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ARN 3236

Cat. No. 7511 Submit a Review Datasheet / COA / SDS
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Description: Potent inhibitor of salt-inducible kinases
Chemical Name: 3-(2,4-Dimethoxyphenyl)-4-(3-thienyl)-1H-pyrrolo[2,3-b]pyridine
Purity: ≥98% (HPLC)
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Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for ARN 3236

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.

Technical Data for ARN 3236

M. Wt 336.41
Formula C19H16N2O2S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1613710-01-2
PubChem ID 74766530
InChI Key WEHOIIGXTMKVRG-UHFFFAOYSA-N
Smiles COC1=CC(OC)=C(C=C1)C2=CNC3=C2C(C4=CSC=C4)=CC=N3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for ARN 3236

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 6.73 20

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 will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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 0.3 mL 1.49 mL 2.97 mL

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References for ARN 3236

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

Zhou et al (2017) A novel compound ARN-3236 inhibits salt-inducible kinase 2 and sensitizes ovarian cancer cell lines and xenografts to Paclitaxel. Clin.Cancer Res. 23 1945 PMID: 27678456

Lombardi et al (2016) SIK inhibition in human myeloid cells modulates TLR and IL-1R signaling and induces an anti-inflammatory phenotype. J.Leukoc.Biol. 99 711 PMID: 26590148

Liu et al (2021) The selective SIK2 inhibitor ARN-3236 Produces strong antidepressant-like efficacy in mice via the hippocampal CRTC1-CREB-BDNF pathway. Front.Pharmacol. 11 624429 PMID: 33519490

If you know of a relevant reference for ARN 3236, please let us know.

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Keywords: ARN 3236, ARN 3236 supplier, ARN3236, potent, inhibitors, inhibits, salt-inducible, kinase, 2, SIK2, centrosome, separation, antidepressant, depression, anti-inflammatory, Other, Kinases, 7511, Tocris Bioscience

Citations for ARN 3236

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