ARN-3236

Research use only, not for human use.

ARN-3236 is a novel potent, selective, and orally active SIK2 inhibitor with IC50 of <1 nM.

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.

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.

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.

ARN3236

Autophagy

SIK

SIK

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1613710-01-2

336.409

C19H16N2O2S

>98% (HPLC)

DMSO : 130 mg/mL. 386.43 mM

COC1=CC=C(C2=CNC3=NC=CC(C4=CSC=C4)=C32)C(OC)=C1

3-(2,4-Dimethoxyphenyl)-4-(3-thienyl)-1H-pyrrolo[2,3-b]pyridine

(-20℃)

With Ice Pack

≥ 2 years