Chemical Structure
DYRK1A/B Inhibitor AnnH75
AG-CR1-3651
Overview
- SupplierAdipoGen Life Sciences
- Product NameDYRK1A/B Inhibitor AnnH75
- Delivery Days Customer10
- CertificationResearch Use Only
- Estimated Purity>98%
- Hazard InformationWarning
- Molecular FormulaC14H10ClN3O
- Molecular Weight271.7
- Scientific DescriptionChemical. Formula: C14H10ClN2O. MW: 271.7. Synthetic. Potent selective membrane-permeable DYRK1A (IC50=181nM) and DYRK1B inhibitor. Off-target inhibition of CLK1, CLK4 and Haspin/GSG2. Shows no inhibitory effects on monoamine oxidase A (MAO A). Inhibited the cotranslational tyrosine autophosphorylation of DYRK1A and threonine phosphorylation of an exogenous substrate protein with similar potency. Dose-dependently reduced the phosphorylation of three known DYRK1A substrates (SF3B1, SEPT4 and tau) without negative effects on cell viability in celular assays. Moderate inhibitor of CDK8, CLK2, GRK4, MEK2, PIM1, PIM3 and PKCepsilon. Shows minimal cytotoxic effects in HeLa and PC12 cells up to 10microM. The pleiotropic protein kinase DYRK1A has diverse functions in cell cycle control, neuronal differentiation and synaptic transmission and has attracted increasing interest as a potential drug target, due to its role in the pathology of Down syndrome, neurodegenerative diseases such as Alzheimers disease and cancer. The closely related kinase DYRK1B has been associated with cancer cell survival by arresting cells in a quiescent state to allow cellular repair and mutations in DYRK1B might be causative in metabolic syndrome. - Potent selective membrane-permeable DYRK1A (IC50=181nM) and DYRK1B inhibitor. Off-target inhibition of CLK1, CLK4 and Haspin/GSG2. Shows no inhibitory effects on monoamine oxidase A (MAO A). Inhibited the cotranslational tyrosine autophosphorylation of DYRK1A and threonine phosphorylation of an exogenous substrate protein with similar potency. Dose-dependently reduced the phosphorylation of three known DYRK1A substrates (SF3B1, SEPT4 and tau) without negative effects on cell viability in celular assays. Moderate inhibitor of CDK8, CLK2, GRK4, MEK2, PIM1, PIM3 and PKCepsilon. Shows minimal cytotoxic effects in HeLa and PC12 cells up to 10microM. The pleiotropic protein kinase DYRK1A has diverse functions in cell cycle control, neuronal differentiation and synaptic transmission and has attracted increasing interest as a potential drug target, due to its role in the pathology of Down syndrome, neurodegenerative diseases such as Alzheimers disease and cancer. The closely related kinase DYRK1B has been associated with cancer cell survival by arresting cells in a quiescent state to allow cellular repair and mutations in DYRK1B might be causative in metabolic syndrome.
- SMILESClC1=NC=CC2=C1N(CC#N)C3=CC(OC)=CC=C32
- Storage Instruction-20°C,2°C to 8°C
- UNSPSC51202000
References
- Selectivity profiling and biological activity of novel beta-carbolines as potent and selective DYRK1 kinase inhibitors: K. Ruben, et al.; PLos One 10, e0132453 (2015)