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AdipoGen Life Sciences
AZ191
35
CHF
CHF 35.00
In stock
AG-CR1-3657-M0011 mgCHF 35.00
AG-CR1-3657-M0055 mgCHF 120.00
AG-CR1-3657-M02525 mgCHF 450.00
| Product Details | |
|---|---|
| Synonyms | N-[2-Methoxy-4-(4-methyl-1-piperazinyl)phenyl]-4-(1-methyl-1H-pyrrolo[2,3-c]pyridin-3-yl)-2-pyrimidinamine |
| Product Type | Chemical |
| Properties | |
| Formula |
C24H27N7O |
| MW | 429.5 |
| CAS | 1594092-37-1 |
| Purity Chemicals | ≥98% |
| Appearance | White to off-white solid. |
| Solubility | Soluble in DMSO (5mg/ml), ethanol (2mg/ml) or DMF (2mg/ml). |
| Identity | Determined by 1H-NMR. |
| InChi Key | ZYVXTMKTGDARKR-UHFFFAOYSA-N |
| Smiles | CN1C2=C(C=CN=C2)C(C3=CC=NC(NC4=C(OC)C=C(N5CCN(C)CC5)C=C4)=N3)=C1 |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice | Keep cool and dry. |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- Cell permeable azaindole that inhibits the serine/threonine kinase activity of DYRK1B (IC50=17nM) with 5-fold and 110-fold selectivity against the related family members DYRK1A and DYRK2, respectively.
- Used as a probe to elucidate the mechanism of DYRK1B regulation of cell cycle progression.
- 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. It is upregulated in solid tumors and gain-of-function mutations in the gene encoding this kinase have been linked to metabolic syndrome.
Product References
- A novel DYRK1B inhibitor AZ191 demonstrates that DYRK1B acts independently of GSK3β to phosphorylate cyclin D1 at Thr(286), not Thr(288): A.L. Ashford, et al.; Biochem. J. 457, 43 (2014)
- Comparative Efficacy and Selectivity of Pharmacological Inhibitors of DYRK and CLK Protein Kinases: M.F. Lindberg, et al.; J. Med. Chem. ahead of print (2023)
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