[CAS NO. 1594092-37-1] AZ191

Name: AZ191
Brand: Arctom Scientific
SKU: SLK-S7338

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PRODUCTS SPECIFICATIONS [1594092-37-1]

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Catalog

SLK-S7338

Brand

Selleck

CAS

1594092-37-1

DESCRIPTION [1594092-37-1]

Overview

MDL	MFCD28015098
Molecular Weight	429.52
Molecular Formula	C24H27N7O
SMILES	CN1C=C(C2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3OC)=NC=C2)C5=C1C=NC=C5

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.3282 mL	11.6409 mL	23.2818 mL
5 mM	0.4656 mL	2.3282 mL	4.6564 mL
10 mM	0.2328 mL	1.1641 mL	2.3282 mL
50 mM	0.0466 mL	0.2328 mL	0.4656 mL

Description

AZ191 is a potent and selective inhibitor with 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, p21 and p27, and increases cell-cycle progression.

References

[1] Ashford AL, et al. Biochem J. 2014, 457(1), 43-56.