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Results for "

serine-threonine kinase activity

" in MedChemExpress (MCE) Product Catalog:

By Targets:	MASTL (1) Ser/Thr Kinase (1) Apoptosis (5) ATM/ATR (2) Autophagy (3) Bacterial (1) Biochemical Assay Reagents (1) c-Fms (2) c-Kit (2) c-Met/HGFR (1) Casein Kinase (1) CDK (2) EGFR (1) FLT3 (3) IGF-1R (2) Insulin Receptor (2) MAP4K (1) Parasite (1) PD-1/PD-L1 (2) PDGFR (2) Pim (1) PKC (1) Polo-like Kinase (PLK) (1) Reference Standards (2) RIP kinase (1) Ser/Thr Protease (3) STING (2) VEGFR (3)
By Research Areas:	Cancer (15) Cardiovascular Disease (3) Endocrinology (2) Infection (2) Inflammation/Immunology (7) Neurological Disease (1)

Inhibitors & Agonists

Screening Libraries

Peptides

Targets Recommended: Ser/Thr Kinase STK33 Microtubule‐associated serine/threonine kinase (MAST) FASTK TSSK MASTL PASK/STK37

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-50751

Linifanib 5 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-11107

PHA-665752 Maximum Cited Publications 14 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-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-150617

Lartesertib 1 Publications Verification M4076; ATM Inhibitor-5	ATM/ATR STING PD-1/PD-L1	Cardiovascular Disease Inflammation/Immunology Cancer
Lartesertib (M4076) is an inhibitor of the serine/threonine protein kinase ATM with high potency. Lartesertib can inhibit the growth of multiple hematopoietic cell lines. Additionally, when combined with the ATR inhibitor Tuvusertib (HY-111451), Lartesertib can promote the death of tumor cells, activate the immune signaling pathway, and exhibit anti-tumor activity .

HY-137552

MKI-1 1 Publications Verification MASTL kinase Inhibitor-1	MASTL	Cancer
MKI-1, an inhibitor of MASTL (microtubule-associated serine/threonine kinase-like) with an IC₅₀ of 9.9 μM, exerts antitumor and radiosensitizer activities through PP2A activation in breast cancer .

HY-139439

SBI-581	Ser/Thr Protease	Cancer
SBI-581 is an orally active and potent selective serine-threonine kinase TAO3 inhibitor, with an IC₅₀ of 42 nM. SBI-581 promotes TKS5α accumulation at RAB11-positive vesicles. SBI-581 inhibits invadopodia formation. SBI-581 shows reasonable pharmacokinetics in mice using IP injection. SBI-581 shows antitumor activity . SBI-581 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-P4484

Suc-AAPK-pNA	Biochemical Assay Reagents	Others
Suc-AAPK-pNA is a chromogenic substrate for the determination of serine/threonine kinase activity and enzyme kinetic parameters .

HY-147404

Tilpisertib fosmecarbil GS 5290	Ser/Thr Protease	Inflammation/Immunology
Tilpisertib fosmecarbil (GS 5290) is a potent **serine/threonine kinase** inhibitor. Tilpisertib fosmecarbil has anti-inflammatory activity .

HY-116611

IMB-YH-8	Ser/Thr Kinase Bacterial	Infection
IMB-YH-8 is a serine/threonine protein kinase (PknB) inhibitor. IMB-YH-8 has strong antibacterial activity against Mycobacterium tuberculosis (MIC = 0.25 µg/mL). IMB-YH-8 can be used in the research of tuberculosis .

HY-50751R

Linifanib (Standard) ABT-869 (Standard); AL-39324 (Standard)	PDGFR VEGFR FLT3 c-Fms c-Kit Autophagy Apoptosis Reference Standards	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-147404A

Tilpisertib fosmecarbil TFA GS 5290 TFA	Ser/Thr Protease	Inflammation/Immunology
Tilpisertib fosmecarbil TFA (GS 5290 TFA) is a potent **serine/threonine kinase** inhibitor. Tilpisertib fosmecarbil TFA has anti-inflammatory activity .

HY-159123

KHK-6	MAP4K	Cancer
KHK-6 is an inhibitor for serine/threonine kinase *hematopoietic progenitor kinase* 1 (HPK 1) with an IC₅₀** of 20 nM. KHK-6 enhances CD3/CD28-induced cytokine production, enhances CD69, CD25 and HLA-DR markers on CD4+ and CD8+ T cells, and enhances T cell-mediated killing activity of SKOV3 and A549 cells .

HY-150617A

(Rac)-Lartesertib (Rac)-M4076; (Rac)-ATM Inhibitor-5	ATM/ATR STING PD-1/PD-L1	Cardiovascular Disease Inflammation/Immunology Cancer
(Rac)-Lartesertib ((Rac)-M4076) is an isoform of Lartesertib (HY-150617). Lartesertib (M4076) is an inhibitor of the serine/threonine protein kinase ATM with high potency. Lartesertib can inhibit the growth of multiple hematopoietic cell lines. Additionally, when combined with the ATR inhibitor Tuvusertib (HY-111451), Lartesertib can promote the death of tumor cells, activate the immune signaling pathway, and exhibit anti-tumor activity .

