AZ191

SKU: orb1223267

Description

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.

Key Properties

• CAS Number: 1594092-37-1
• MW: 429.52
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₇N₇O
• SMILES: CN1CCN(CC1)c1cc(c(cc1)Nc1nccc(n1)c1cn(c2c1ccnc2)C)OC
• Target: Bombesin Receptor
• Solubility: DMSO : ≥ 30 mg/mL. 69.85 mM; H2O : < 0.1 mg/mL

Bioactivity

• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AZ191 | AZ-191 | AZ 191

Quick Database Links

Gene Symbol

Bombesin Receptor