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AZ191

Catalog No. T6257 CAS 1594092-37-1

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.

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AZ191, CAS 1594092-37-1

Pack Size	Availability	Price/USD
2 mg	In stock	$ 39.00
5 mg	In stock	$ 63.00
10 mg	In stock	$ 90.00
25 mg	In stock	$ 169.00
50 mg	In stock	$ 270.00
1 mL * 10 mM (in DMSO)	In stock	$ 68.00

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Purity: 99.65%

Purity: 99.13%

Purity: 98.04%

Biological Description

Chemical Properties

Storage & Solubility Information

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.
Targets&IC50	DYRK1B:17 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]
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.

Molecular Weight	429.52
Formula	C24H27N7O
CAS No.	1594092-37-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 1 mg/mL (2.32 mM)

DMSO: 79 mg/mL (183.9 mM)

References and Literature

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

Citations

1. Wang C, Hu R, Wang T, et al.A bivalent β-carboline derivative inhibits macropinocytosis-dependent entry of pseudorabies virus by targeting the kinase DYRK1A.Journal of Biological Chemistry.2023: 104605.

Related compound libraries

This product is contained In the following compound libraries：

Tyrosine Kinase Inhibitor Library Inhibitor Library Target-Focused Phenotypic Screening Library Anti-Cancer Compound Library Bioactive Compound Library Bioactive Compounds Library Max Cell Cycle Compound Library NO PAINS Compound Library Kinase Inhibitor Library

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CLK-IN-T3 GNF2133 CK2/ERK8-IN-1 7BIO DYRKs-IN-1 ARN25068 Harmine AZ-Dyrk1B-33

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

AZ191 1594092-37-1 Cell Cycle/Checkpoint Tyrosine Kinase/Adaptors DYRK Inhibitor Dual specificity tyrosine regulated kinase Dual specificity tyrosine phosphorylation regulated kinase inhibit AZ 191 AZ-191 inhibitor

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