analytical applications. 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-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 70+ 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-50878A

Crizotinib hydrochloride 70+ 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-50878R

Crizotinib (Standard) PF-02341066 (Standard)	Reference Standards Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy	Cancer
Crizotinib (Standard) is the analytical standard of Crizotinib. This product is intended for research and analytical applications. 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-135725

D-69491 hydrochloride	EGFR	Cancer
D-69491 hydrochloride is a HER-2 tyrosine kinase inhibitor that reduces HER-2 phosphorylation, inhibits the proliferation of SKOV-3 cells, and has anticancer activity .

HY-164413

CLM3	VEGFR EGFR RET Apoptosis	Cancer
CLM3, a pyrazolopyrimidine derivative, is a multiple *tyrosine* kinase inhibitor. CLM3 shows antiproliferative and proapoptotic activity on endothelial and cancer cells, synergistically enhanced by SN38 (HY-13704). These effects are mainly due to its inhibition of phosphorylation of VEGFR-2, EGFR and RET tyrosine kinases and their related signaling pathways .

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-50878S2

Crizotinib-d9 PF-02341066-d₉	Isotope-Labeled Compounds	Cancer
Crizotinib-d₉ (PF-02341066-d₉) is 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-50878S1

Crizotinib-d8 PF-02341066-d₈	Isotope-Labeled Compounds ROS Kinase Autophagy c-Met/HGFR Anaplastic lymphoma kinase (ALK)	Cancer
Crizotinib-d₈ (PF-02341066-d₈) is 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-108330

AG126 3 Publications Verification Tyrphostin AG126	ERK Mitosis	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-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-N0737A

Harmine 20+ Cited Publications Telepathine	DYRK 5-HT Receptor	Neurological Disease Cancer
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-176723

RD0392	DYRK	Neurological Disease
RD0392 (Compound 5) is a competitive tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitor (IC₅₀=1.3 nM). RD0392 is promising for research of neurodegenerative diseases like Alzheimer’s .

HY-50878AS

Crizotinib-d9 hydrochloride PF-02341066-d₉ hydrochloride	c-Met/HGFR Autophagy Anaplastic lymphoma kinase (ALK) ROS Kinase Isotope-Labeled Compounds	Cancer
Crizotinib-d₉ hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). 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-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-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-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-129510

4-Methyl erlotinib	EGFR Mitosis	Cancer
4-Methyl erlotinib, is a potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. 4-Methyl erlotinib potently inhibits EGF-mediated tumor cell mitosis by reducing EGFr-specific tyrosine phosphorylation. Using a mouse model of human tumor transplantation, 4-Methyl erlotinib demonstrated significant and sustained suppression of EGFr phosphotyrosine levels, resulting in significant growth inhibition of EGFr-dependent human cancers .

HY-123856

MY10	Phosphatase NF-κB c-Met/HGFR Anaplastic lymphoma kinase (ALK)	Cardiovascular Disease Neurological Disease
MY10 is a potent and orally active *receptor protein tyrosine* phosphatase (RPTPβ/ζ) inhibitor. MY10 reduces NF-κB p65** expression. MY10 activates tyrosine phosphorylation of c-Met. MY10 prevents the alcohol-induced downregulation of Ptprz1 and Alk expression. MY10 attenuates binge-like ethanol consumption and ethanol reward. MY10 can be used in the study of neurological and vascular diseases .

HY-N0737AR

Harmine (Standard) Telepathine (Standard)	Reference Standards DYRK 5-HT Receptor	Neurological Disease Cancer
Harmine (Standard) is the analytical standard of Harmine. This product is intended for research and analytical applications. 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-HT2A serotonin receptor, with an Ki of 397 nM .

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-101084

NSC 228155 10+ 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-108330R

AG126 (Standard)	ERK Mitosis	Inflammation/Immunology
AG126 (Standard) is the analytical standard of AG126. This product is intended for research and analytical applications. 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-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-168265

Dyrk1A-IN-11	DYRK	Neurological Disease Cancer
Dyrk1A-IN-11 (compound 166) is a potent *dual-specificity tyrosine* phosphorylation- regulated 1A (DYRK1A) inhibitor with an EC₅₀** value of 0.0021 µM. Dyrk1A-IN-11 inhibits the Phospho-Tau (Thr212) with an EC₅₀ value of 0.0361 µM .

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-121874

EP009	JAK	Cancer
EP009 is a JAK3 inhibitor that selectively inhibits IL-2-mediated JAK3 tyrosine phosphorylation (IC50=10-20 μM in Kit225 cells) without affecting IL-3-induced JAK2 phosphorylation (up to 50 μM in BaF/3 cells). EP009 significantly reduced Kit225 cell viability (72 h, LD50=5.0 μM) while having no effect on BaF/3 cells. .

HY-137443

Ipivivint	CDK Wnt	Cancer
Ipivivint (Compound 38) is an orally active and potent CDC-like kinase (CLK) inhibitor with EC₅₀ of 1 nM and 7 nM for CLK2 (human) and CLK3 (human), respectively. Ipivivint also inhibits the Wnt pathway (EC50=13 nM) and tyrosine phosphorylation-regulated kinase 1A (human) (EC₅₀=5 nM) .

HY-168339

Tyk2-IN-22	JAK	Inflammation/Immunology
Tyk2-IN-22 (Compound A8) is a selective inhibitor for tyrosine kinase 2 (Tyk2), that it inhibits Tyk2, JAK1, and JAK3 with IC₅₀s of 9.7, 148.6, and 883.3 nM, respectively. Tyk2-IN-22 inhibits the downstream STAT5 phosphorylation .

