1. Immunology/Inflammation
  2. Salt-inducible Kinase (SIK)
  3. ARN-3236

ARN-3236 

Cat. No.: HY-120856 Purity: 98.12%
Handling Instructions

ARN-3236 is an oral active and selective inhibitor of salt-inducible kinase 2 (SIK2), with IC50s of <1 nM, 21.63 nM and 6.63 nM for SIK2, SIK1 and SIK3, respectively. Has anti-cancer activity.

For research use only. We do not sell to patients.

ARN-3236 Chemical Structure

ARN-3236 Chemical Structure

CAS No. : 1613710-01-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 185 In-stock
Estimated Time of Arrival: December 31
2 mg USD 100 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 250 In-stock
Estimated Time of Arrival: December 31
50 mg USD 550 In-stock
Estimated Time of Arrival: December 31
100 mg USD 850 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

ARN-3236 is an oral active and selective inhibitor of salt-inducible kinase 2 (SIK2), with IC50s of <1 nM, 21.63 nM and 6.63 nM for SIK2, SIK1 and SIK3, respectively. Has anti-cancer activity[1][2].

IC50 & Target[1][2]

SIK2

<1 nM (IC50)

SIK1

21.63 nM (IC50)

SIK3

6.63 nM (IC50)

In Vitro

ARN-3236 inhibits SIK2 activity with an IC50 <1 nM[2].
ARN-3236 inhibits cell growth and increases paclitaxel sensitivity in ovarian cancer cells[2].

Cell Viability Assay[2]

Cell Line: HEY and A2780 human ovarian cancer cell lines.
Concentration: 0-10 μM.
Incubation Time: 24 hours.
Result: Inhibited SIK2 activity with an IC50 <1 nM.
In Vivo

ARN-3236 (60 mg/kg, orally) sensitizes ovarian cancer to paclitaxel in vivo[2].

Animal Model: SKOv3ip-bearing mice and OVCAR8-bearing mice[2].
Dosage: 60 mg/kg.
Administration: Orally once daily for 3 weeks (SKOv3ip-bearing mice) and 4 weeks (OVCAR8-bearing mice).
Result: Sensitized ovarian cancer to paclitaxel.
Molecular Weight

336.41

Formula

C₁₉H₁₆N₂O₂S

CAS No.

1613710-01-2

SMILES

COC1=CC=C(C2=CNC3=NC=CC(C4=CSC=C4)=C32)C(OC)=C1

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 130 mg/mL (386.43 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9726 mL 14.8628 mL 29.7256 mL
5 mM 0.5945 mL 2.9726 mL 5.9451 mL
10 mM 0.2973 mL 1.4863 mL 2.9726 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.17 mg/mL (6.45 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.17 mg/mL (6.45 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.17 mg/mL (6.45 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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ARN-3236
Cat. No.:
HY-120856
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