激酶抑制剂
Protein kinases are enzymes that catalyze the transfer of phosphate groups from ATP molecules to various substrates. The process is known as phosphorylation. Kinases regulate many cellar functions, so the overaction of protein kinases in cancer cells may cause fast tumor growth. Thus, kinase-inhibiting molecules might act as antitumor agents and can be used in cancer treatments.
Kinase Inhibitor Library designed by our specialists contains 884 carefully selected small kinase inhibitors. It covers the wide scope of kinase targets and includes approved drugs, highly selective and broad-spectrum inhibitors, and the most recent discoveries.
Related terms: receptor tyrosine kinase, RTK, nRTK, CAMK, calcium/calmodulin-dependent protein kinase, mitogen-activated protein kinase, MAP, cyclin-dependent kinase, CDK, glycogen synthase kinase, GSK
Кinase action on substrate(Created by BioRender.com)
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Highlights
Fedratinib, approved 2019, cancer
Selective MAPK-14 inhibitor
H-7 is a broad spectrum kinase inhibitor
AAK1 and BMP2K inhibitor (2020)
Product Features
A set of 884 kinase inhibitors/modulators with sub-10 micromolar activity coefficient values for HTS/HCS programs.
The library is composed of ligands that target all major kinase classes: protein kinases, lipid kinases and carbohydrate kinases.
Kinase Inhibitors Library covers novel promising preclinical lead compounds, clinical candidates and approved drugs.
Calculated structural diversity of the collection: 0.85.
Comprehensive documentation with structures, trivial names, synonyms, activity coefficient values, types of action on target and references to original literature.
NMR and LCMS validated purity.
All the compounds are available in stock for hit follow-up.
The library is continuously updated.
Product Details
Format: 10 - 100 µL of 10 mM DMSO stock solutions; dry powders (1 mg);
Container: 384-well microplates;
Storage: - 18 °C;
Shipping: Dry ice.
Utility
High throughput screening (HTS);
High content screening (HCS);
Cherry picking.
