SGC-GAK-1
Based on 2 publication(s) in Google Scholar
SGC-GAK-1 is a potent, selective cyclin G-associated kinase (GAK) inhibitor with a Ki of 3.1 nM. SGC-GAK-1 is a chemical probe for GAK.
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- Pureza: 99.92%
- No. CAS: 2226517-76-4
- Fòrmula: C18H17BrN2O3
- Peso molecular:389.24
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) SGC-GAK-1
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Actividad biológica
Ki: 3.1 nM (GAK)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CWR22R | IC50 |
0.17 μM
Compound: 11; SGC-GAK-1, CA93.0
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Cytotoxicity against human 22Rv1 cells after 72 hrs by MTS assay
Cytotoxicity against human 22Rv1 cells after 72 hrs by MTS assay
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[PMID: 30768268] |
| HEK293 | IC50 |
48 nM
Compound: 3; CA93.0
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Inhibition of tracer 5 binding to human N-terminal nano luciferase-fused GAK expressed in HEK293 cells measured after 2 hrs by nanoBRET assay
Inhibition of tracer 5 binding to human N-terminal nano luciferase-fused GAK expressed in HEK293 cells measured after 2 hrs by nanoBRET assay
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[PMID: 30973735] |
| Huh-7 | CC50 |
>10 μM
Compound: 29
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Cytotoxicity against human Huh-7 cells infected with DENV2 by alamar blue assay
Cytotoxicity against human Huh-7 cells infected with DENV2 by alamar blue assay
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[PMID: 32631507] |
| LNCaP | IC50 |
0.65 μM
Compound: 11; SGC-GAK-1, CA93.0
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Cytotoxicity against human LNCAP cells after 72 hrs by MTS assay
Cytotoxicity against human LNCAP cells after 72 hrs by MTS assay
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[PMID: 30768268] |
SGC-GAK-1 potently binds cyclin G-associated kinase (GAK), adaptor protein 2-associated kinase (AAK1), serine/threonine kinase 16 (STK16) with Kis of 3.1 nM, 53 μM, 51 μM, respectively[1].
SGC-GAK-1 potently binds cyclin G-associated kinase (GAK), receptor-interacting protein kinase 2 (RIPK2), AarF domain containing kinase 3 (ADCK3), and nemo-like kinase (NLK) with KDs of 1.9 nM, 110 nM, 190 nM, and 520 nM, respectively[1].
SGCGAK-1 (0.1, 1, and 10 μM, 48 hours or 72 hours) shows strong growth inhibition in LNCaP, VCaP, and 22Rv1 cells at 10 μM, but minimal effect in PC3 and DU145 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Prostate cancer cells (22Rv1, LNCaP, VCaP, PC3, DU145)
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Concentration:0.1, 1, and 10 µM
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Incubation Time:48 hours or 72 hours
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Result:Showed potent antiproliferative activity in LNCaP and 22Rv1 cells with IC50s of 0.05±0.15 µM and 0.17±0.65 µM, respectively.
Chemical Information
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No. CAS 2226517-76-4
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Appearance Solid
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Peso molecular 389.24
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Fòrmula C18H17BrN2O3
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Color Light yellow to yellow
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SMILES
COC1=C(C(OC)=CC(NC2=CC=NC3=CC=C(C=C23)Br)=C1)OC
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Antiviral Res
Numb-associated kinases are required for SARS-CoV-2 infection and are cellular targets for antiviral strategies. [Abstract]2022 Aug:204:105367. PMID: 35738348
Solvente y solubilidad
DMSO : 41.67 mg/mL (107.05 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: ≥ 2.08 mg/mL (5.34 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 2.08 mg/mL (5.34 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.08 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
Pureza y Documentación
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Ficha de datos (279 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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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.5691 mL | 12.8455 mL | 25.6911 mL | 64.2277 mL |
| 5 mM | 0.5138 mL | 2.5691 mL | 5.1382 mL | 12.8455 mL | |
| 10 mM | 0.2569 mL | 1.2846 mL | 2.5691 mL | 6.4228 mL | |
| 15 mM | 0.1713 mL | 0.8564 mL | 1.7127 mL | 4.2818 mL | |
| 20 mM | 0.1285 mL | 0.6423 mL | 1.2846 mL | 3.2114 mL | |
| 25 mM | 0.1028 mL | 0.5138 mL | 1.0276 mL | 2.5691 mL | |
| 30 mM | 0.0856 mL | 0.4282 mL | 0.8564 mL | 2.1409 mL | |
| 40 mM | 0.0642 mL | 0.3211 mL | 0.6423 mL | 1.6057 mL | |
| 50 mM | 0.0514 mL | 0.2569 mL | 0.5138 mL | 1.2846 mL | |
| 60 mM | 0.0428 mL | 0.2141 mL | 0.4282 mL | 1.0705 mL | |
| 80 mM | 0.0321 mL | 0.1606 mL | 0.3211 mL | 0.8028 mL | |
| 100 mM | 0.0257 mL | 0.1285 mL | 0.2569 mL | 0.6423 mL |
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