ARN-3236
Based on 5 publication(s) in Google Scholar
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.66%
- CAS. Nr.: 1613710-01-2
- Formel: C19H16N2O2S
- Molecular Weight:336.41
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) ARN-3236
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Customer Validation & Images
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ELISA
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Histological Imaging/Staining
Biologische Aktivität
Beschreibung
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QIK/SIK2 <1 nM (IC50) |
SIK1 21.63 nM (IC50) |
QSK/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.
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Cell Line:HEY and A2780 human ovarian cancer cell lines.
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Concentration:0-10 μM.
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Incubation Time:24 hours.
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Result:Inhibited SIK2 activity with an IC50 <1 nM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SKOv3ip-bearing mice and OVCAR8-bearing mice[2].
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Dosage:60 mg/kg.
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Administration:Orally once daily for 3 weeks (SKOv3ip-bearing mice) and 4 weeks (OVCAR8-bearing mice).
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Result:Sensitized ovarian cancer to NSC 125973.
Chemical Information
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CAS. Nr. 1613710-01-2
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Appearance Solid
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Molecular Weight 336.41
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Formel C19H16N2O2S
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Color White to off-white
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SMILES
COC1=CC=C(C2=CNC3=NC=CC(C4=CSC=C4)=C32)C(OC)=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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J Neuroinflammation
SIK2 mediated mitochondrial homeostasis in spinal cord injury: modulating oxidative stress and the AIM2 inflammasome via CRTC1/CREB signaling. [Abstract]2025 Dec 3;22(1):283. PMID: 41339921
ARN-3236 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2025 Dec 3;22(1):283. [Abstract]
Western blot and statistical analysis of HO-1 and SOD1 expression in BV2 cells after TBHP or ARN-3236 (1 μM) treatment for 6 h.
ARN-3236 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2025 Dec 3;22(1):283. [Abstract]
Immunofluorescence staining for HO-1 and statistical analysis in BV2 cells in each group as above designed, cells were treated with TBHP or ARN-3236 (1 μM) for 6 h.
ARN-3236 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2025 Dec 3;22(1):283. [Abstract]
ELISA-based statistical evaluation of inflammatory cytokine levels in culture supernatant treated with ARN-3236 (1 μM).
ARN-3236 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2025 Dec 3;22(1):283. [Abstract]
Representative tissue morpha and HE staining of mice bladder in each group at 28dpi treated with ARN-3236 (30 mg/kg p.o.).
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Oncogene
SIK2 maintains breast cancer stemness by phosphorylating LRP6 and activating Wnt/β-catenin signaling. [Abstract]2022 Apr;41(16):2390-2403. PMID: 35277657 -
Transl Res
SIK2 protects against renal tubular injury and the progression of diabetic kidney disease. [Abstract]2023 Mar:253:16-30. PMID: 36075517 -
BMC Pulm Med
Salt-inducible kinase 2 (SIK2) inhibitor ARN-3236 attenuates bleomycin-induced pulmonary fibrosis in mice. [Abstract]2022 Apr 11;22(1):140. PMID: 35410283 -
Lösungsmittel & Löslichkeit
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Reinheit & Dokumentation
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Data Sheet (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Lombardi MS, et al. SIK inhibition in human myeloid cells modulates TLR and IL-1R signaling and induces an anti-inflammatory phenotype. J Leukoc Biol. 2016 May;99(5):711-21. [Content Brief]
[2]. Zhou J, et al. A Novel Compound ARN-3236 Inhibits Salt-Inducible Kinase 2 and Sensitizes Ovarian Cancer Cell Lines and Xenografts. Clin Cancer Res. 2017 Apr 15;23(8):1945-1954. [Content Brief]
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 |
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| 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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