AZ191 - CAS 1594092-37-1
Catalog number:
1594092-37-1
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C24H27N7O
Molecular Weight:
429.52
COA:
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Targets:
DYRK
Description:
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.
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Purity:
>98%
MSDS:
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1.A novel DYRK1B inhibitor AZ191 demonstrates that DYRK1B acts independently of GSK3β to phosphorylate cyclin D1 at Thr(286), not Thr(288).
Ashford AL1, Oxley D, Kettle J, Hudson K, Guichard S, Cook SJ, Lochhead PA. Biochem J. 2014 Jan 1;457(1):43-56. doi: 10.1042/BJ20130461.
DYRK1B (dual-specificity tyrosine phosphorylation-regulated kinase 1B) is amplified in certain cancers and may be an oncogene; however, our knowledge of DYRK1B has been limited by the lack of selective inhibitors. In the present study we describe AZ191, a potent small molecule inhibitor that selectively inhibits DYRK1B in vitro and in cells. CCND1 (cyclin D1), a key regulator of the mammalian G1-S-phase transition, is phosphorylated on Thr(286) by GSK3β (glycogen synthase kinase 3β) to promote its degradation. DYRK1B has also been proposed to promote CCND1 turnover, but was reported to phosphorylate Thr(288) rather than Thr(286). 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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CAS 1594092-37-1 AZ191

AZ191
(CAS: 1594092-37-1)

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...

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CAS 1594092-37-1 AZ191

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