Introduction:Basic information about CAS 1594092-37-1|AZ 191, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | AZ 191 |
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| CAS Number | 1594092-37-1 | Molecular Weight | 429.51700 |
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| Density | / | Boiling Point | / |
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| Molecular Formula | C24H27N7O | Melting Point | / |
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| MSDS | USA | Flash Point | / |
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Names
| Name | 2-Pyrimidinamine, N-[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]-4-(1-methyl-1H-pyrrolo[2,3-c]pyridin-3-yl)- |
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| Synonym | More Synonyms |
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AZ 191 BiologicalActivity
| Description | AZ191 is a potent small molecule inhibitor that selectively inhibits DYRK1B with IC50 of 17 nM; selective for DYRK1B over both DYRK1A and DYRK2.IC50 value: 17 nM [1]Target: DYRK1B inhibitorin vitro: Using in vitro kinase assays, phospho-specific immunoblot analysis and MS in conjunction with AZ191 we now show that DYRK1B phosphorylates CCND1 at Thr(286), not Thr(288), in vitro and in cells. In HEK (human embryonic kidney)-293 and PANC-1 cells (which exhibit DYRK1B amplification) DYRK1B drives Thr(286) phosphorylation and proteasome-dependent turnover of CCND1 and this is abolished by AZ191 or DYRK1B RNAi, but not by GSK3β inhibitors or GSK3β RNAi. |
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| Related Catalog | Signaling Pathways >>Protein Tyrosine Kinase/RTK >>DYRKResearch Areas >>Cancer |
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| References | [1]. Ashford AL, 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 Jan 1;457(1):43-56. |
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Chemical & Physical Properties
| Molecular Formula | C24H27N7O |
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| Molecular Weight | 429.51700 |
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| Exact Mass | 429.22800 |
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| PSA | 71.34000 |
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| LogP | 3.61020 |
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| InChIKey | ZYVXTMKTGDARKR-UHFFFAOYSA-N |
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| SMILES | COc1cc(N2CCN(C)CC2)ccc1Nc1nccc(-c2cn(C)c3cnccc23)n1 |
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| Storage condition | -20℃ |
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Safety Information
| RIDADR | NONH for all modes of transport |
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Synonyms
| [2-Methoxy-4-(4-methyl-piperazin-1-yl)-phenyl]-[4-(1-methyl-1H-pyrrolo[2,3-c]pyridin-3-yl)-pyrimidin-2-yl]-amine |
| AZ191 |