AZ191

Catalog No.S7338

AZ191 Chemical Structure

Molecular Weight(MW): 429.52

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.

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Cited by 5 Publications

3 Customer Reviews

  • In (e), quiescent cells were left untreated or treated for 30 min with 10 nM R1881, in the absence or presence of the DYRK 1B inhibitor AZ191, which was added (1 μM) 15 min before hormonal stimulation. Control cells in right panel were treated with the inhibitor alone. In left panels, lysate proteins were immunoprecipitated with anti-DYRK 1B antibody. Immune complexes were analyzed for DYRK 1B activity using MBP as a substrate. DYRK 1B levels in immune complexes were detected by immunoblot with anti-DYRK 1B antibody. In right panels, lysate proteins were analyzed by western blot, using antibodies against the indicated proteins.

    Cell Death Dis, 2014, 5:e1548.. AZ191 purchased from Selleck.

    (E) BEL7402 and HepG2 cells were treated with vehicle or 10 μM of the DYRK1B inhibitor, AZ191, alone and in combination with BafA1 for 24 h. Cyclin D1 expression was examined by immunoblot analysis.

    Sci Rep, 2016, 6:37052.. AZ191 purchased from Selleck.

  • Levels of endogenous GLI1 in Panc1 cells treated for the indicated times with 1 μM of AZ191.

    Oncotarget, 2017, 8(1):833-845. AZ191 purchased from Selleck.

Purity & Quality Control

Choose Selective DYRK Inhibitors

Biological Activity

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.
Targets
DYRK1B [1]
(Cell-free assay)
DYRK1A [1]
(Cell-free assay)
17 nM 88 nM
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]

Protocol

Solubility (25°C)

In vitro DMSO 85 mg/mL (197.89 mM)
Ethanol 1 mg/mL (2.32 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 429.52
Formula

C24H27N7O

CAS No. 1594092-37-1
Storage powder
in solvent
Synonyms N/A

Bio Calculators

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID