Description

• ARN 3236 is a potent of salt-inducible kinase 2 (SIK2) inhibitor (IC50 values are <1 nM, 6.63 nM and 21.63 nM for SIK2, SIK3 and SIK1 respectively)
• ARN 3236 inhibits centrosome separation by uncoupling the centrosome from the nucleus
• It also induces cell-cycle arrest and apoptosis by attenuating the AKT/survivin pathway
• ARN 3236 inhibits growth and enhances Taxol (Cat
• No
• 1097) sensitivity in ovarian cancer cell lines in vitro and in vivo
• In human myeloid cells, ARN 3236 blocks TNF and induces IL-10 upon LPS stimulation; it also reduces the production of IL-1β upon activation of TLR4 and TLR2 signaling
• In depression models, ARN 3236 exhibits antidepressant-like effects via the hippocampal CRTC1-CREB-BDNF pathway
• ARN 3236 penetrates the blood-brain barrier, and it is orally bioavailable.