| Name | AZ191 |
| Description | AZ191(IC50 of 17 nM) is an effective and specific DYRK1B inhibitor. The specificity of AZ191 for DYRK1B is about 5- and 110-fold greater over DYRK1A and DYRK2, respectively. |
| Kinase Assay | Biochemical Binding Affinity – HTRF Assay: The p53-MDM2 HTRF assay is performed in buffer containing 50 mM Tris-HCl, pH 7.4, 100 mM NaCl, 1 mM DTT, 0.02 or 0.2 mg/ml BSA. Small-molecule inhibitors are stored in aliquots as 10 mM stock solutions in DMSO at 4°C in 96-deep-well plates. It is thawed and mixed immediately prior to testing. The compound is incubated with GST-MDM2 and a biotinylated p53 peptide for one hour at 37°C. Phycolink goat anti-GST (Type 1) allophycocyanin and Eu-8044-streptavidin are then added and followed by one hour incubation at room temperature. Plates are read using the Envision fluorescence reader. IC50 values are determined from inter-plate duplicate or triplicate sets of data. Data are analyzed by XLfit4 (Microsoft) using a 4 Parameter Logistic Model (Sigmoidal Dose-Response Model) and the equation Y= (A+ ((B-A)/ (1+ ((C/x)^D)))), where A and B are enzyme activity in the absence or presence of infinite inhibitor compound, respectively, C is the IC50 and D is the Hill coefficient. |
| In vitro | AZ191 selectively inhibits DYRK1B serine/threonine kinase activity with no effect on tyrosine kinase autophosphorylation. In HEK-293 cells, AZ191 also displays much greater potency for DYRK1B over DYRK1A, inhibiting CCND1 phosphorylation. In HD1B cells, AZ191 strongly inhibits the levels of the cell-cycle regulators, p21Cip1 and p27Kip1, and increases cell-cycle progression. [1] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.66 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 1 mg/mL (2.33 mM), Sonication is recommended.
DMSO : 79 mg/mL (183.93 mM), Sonication is recommended.
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| Keywords | Inhibitor | inhibit | DYRK2 | DYRK1B | DYRK1A | DYRK | Dual specificity tyrosine regulated kinase | Dual specificity tyrosine phosphorylation regulated kinase | AZ-191 | AZ191 | AZ 191 |
| Inhibitors Related | ML 315 | EHT 1610 | ARN25068 | MBM-55S | CK2/ERK8-IN-1 | YK-2-69 | AnnH31 | GNF4877 | Harmine hydrochloride | 2-Amino-4-hydroxypyrrolo[2,3- d]pyrimidi | RD0392 | LDN-192960 |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Multi-Target Compound Library | Post-Translational Modification Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Cell Cycle Compound Library | Anti-Cancer Compound Library |
United States
