Search Result

Pathways Recommended:	Protein Tyrosine Kinase/RTK

Results for "

tyrosine and serine kinases

" in MedChemExpress (MCE) Product Catalog:

By Targets:	FLT3 (2) Ser/Thr Kinase (2) Apoptosis (5) Autophagy (3) c-Fms (2) c-Kit (2) c-Met/HGFR (2) EGFR (3) IGF-1R (1) IKK (3) Insulin Receptor (2) JAK (1) PDGFR (2) Phosphatase (1) Pim (1) PKA (1) PKC (3) Ras (1) Tyrosinase (1) VEGFR (3)
By Research Areas:	Cancer (13) Cardiovascular Disease (1) Endocrinology (1) Inflammation/Immunology (3) Metabolic Disease (3)

Inhibitors & Agonists

Screening Libraries

Targets Recommended: Tyrosine Hydroxylase Serine Racemase (SR) Microtubule‐associated serine/threonine kinase (MAST) Btk Syk SRPK SHMT Ser/Thr Protease DYRK STK33 ASCT Ser/Thr Kinase Serpin MASTL Pyk2 TNK1 Fat Mass and Obesity-associated Protein (FTO) BRK Enteropeptidase FAK FLT3 Anaplastic lymphoma kinase (ALK)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-W013852

PKC-IN-6	Ser/Thr Kinase Tyrosinase PKA PKC EGFR	Cancer
PKC-IN-6 (Compound 21) is a selective inhibitor of **tyrosine and serine kinases. PKC-IN-6 shows inhibitory activity against PKC-α, PKC-δ, PKA, EGF-R with IC₅₀** values of 240, >500, >500, >100 μM, respectively. PKC-IN-6 is promising for research of cancers .

HY-401475

Protein kinase inhibitor 9	PKC	Cardiovascular Disease Inflammation/Immunology Cancer
Protein kinase inhibitor 9 (Compound example 175) is an inhibitor of **serine/threonine and tyrosine kinase** activity. Protein kinase inhibitor 9 can be used for the research of cancer, hyper proliferative disorders, rheumatoid arthritis, disorders of the immune system, transplant rejections and imflammatory disorders .

HY-W174279

Tyrphostin 8	EGFR Ras Phosphatase	Metabolic Disease
Tyrphostin 8 is a **tyrosine kinase, with an IC₅₀** of 560 μM for EGFR kinase. Tyrphostin 8 is also a GTPase inhibitor. Tyrphostin 8 can inhibit the protein serine/threonine phosphatase calcineurin (IC₅₀=21 μM) .

HY-13802

SC-514 5+ Cited Publications GK 01140	IKK	Cancer
SC-514 is a selective IKK-2 inhibitor (IC₅₀=11.2 μM), which does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.

HY-171291

Protein kinase inhibitor 14	Ser/Thr Kinase	Inflammation/Immunology Cancer
Protein kinase inhibitor 14 (Compound 13) exhibits inhibitory effects against a variety of serine/threonine kinase and receptor/non-receptor tyrosine kinase .

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-120857

BPIQ-II hydrochloride PD 158294	EGFR	Others
BPIQ-II is a linear imidazoloquinazoline that potently inhibits the tyrosine kinase activity of the epidermal growth factor receptor (EGFR; IC₅₀=8 pM). It is selective for EGFR over an assortment of other tyrosine and serine/threonine kinases. Cellular studies indicate that BPIQ-II can enter cells and very selectively shut down EGF-stimulated signal transmission by binding competitively at the ATP site of EGFR.

HY-164041

Staurosporine-Boc	PKC	Others
Staurosporine-Boc, a natural product isolated from the actinomyces Streptomyces staurosporeus, is a potent non-selective inhibitor of protein kinase. Staurosporine-Boc inhibits a variety of protein kinases, including protein kinase C (PKC), **tyrosine kinase*, and serine/threonine kinase*. Because of its broad inhibition profile, Staurosporine-Boc is widely used as a tool compound in biological research, especially when studying cell signaling pathways .

