AZ191

SKU: orb1300930

Description

AZ191 is a potent and selective DYRK1B inhibitor with an IC50 of 17 nM, exhibiting approximately 5-fold and 110-fold selectivity over DYRK1A and DYRK2, respectively. This small molecule is a valuable research tool for studying DYRK1B's role in cellular signaling, proliferation, and metabolic pathways in both in vitro and in vivo models.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1594092-37-1
• MW: 429.52
• Purity: 99.17%
• Formula: C₂₄H₂₇N₇O
• SMILES: COc1cc(ccc1Nc1nccc(n1)-c1cn(C)c2cnccc12)N1CCN(C)CC1
• Target: DYRK
• Solubility: Ethanol:1 mg/mL (2.33 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.66 mM);DMSO:79 mg/mL (183.93 mM)

Bioactivity

• Target IC50:
  DYRK1B:17 nM
• In Vitro:
  AZ191 selectively inhibits DYRK1B serine/threonine kinase activity with no effect on tyrosine kinase autophosphorylation. In HEK-293 cells, AZ191 also displays much greater potency for DYRK1B over DYRK1A, inhibiting CCND1 phosphorylation. In HD1B cells, AZ191 strongly inhibits the levels of the cell-cycle regulators, p21Cip1 and p27Kip1, and increases cell-cycle progression.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AZ 191, AZ191, AZ-191, DYRK, DYRK1A, DYRK1B, DYRK2, Dual specificity tyrosine regulated kinase, Dual specificity tyrosine phosphorylation regulated kinase, inhibit, Inhibitor

Compound Identifiers

PubChem CID

72716071