ARN-3236
| CAS No. | 1613710-01-2 | Cat. No. | BCP25158 |
| Name | ARN-3236 | ||
| Synonyms | ARN 3236; ARN3236; | ||
| Formula | C19H16N2O2S | M. Wt | 336.41 |
| Description | ARN-3236 is potent, orally active and selective SIK2 inhibitor. ARN-3236 inhibited the growth of 10 ovarian cancer cell lines at an IC50 of 0.8 to 2.6 μmol/L. ARN-3236 enhanced sensitivity to paclitaxel in 8 of 10 cell lines, as well as in SKOv3ip (P = 0.028) and OVCAR8 xenografts. 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. ARN-3236 is the first orally available inhibitor of SIK2 to be evaluated against ovarian cancer in preclinical models and shows promise in inhibiting ovarian cancer growth and enhancing paclitaxel chemosensitivity. | ||
| Pathways | Others Pathway | ||
| Targets | Others | ||
Structure
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