ARN 3236

Product 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.

Solubility

Preparing Stock Solutions for ARN 3236

The following data is based on the product molecular weight 336.41

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.2 mM	14.86 mL	74.31 mL	148.63 mL
1 mM	2.97 mL	14.86 mL	29.73 mL
2 mM	1.49 mL	7.43 mL	14.86 mL
10 mM	0.30 mL	1.49 mL	2.97 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Lombardi SIK inhibition in human myeloid cells modulates TLR and IL-1R signaling and induces an anti-inflammatory phenotype. J.Leukoc.Biol. 2016 PMID: 26590148
• Liu The selective SIK2 inhibitor ARN-3236 Produces strong antidepressant-like efficacy in mice via the hippocampal CRTC1-CREB-BDNF pathway. Front.Pharmacol. 2021 PMID: 33519490
• Zhou A novel compound ARN-3236 inhibits salt-inducible kinase 2 and sensitizes ovarian cancer cell lines and xenografts to Paclitaxel. Clin.Cancer Res. 2017 PMID: 27678456