ARN 3236

Name: ARN 3236
Brand: Tocris Bioscience
SKU: 7511

Tocris Bioscience, part of Bio-Techne | Catalog # 7511

COA / SDS

Potent inhibitor of salt-inducible kinases

Key Product Details

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)
Molecular Weight:	336.41

View Full Technical Details for ARN 3236

Technical Data
Citations

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 for ARN 3236

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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.

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

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References for ARN 3236

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