AZ 191
Modify Date: 2024-01-10 22:15:59
AZ 191 structure
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Common Name | AZ 191 | ||
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| CAS Number | 1594092-37-1 | Molecular Weight | 429.51700 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C24H27N7O | Melting Point | N/A | |
| MSDS | USA | Flash Point | N/A | |
Use of AZ 191AZ191 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. |
| 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 |
| 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 | |
| References |
| Molecular Formula | C24H27N7O |
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| Molecular Weight | 429.51700 |
| Exact Mass | 429.22800 |
| PSA | 71.34000 |
| LogP | 3.61020 |
| Storage condition | -20℃ |
| RIDADR | NONH for all modes of transport |
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| [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 |