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AZ191

Item № 17693
CAS № 1594092-37-1
Purity ≥98%
product image
                (CAS 1594092-37-1)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     1 mg $25.00 0.00
     5 mg $88.00 0.00
     10 mg $163.00 0.00
     25 mg $375.00 0.00

Pricing updated 2019-06-15. Prices are subject to change without notice.

Description

Dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1B (DYRK1B) belongs to a family of nuclear-localized protein kinases and participates in the regulation of the cell cycle with key roles in proliferation and differentiation.1 It is upregulated in solid tumors and gain-of-function mutations in the gene encoding this kinase have been linked to metabolic syndrome.2,3 AZ191 is a cell-permeable azaindole that inhibits the serine/threonine kinase activity of DYRK1B (IC50 = 17 nM) with 5-fold and 110-fold selectivity against the related family members DYRK1A and DYRK2, respectively.4 This compound has been used as a probe to elucidate the mechanism of DYRK1B regulation of cell cycle progression.4

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Technical Information
Formal Name
N-[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]-4-(1-methyl-1H-pyrrolo[2,3-c]pyridin-3-yl)-2-pyrimidinamine
CAS Number
1594092-37-1
Molecular Formula
C24H27N7O
Formula Weight
429.5
Purity
≥98%
Formulation
A crystalline solid
λmax
219, 264, 303 nm
SMILES
CN1CCN(C2=CC=C(NC3=NC=CC(C4=CN(C)C5=C4C=CN=C5)=N3)C(OC)=C2)CC1
InChI Code
InChI=1S/C24H27N7O/c1-29-10-12-31(13-11-29)17-4-5-21(23(14-17)32-3)28-24-26-9-7-20(27-24)19-16-30(2)22-15-25-8-6-18(19)22/h4-9,14-16H,10-13H2,1-3H3,(H,26,27,28)
InChI Key
ZYVXTMKTGDARKR-UHFFFAOYSA-N

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Stability
≥ 2 years
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Additional Information

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References & Product Citations
Product Description References

1. Becker, W. Emerging role of DYRK family protein kinases as regulators of protein stability in cell cycle control Cell Cycle 11(18), 3389-3394 (2012).

2. Gao, J., Zheng, Z., Rawal, B., et al. Mirk/Dyrk1B, a novel therapeutic target, mediates cell survival in non-small cell lung cancer cells Cancer Biology and Therapy 8(17), 1671-1679 (2009).

3. Keramati, A.R., Fathzadeh, M., Go, G.W., et al. A form of the metabolic syndrome associated with mutations in DYRK1B New England Journal of Medicine 370(20), 1909-1919 (2014).

4. Ashford, A.L., 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) Biochemistry Journal 457(1), 43-56 (2014).

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