CAS 1594092-37-1|AZ 191

Introduction:Basic information about CAS 1594092-37-1|AZ 191, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameAZ 191
CAS Number1594092-37-1Molecular Weight429.51700
Density/Boiling Point/
Molecular FormulaC24H27N7OMelting Point/
MSDSUSAFlash Point/

Names

Name2-​Pyrimidinamine, N-​[2-​methoxy-​4-​(4-​methyl-​1-​piperazinyl)​phenyl]​-​4-​(1-​methyl-​1H-​pyrrolo[2,​3-​c]​pyridin-​3-​yl)​-
SynonymMore Synonyms

AZ 191 BiologicalActivity

DescriptionAZ191 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.
Related CatalogSignaling Pathways >>Protein Tyrosine Kinase/RTK >>DYRKResearch Areas >>Cancer
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.

Chemical & Physical Properties

Molecular FormulaC24H27N7O
Molecular Weight429.51700
Exact Mass429.22800
PSA71.34000
LogP3.61020
InChIKeyZYVXTMKTGDARKR-UHFFFAOYSA-N
SMILESCOc1cc(N2CCN(C)CC2)ccc1Nc1nccc(-c2cn(C)c3cnccc23)n1
Storage condition-20℃

Safety Information

RIDADRNONH for all modes of transport

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
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