AZ191

Research use only, not for human use.

AZ191（IC50 of 17 nM） is an effective and specific DYRK1B inhibitor. The specificity of AZ191 for DYRK1B is about 5- and 110-fold greater over DYRK1A and DYRK2, respectively.

AZ191 is a novel, potent and selective DYRK1B inhibitor. AZ191 demonstrates that DYRK1B acts independently of GSK3β to phosphorylate cyclin D1 at Thr(286), not Thr(288). AZ191 selectively inhibits DYRK1B in vitro and in cells. DYRK1B (dual-specificity tyrosine phosphorylation-regulated kinase 1B) is amplified in certain cancers and may be an oncogene. AZ191 may prove useful in defining further substrates and biological functions of DYRK1B.

Cell Proliferation Assay Cell Line:SW872, SW982 liposarcoma cells Concentration:0.01, 0.03, 0.1, 0.3, 0.6, 1, 3, 6, 10, 20, 60 μM Incubation Time:5 days Result:Dose-dependent growth inhibition with IC50s of 3.183 μM and 1.279 μM for SW872 and SW982 cell lines, respectively.Western Blot Analysis Cell Line:SW872, SW982 liposarcoma cells Concentration:1, 2, 3, 4, 5 μM Incubation Time:48 hours Result:Down-regulated three anti-apoptotic proteins (Bcl-2, p21, and survivin) at higher concentrations.

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AZ191 | AZ-191 | AZ 191

GPCR/G Protein

Bombesin Receptor

DYRK1A| DYRK1B| DYRK2

Cancer

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1594092-37-1

429.52

C24H27N7O

>98% (HPLC)

DMSO : ≥ 30 mg/mL. 69.85 mM; H2O : < 0.1 mg/mL

CN1CCN(CC1)c1cc(c(cc1)Nc1nccc(n1)c1cn(c2c1ccnc2)C)OC

N-(2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)-4-(1-methyl-1H-pyrrolo[2,3-c]pyridin-3-yl)pyrimidin-2-amine

(-20℃)

With Ice Pack

≥ 2 years