product name AZ191
Description: AZ191 is a potent and selective DYRK1B inhibitor with IC50 of 17 nM in a cell-free assay, about 5- and 110-fold selectivity over DYRK1A and DYRK2, respectively. 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.
References: Biochem J. 2014 Jan 1;457(1):43-56.
429.52
Formula
C24H27N7O
CAS No.
1594092-37-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 86 mg/mL (200.2 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: In HEK-293 cells, AZ191 at 1uM could’t inhibit DYRK1B autophospho-Tyr273 and selectively inhibited DYRK1B serine/threonine kinase activity. In HEK-293 cells co-expressing CCND1 with either DYRK1A or DYRK1B, AZ191 inhibited phosphorylation of CCND1 with greater potency for DYRK1B over DYRK1A at doses as low as 30–100 nM. AZ191 is a novel DYRK1B-selective inhibitor with ∼100-fold selectivity over DYRK2 and 5–10-fold selectivity over DYRK1A. AZ191 will be used as a useful probe for defining DYRK1B functions and DYRK1B substrates. |
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| In Vivo | |
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| Formulation & Dosage | |
| References | Biochem J. 2014 Jan 1;457(1):43-56. |
