AZ191

Cas No.:	1594092-37-1
Chemical Name:	N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]-4-(1-methylpyrrolo[2,3-c]pyridin-3-yl)pyrimidin-2-amine
Synonyms:	AZ 191;[2-Methoxy-4-(4-methyl-piperazin-1-yl)-phenyl]-[4-(1-methyl-1H-pyrrolo[2,3-c]pyridin-3-yl)-pyrimidin-2-yl]-amine;2-​Pyrimidinamine, N-​[2-​methoxy-​4-​(4-​methyl-​1-​piperazinyl)​phenyl]​-​4-​(1-​methyl-​1H-​pyrrolo[2,​3-​c]​pyridin-​3-​yl)​-;AZ-191;AZ191;N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]-4-(1-methylpyrrolo[2,3-c]pyridin-3-yl)pyrimidin-2-amine;N-(2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)-4-(1-methyl-1H-pyrrolo[2,3-c]pyridin-3-yl)pyrimidin-2-amine;C24H27N7O;GTPL9268;HMS3653O14;BCP12820;BDBM50081174;s7338;Compound 19 [PMID25738750];2-Pyrimidinamine, N-[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]-4-(1-
SMILES:	O(C([H])([H])[H])C1=C(C([H])=C([H])C(=C1[H])N1C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])C1([H])[H])N([H])C1=NC([H])=C([H])C(C2=C([H])N(C([H])([H])[H])C3C([H])=NC([H])=C([H])C2=3)=N1
Formula:	C24H27N7O
M.Wt:	429.5175
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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.

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.