| Name | ARN-3236 |
| Description | ARN-3236 is an orally active and selective inhibitor of salt-inducible kinase 2 (SIK2), with IC50 values of <1 nM for SIK2, 21.63 nM for SIK1, and 6.63 nM for SIK3. ARN-3236 exhibits anti-cancer activity. |
| Cell Research | SIK2 expression was determined in ovarian cancer tissue samples and cell lines.?ARN-3236 was tested for its efficiency to inhibit growth and enhance paclitaxel sensitivity in cultures and xenografts of ovarian cancer cell lines.?SIK2 siRNA and ARN-3236 were compared for their ability to produce nuclear-centrosome dissociation, inhibit centrosome splitting, block mitotic progression, induce tetraploidy, trigger apoptotic cell death and reduce AKT/survivin signaling. |
| In vitro | Salt-inducible kinase 2 (SIK2) is overexpressed in approximately 30% of high-grade serous ovarian cancers.?ARN-3236 inhibited the growth of 10 ovarian cancer cell lines at an IC50 of 0.8 to 2.6 μmol/L, where the IC50 of ARN-3236 was inversely correlated with endogenous SIK2 expression (Pearson r = -0.642, P = 0.03).?ARN-3236 enhanced sensitivity to paclitaxel in 8 of 10 cell lines, as well as in SKOv3ip (P = 0.028) and OVCAR8 xenografts.?In at least three cell lines, a synergistic interaction was observed.?ARN-3236 uncoupled the centrosome from the nucleus in interphase, blocked centrosome separation in mitosis, caused prometaphase arrest, and induced apoptotic cell death and tetraploidy.?ARN-3236 also inhibited AKT phosphorylation and attenuated survivin expression. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 130 mg/mL (386.43 mM)
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| Keywords | inhibit | ARN 3236 | ARN-3236 | Salt-inducible Kinase (SIK) | ARN3236 | Inhibitor |
| Inhibitors Related | Phenformin hydrochloride | AICAR | Doxorubicin hydrochloride | Adenosine monophosphate | Metformin | Methyl cinnamate | A-769662 | Metformin hydrochloride | Chitosan oligosaccharide | Buformin hydrochloride | HTH-01-015 | AMPK activator 4 |
| Related Compound Libraries | PI3K-AKT-mTOR Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Cancer Metabolism Compound Library | Autophagy Compound Library | Antioxidant Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library |
United States