HY-107591B

PF-184	IKK	Inflammation/Immunology
PF-184 is a potent and selective IKK-2 inhibitor (IC₅₀: 37 nM) over rhIKK-1, IKKi, and more than 30 tyrosine and serine/threonine kinases. PF-184 can be used in the research of inflammation, such as asthma and chronic obstructive pulmonary disease .

HY-13802R

SC-514 (Standard)	IKK	Cancer
SC-514 (Standard) is the analytical standard of SC-514. This product is intended for research and analytical applications. SC-514 is a selective IKK-2 inhibitor (IC50=11.2 μM), which does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.

HY-11107

PHA-665752 Maximum Cited Publications 13 Publications Verification	c-Met/HGFR Autophagy Apoptosis	Cancer
PHA-665752 is a selective, ATP-competitive, and active-site inhibitor of the catalytic activity of c-Met kinase (K_i=4 nM; IC₅₀=9 nM). PHA-665752 exhibits >50-fold selectivity for c-Met compared with a panel of diverse tyrosine and serine-threonine kinases. PHA-665752 induces apoptosis and cell cycle arrest, and exhibits cytoreductive antitumor activity .

HY-13590

CEP-7055	VEGFR	Cancer
CEP-7055 (compound 21) is a novel vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase inhibitor with potent inhibitory activity. Studies have found that the inhibitor activity can be significantly improved by optimizing the R9 substituent. Compound 21 has potent low nanomolar inhibition of human VEGF-R tyrosine kinase and shows good selectivity against multiple tyrosine and serine/threonine kinases. N,N-dimethylglycine ester 40 was prepared to improve its water solubility and oral bioavailability. In animal pharmacokinetic studies, a significant increase in the plasma level of 21 was observed after oral administration of 40. Compound 21 showed significant in vivo antitumor activity in multiple tumor models and has entered phase I clinical trials as a water-soluble N,N-dimethylglycine ester proagent of 40 (CEP-7055).

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-50751

Linifanib 4 Publications Verification ABT-869; AL-39324	PDGFR VEGFR FLT3 c-Fms c-Kit Autophagy Apoptosis	Cancer
Linifanib (ABT-869) is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC₅₀s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib shows prominent antitumor activity. Linifanib has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib is a specific miR-10b inhibitor that blocks miR-10b biogenesis .

HY-10524

GSK1904529A 5+ Cited Publications	IGF-1R Insulin Receptor Apoptosis	Endocrinology Cancer
GSK1904529A is a potent, selective, orally active, and ATP-competitive inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR), with IC₅₀s of 27 and 25 nM, respectively. GSK1904529A shows poor activity (IC₅₀>1 μM) in 45 other serine/threonine and tyrosine kinases. GSK1904529A exhibits anti-tumor activity .

HY-16576A

SMI-4a 1 Publications Verification TCS-PIM-1-4a	Pim	Cancer
SMI-4a (TCS-PIM-1-4a) is a poten, selective, cell-permeable and ATP-competitive Pim-1 inhibitor with an IC₅₀ of 24 μM and a K_i of 0.6 μM. SMI-4a also inhibits Pim-2 (IC₅₀ of 100 μM), and does not significantly inhibit the other serine/threonine- or tyrosine-kinases. SMI-4a has anticancer activity .

HY-50751R

Linifanib (Standard)	PDGFR VEGFR FLT3 c-Fms c-Kit Autophagy Apoptosis	Cancer
Linifanib (Standard) is the analytical standard of Linifanib. This product is intended for research and analytical applications. Linifanib (ABT-869) is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC50s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib shows prominent antitumor activity. Linifanib has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib is a specific miR-10b inhibitor that blocks miR-10b biogenesis .

HY-13775

XL019 5 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 .

Cat. No.	Product Name

HY-L081

Phosphatase Inhibitor Library	157 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 157 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.

Phosphatase Inhibitor Library

157 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 157 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.

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