HY-153991

STAT6-IN-2	STAT	Inflammation/Immunology
STAT6-IN-2 (Compound R-84) is a STAT6 inhibitor that can inhibit the tyrosine phosphorylation of STAT6. STAT6-IN-2 can also inhibit the secretion of eotaxin-3. STAT6-IN-2 can be used in the research of immune diseases and allergic inflammatory diseases such as asthma .

HY-115605

CN009543V	EGFR p38 MAPK ERK Phosphatase	Cancer
CN009543V is an epidermal growth factor receptor (EGFR) agonist. CN009543V enhances tyrosine phosphorylation of EGFR at Tyr1068 and Tyr1173, thereby activating the MAPK/ERK cascade. CN009543V inhibits the activity of PTP-1B in MDA MB468 cells. CN009543V can be used in cancer research .

HY-101960A

Tyrphostin A51 1 Publications Verification AG-183	EGFR	Cancer
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-129510R

4-Methyl erlotinib (Standard)	EGFR Mitosis Reference Standards	Cancer
4-Methyl erlotinib (Standard) is the analytical standard of 4-Methyl erlotinib. This product is intended for research and analytical applications. 4-Methyl erlotinib, is a potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. 4-Methyl erlotinib potently inhibits EGF-mediated tumor cell mitosis by reducing EGFr-specific tyrosine phosphorylation. Using a mouse model of human tumor transplantation, 4-Methyl erlotinib demonstrated significant and sustained suppression of EGFr phosphotyrosine levels, resulting in significant growth inhibition of EGFr-dependent human cancers .

HY-50683

JNJ-38877605 4 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-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-101798

MDVN1003	PI3K	Cancer
MDVN1003 is a Bruton's tyrosine kinase (BTK) and phosphatidylinositol-3-kinase delta (PI3Kδ) dual inhibitor which prevents the activation of B cells and inhibits the phosphorylation of protein kinase B (AKT) and extracellular signal-regulated kinase 1/2 (ERK 1/2). MDVN1003 can be used for non-Hodgkin’s lymphoma (NHL) research .

Cat. No.	Product Name

HY-L081

Phosphatase Inhibitor Library

155 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 155 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

786 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 786 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	Target	Research Area

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 .

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 Anacardiaceae Cancer	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-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 .

HY-N0737A

Harmine 20+ Cited Publications Telepathine	Alkaloids Structural Classification Zygophyllaceae Peganum harmala Linn. Source classification Plants Indole Alkaloids	DYRK 5-HT Receptor
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-N0737AR

Harmine (Standard) Telepathine (Standard)	Alkaloids Structural Classification Zygophyllaceae Peganum harmala Linn. Source classification Plants Indole Alkaloids	Reference Standards DYRK 5-HT Receptor
Harmine (Standard) is the analytical standard of Harmine. This product is intended for research and analytical applications. 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-HT2A serotonin receptor, with an Ki of 397 nM .

HY-N12625

(R)-(+)-O-Demethylbuchenavianine	Structural Classification Alkaloids Flavonoids Flavones Other Alkaloids Buchenavia macrophylla Spruce ex Eichler Combretaceae Source classification Plants	CDK DYRK GSK-3
(R)-(+)-O-Demethylbuchenavianine is an inhibitor for Cyclin-dependent kinases (CDK). (R)-(+)-O-Demethylbuchenavianine inhibits CDK1, CDK5, glycogen synthase kinase-3 (GSK3), cdc2-like kinase (CLK1) and dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A), with IC₅₀s of 1.1, 0.95, >10, >10 and >10 μM, respectively .

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* .

HY-N3550

Catalponol	Other Terpenoids Structural Classification Catalpa ovata G. Don Classification of Application Fields Terpenoids Source classification Bignoniaceae Plants 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-N0755R

Rhoifolin (Standard)	Structural Classification Rhus succedanea Flavonoids Flavones Plants Anacardiaceae	Reference Standards Insulin Receptor GLUT NF-κB p38 MAPK Autophagy
Rhoifolin (Standard) is the analytical standard of Rhoifolin. This product is intended for research and analytical applications. 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 .

Species:	Human (6)
Tag:	His (3) Tag Free (1) GST (3) Flag (1)
Source:	Sf9 insect cells (3) E. coli (3)

Cat. No.	Compare	Product Name	Species	Source

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.

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.

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.

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.

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.

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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 . 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 . 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 .

HY-50878S2

Crizotinib-d9

Crizotinib-d₉ (PF-02341066-d₉) is 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-50878S1

Crizotinib-d8

Crizotinib-d₈ (PF-02341066-d₈) is 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-50878AS

Crizotinib-d9 hydrochloride

Crizotinib-d₉ hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). 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-169984S

Tyk2-IN-22-d3
Tyk2-IN-22-d3 (Compound 1) is the deuterated analog of Tyk2-IN-22 (HY-168339). Tyk2-IN-22 (Compound A8) is a selective inhibitor for tyrosine kinase 2 (Tyk2), that it inhibits Tyk2, JAK1, and JAK3 with IC₅₀s of 9.7, 148.6, and 883.3 nM, respectively. Tyk2-IN-22 inhibits the downstream STAT5 phosphorylation .

Cat. No.	Product Name		Classification