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

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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 204 In-stock
Solution
10 mM * 1 mL in DMSO USD 204 In-stock
Solid
2 mg USD 110 In-stock
5 mg USD 165 In-stock
10 mg USD 275 In-stock
50 mg USD 605 In-stock
100 mg USD 935 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

ARN-3236 Related Antibodies

Top Publications Citing Use of Products

View All Salt-inducible Kinase (SIK) Isoform Specific Products:

View All Isoforms
SIK1 SIK2 SIK3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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 NSC 125973 sensitivity in ovarian cancer cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ARN-3236 Related Antibodies

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 NSC 125973 in vivo[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 NSC 125973.
Molecular Weight

336.41

Formula

C19H16N2O2S
CAS No.
Appearance

Solid

Color

White to off-white

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (148.63 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.60%

COA (261 KB) HNMR (263 KB) LCMS (267 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9726 mL 14.8628 mL 29.7256 mL 74.3141 mL
5 mM 0.5945 mL 2.9726 mL 5.9451 mL 14.8628 mL
10 mM 0.2973 mL 1.4863 mL 2.9726 mL 7.4314 mL
15 mM 0.1982 mL 0.9909 mL 1.9817 mL 4.9543 mL
20 mM 0.1486 mL 0.7431 mL 1.4863 mL 3.7157 mL
25 mM 0.1189 mL 0.5945 mL 1.1890 mL 2.9726 mL
30 mM 0.0991 mL 0.4954 mL 0.9909 mL 2.4771 mL
40 mM 0.0743 mL 0.3716 mL 0.7431 mL 1.8579 mL
50 mM 0.0595 mL 0.2973 mL 0.5945 mL 1.4863 mL
60 mM 0.0495 mL 0.2477 mL 0.4954 mL 1.2386 mL
80 mM 0.0372 mL 0.1858 mL 0.3716 mL 0.9289 mL
100 mM 0.0297 mL 0.1486 mL 0.2973 mL 0.7431 mL
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ARN-3236 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ARN-32361613710-01-2ARN3236ARN 3236Salt-inducible Kinase (SIK)Inhibitorinhibitorinhibit

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