| Bioactivity | ARN-3236 is an oral active and selective inhibitor of salt-inducible kinase 2 (SIK2), with IC50s of <1 nM, 21.63 nM and 6.63 nM for SIK2, SIK1 and SIK3, respectively. Has anti-cancer activity[1][2]. | ||||||||||||
| Invitro | ARN-3236 inhibits SIK2 activity with an IC50 <1 nM[2].ARN-3236 inhibits cell growth and increases NSC 125973 sensitivity in ovarian cancer cells[2]. Cell Viability Assay[2] Cell Line: | ||||||||||||
| In Vivo | ARN-3236 (60 mg/kg, orally) sensitizes ovarian cancer to NSC 125973 in vivo[2]. Animal Model: | ||||||||||||
| Name | ARN-3236 | ||||||||||||
| CAS | 1613710-01-2 | ||||||||||||
| Formula | C19H16N2O2S | ||||||||||||
| Molar Mass | 336.41 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Lombardi MS, et al. SIK inhibition in human myeloid cells modulates TLR and IL-1R signaling and induces an anti-inflammatory phenotype. J Leukoc Biol. 2016 May;99(5):711-21. [2]. Zhou J, et al. A Novel Compound ARN-3236 Inhibits Salt-Inducible Kinase 2 and Sensitizes Ovarian Cancer Cell Lines and Xenografts. Clin Cancer Res. 2017 Apr 15;23(8):1945-1954. |