AZ191 is a potent and selective DYRK1B inhibitor with IC50 value of 17 nM [1].
DYRK1B (dual-specificity tyrosine phosphorylation-regulated kinase 1B) is particularly expressed in the testis and muscle where it plays an important role in myoblast differentiation. DYRK1B is overexpressed in certain cancers suggesting that it may be an oncogene [1].
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 [1].
References:
[1]. Ashford AL, Oxley D, Kettle J, et al. A novel DYRK1B inhibitor AZ191 demonstrates that DYRK1B acts independently of GSK3β to phosphorylate cyclin D1 at Thr(286), not Thr(288). Biochem J, 2014, 457(1): 43-56.
AZ191
Catalog No.: GC17654Purity:>99.50%
DYRK1B inhibitor,potent and selective
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1594092-37-1
10mM (in 1mL DMSO)In Stock
$74.00
1
1mgIn Stock
$30.00
1
5mgIn Stock
$68.00
1
10mgIn Stock
$99.00
1
25mgIn Stock
$158.00
1
50mgIn Stock
$246.00
1
100mgIn Stock
$344.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $74.00 | In Stock | 1 | |
| 1mg | $30.00 | In Stock | 1 | |
| 5mg | $68.00 | In Stock | 1 | |
| 10mg | $99.00 | In Stock | 1 | |
| 25mg | $158.00 | In Stock | 1 | |
| 50mg | $246.00 | In Stock | 1 | |
| 100mg | $344.00 | In Stock | 1 |
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Nature641, 529–536 (2025)
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Cell187(9):2288-2304 (2024)
Cell183(7):1867-1883 (2020)
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Description
Product Documents
Purity:>99.50%Appearance:A solid
Chemical Properties
CAS No.
1594092-37-1
Chemical Name
N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]-4-(1-methylpyrrolo[2,3-c]pyridin-3-yl)pyrimidin-2-amine
SMILES
CN1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=CC(=N3)C4=CN(C5=C4C=CN=C5)C)OC
Molecular Formula
C24H27N7O
Molecular Weight
429.52
Solubility
≥ 13.15mg/mL in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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