GSK-626616
Based on 8 publication(s) in Google Scholar
GSK-626616 is a potent, orally bioavailable inhibitor of DYRK3 (IC50=0.7 nM). GSK-626616 inhibits other members of the DYRK family (e.g., DYRK1A and DYRK2) with similar potency, which is a potential therapy for the treatment of anemia.
For research use only. We do not sell to patients.
- Purity: 99.88%
- CAS No.: 1025821-33-3
- Formula: C18H10Cl2N4OS
- Molecular Weight:401.27
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GSK-626616
More- J Med Chem. 2023 Mar 23;66(6):4106-4130. [Abstract]
- Biomedicines. 2024 Jan 16;12(1):197. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- Technical University of Dresden. 2025.
- bioRxiv. 2025 January 18.
- bioRxiv. 2025 Feb 16:2025.02.12.637879. [Abstract]
- bioRxiv. 2024 September 27.
- bioRxiv. 2023 Dec 1.
Biological Activity
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DYRK1 |
DYRK2 |
DYRK3 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-22 | IC50 |
27.8 μM
Compound: 13; GSK-626616
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Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
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[PMID: 36876904] |
GSK-626616 abolishes the phosphorylation of S6K1 at Thr389 in nonstimulated HeLa cells. GSK-626616 reduces the phosphorylation of S6K1 at Thr389 in EGF- and insulin-stimulated HeLa cells, showing that mTORC1 activity is impaired[2].
GSK-626616 (serum-deprived HeLa cells) reduces EGF-induced phosphorylation of PRAS40 at Thr246. Binding of PRAS40 to mTORC1 is enhanced by GSK-626616[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1025821-33-3
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Appearance Solid
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Molecular Weight 401.27
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Formula C18H10Cl2N4OS
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Color Light yellow to yellow
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SMILES
O=C1N=C(NC2=C(Cl)C=CC=C2Cl)S/C1=C\C3=CC=C4N=CC=NC4=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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J Med Chem
Comparative Efficacy and Selectivity of Pharmacological Inhibitors of DYRK and CLK Protein Kinases. [Abstract]2023 Mar 23;66(6):4106-4130. PMID: 36876904 -
Biomedicines
A Novel Druggable Dual-Specificity tYrosine-Regulated Kinase3/Calmodulin Kinase-like Vesicle-Associated Signaling Module with Therapeutic Implications in Neuroblastoma. [Abstract]2024 Jan 16;12(1):197. PMID: 38255303 -
PLoS One
A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]2024 Nov 1;19(11):e0308647. PMID: 39485774 -
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bioRxiv
2025 Feb 16:2025.02.12.637879. PMID: 39990424 -
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Solvent & Solubility
DMSO : 50 mg/mL (124.60 mM; Need ultrasonic; 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 5 mg/mL (12.46 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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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 | 2.4921 mL | 12.4604 mL | 24.9209 mL | 62.3022 mL |
| 5 mM | 0.4984 mL | 2.4921 mL | 4.9842 mL | 12.4604 mL | |
| 10 mM | 0.2492 mL | 1.2460 mL | 2.4921 mL | 6.2302 mL | |
| 15 mM | 0.1661 mL | 0.8307 mL | 1.6614 mL | 4.1535 mL | |
| 20 mM | 0.1246 mL | 0.6230 mL | 1.2460 mL | 3.1151 mL | |
| 25 mM | 0.0997 mL | 0.4984 mL | 0.9968 mL | 2.4921 mL | |
| 30 mM | 0.0831 mL | 0.4153 mL | 0.8307 mL | 2.0767 mL | |
| 40 mM | 0.0623 mL | 0.3115 mL | 0.6230 mL | 1.5576 mL | |
| 50 mM | 0.0498 mL | 0.2492 mL | 0.4984 mL | 1.2460 mL | |
| 60 mM | 0.0415 mL | 0.2077 mL | 0.4153 mL | 1.0384 mL | |
| 80 mM | 0.0312 mL | 0.1558 mL | 0.3115 mL | 0.7788 mL | |
| 100 mM | 0.0249 mL | 0.1246 mL | 0.2492 mL | 0.6230 mL |
GSK-626616 Related Classifications
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