ARN-3236

SKU: orb1226057

Description

ARN-3236 is a novel potent, selective, and orally active SIK2 inhibitor with IC50 of <1 nM; does not significantly inhibit SIK1 and SIK3, as well as other AMPK family members; inhibits the growth of 10 ovarian cancer cell lines with IC50 of 0.8-2.6 uM; increasess centrosome uncoupling from nucleus, and inhibits centrosome splitting in mitotic cells; induces cell cycle arrest, apoptosis and tetraploidy, also inhibits AKT phosphorylation and attenuates survivin expression; sensitizes ovarian cancer to paclitaxel in SKOv3ip xenograft model.

Key Properties

• CAS Number: 1613710-01-2
• MW: 336.409
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₆N₂O₂S
• SMILES: COC1=CC=C(C2=CNC3=NC=CC(C4=CSC=C4)=C32)C(OC)=C1
• Target: SIK
• Solubility: DMSO : 130 mg/mL. 386.43 mM

Bioactivity

• In Vivo:
  ARN-3236 (60 mg/kg, orally) sensitizes ovarian cancer to NSC 125973 In vivo. Animal model: SKOv3ip-bearing mice and OVCAR8-bearing mice. Dosage: 60 mg/kg. Administration: Orally once daily for 3 weeks (SKOv3ip-bearing mice) and 4 weeks (OVCAR8-bearing mice). Result: Sensitized ovarian cancer to NSC 125973.
• In Vitro:
  ARN-3236 inhibits SIK2 activity with an IC50 <1 nM. ARN-3236 inhibits cell growth and increases NSC 125973 sensitivity in ovarian cancer cells. Cell Viability Assay Cell line: HEY and A2780 human ovarian cancer cell lines. Concentration: 0-10 μM. Incubation time: 24 hours. Result: Inhibited SIK2 activity with an IC50 <1 nM.

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

ARN3236

Quick Database Links

Gene Symbol

SIK