HY-E70691

CLK1 Recombinant Human Active Protein Kinase	CDK	Cancer
CLK1 is one of the dual specificity kinases and is the founding member of the 'LAMMER' family of kinases. CLK1 activity is positively regulated by phosphorylation on either tyrosine residues or serine/threonine residues, and is negatively regulated by steric constraints mediated by the N-terminal domain, as well as, by phosphorylation on a subset of serine/threonine residues within the catalytic domain. CLK1 Recombinant Human Active Protein Kinase is a recombinant CLK1 protein that can be used to study CLK1-related functions .

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-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-121634

DAP-81	Polo-like Kinase (PLK)	Others
DAP-81 is an inhibitory agent targeting Polo-like kinases (Plks), a class of evolutionarily conserved serine/threonine kinases. DAP-81 dose-dependently increases the number of monopolar spindles in treated cells. High-resolution live-cell microscopy revealed that Plk activity is required for the assembly and maintenance of bipolar mitotic spindles. Plk inhibition destabilizes centromeric microtubules while stabilizing other spindle microtubules, leading to the formation of monopolar spindles. Further testing of compounds based on "privileged scaffolds" such as the DAP scaffold may lead to the discovery of new cell division probes and anti-microtubule agents.

HY-162237

RIPK1-IN-22	RIP kinase	Inflammation/Immunology
RIPK1-IN-13 (compound 28) is a selective inhibitor for receptor-interacting serine/threonine-protein kinase 1 (RIPK1), the inhibitory activity is measured by ADP-Glo Kinase Assay with a pK_i of 7.66. RIPK1-IN-13 inhibits human leukaemia cells U937 with a pIC₅₀ of 7.2 .

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-120808

GSK2188764	Parasite	Infection
GSK2188764 is a Toxoplasma gondii rhoptry protein 18 (ROP18) inhibitor with reported IC₅₀ values of 7.49 μM against Toxoplasma gondii. GSK2188764 inhibits serine-threonine kinase activity of ROP18 in vitro.GSK2188764 can be used for the research of toxoplasmosis .

HY-10524R

GSK1904529A (Standard)	Reference Standards IGF-1R Insulin Receptor Apoptosis	Endocrinology Cancer
GSK1904529A (Standard) is the analytical standard of GSK1904529A (HY-10524). This product is intended for research and analytical applications. 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-123859

SR-2890	Casein Kinase FLT3 CDK	Neurological Disease Inflammation/Immunology Cancer
SR-2890 is a highly selective, ATP-competitive inhibitor of *casein kinase* CK1δ and CK1ε, with IC₅₀ values of 4 nM and 44 nM, respectively, and a K_i of 14 nM for CK1δ. SR-2890 exhibits antiproliferative effects. SR-2890 blocks the serine/threonine kinase** activity of CK1δ and weakly inhibits a few off-target kinases such as FLT3, CDK4. SR-2890 has an oral bioavailability of 10% and a blood-brain barrier penetration rate of <1%. SR-2890 demonstrates stable in vitro metabolism and favorable in vivo pharmacokinetic properties, effectively inhibiting the growth of human A375 melanoma cells. SR-2890 can be used in melanoma research and is also a useful compound for studying CK1δ/ε-related diseases such as Alzheimer's disease .

Cat. No.	Product Name

HY-L164

Serine/Threonine Kinase Inhibitor Library	2,186 compounds
Protein serine/threonine kinases (PSKs) are protein kinases that use ATP as a high-energy donor molecule to transfer phosphate groups to serine/threonine residues of target protein. As an important signal transduction regulator, serine/threonine kinases can affect the function of target proteins by disrupting enzyme activity or binding of target proteins to other proteins. Serine/threonine kinases are involved in the regulation of immune response, cell proliferation, differentiation, apoptosis and other physiological processes. Serine/threonine kinase inhibitors are an important class of compounds that have been widely studied in cancer, chronic inflammation, autoimmune diseases, aging and other diseases. MCE designs a unique collection of 2,186 serine/threonine kinase inhibitors, mainly targeting the receptor PKA, Akt, PKC, MAPK/ERK, etc, which is an effective tool for development and research of anti-cancer, anti-chronic inflammatory diseases, anti-autoimmune diseases and anti-aging compounds.

Serine/Threonine Kinase Inhibitor Library

2,186 compounds

Protein serine/threonine kinases (PSKs) are protein kinases that use ATP as a high-energy donor molecule to transfer phosphate groups to serine/threonine residues of target protein. As an important signal transduction regulator, serine/threonine kinases can affect the function of target proteins by disrupting enzyme activity or binding of target proteins to other proteins. Serine/threonine kinases are involved in the regulation of immune response, cell proliferation, differentiation, apoptosis and other physiological processes. Serine/threonine kinase inhibitors are an important class of compounds that have been widely studied in cancer, chronic inflammation, autoimmune diseases, aging and other diseases.

MCE designs a unique collection of 2,186 serine/threonine kinase inhibitors, mainly targeting the receptor PKA, Akt, PKC, MAPK/ERK, etc, which is an effective tool for development and research of anti-cancer, anti-chronic inflammatory diseases, anti-autoimmune diseases and anti-aging compounds.

HY-L081

Phosphatase Inhibitor Library	177 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 177 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

177 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 177 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.

Cat. No.	Product Name	Target	Research Area

HY-P4484

Suc-AAPK-pNA	Biochemical Assay Reagents	Others
Suc-AAPK-pNA is a chromogenic substrate for the determination of serine/threonine kinase activity and enzyme kinetic parameters .

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