ARN-3236 Chemical Properties

Density 

1.278±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO:65.67(Max Conc. mg/mL);195.21(Max Conc. mM)
Ethanol:2.0(Max Conc. mg/mL);5.95(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);89.18(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:4):0.2(Max Conc. mg/mL);0.59(Max Conc. mM)

form 

A crystalline solid

pka

13.33±0.40(Predicted)

color 

White to off-white

ARN-3236 Usage And Synthesis

Biological Activity

ARN-3236 is an orally active, ATP-competitive, SIK2-selective salt-inducible kinase inhibitor (IC50 = 21.63 nM/SIK1, <1 nM/SIK2, 6.63 nM/SIK3) th at suppresses cellular SIK2 activity (by 58% at 1 μM; SKOv3-SIK2 cells, 48 h) with high selectivity over >456 kinases. ARN-3236 effectively suppresses SIK2-dependent growth of ovarian cancer cultures (IC50 = 0.8-2.6 μM in 10 lines, 72 h) and in murine xenograft models in vivo (30, 60, 100 mg/kg/day p.o.). In addition, ARN-3236 sensitizes ovarian cancer cells to paclitaxel in vitro and in vivo. ARN-3236 completes the SIK1-selective HG-9-91-01 (SIK1/2/3 IC50 = 0.6/6.6/9.6 nM) in probing SIKs-mediated cellular signaling events.

storage

Store at -20°C