SK2188
Based on 1 Customer Validation
SK2188 (JB325) is a highly efficient and selective PROTAC degrader targeting AURKA (DC50 = 3.9 nM). SK2188 induces DNA damage and cell apoptosis. SK2188 indirectly degrades MYCN, inhibits tumor cell proliferation, and provides insights into the study of MYCN-amplified neuroblastoma.
(Pink: Aurora Kinase ligand (HY-13252); Blue: Cereblon ligand (HY-14658); Black: linker (HY-W008005)).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.87%
- No. CAS: 3038446-94-2
- Fòrmula: C43H46ClFN6O10S
- Peso molecular:893.38
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Ver todos los productos específicos de isoformas PROTACs
MoreVer todos los productos específicos de isoformas Caspase
MoreVer todos los productos específicos de isoformas Aurora Kinase
More
Actividad biológica
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Caspase 3 |
Caspase-7 |
Aurora A |
Cereblon |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| IMR-32 | IC50 |
21.5 nM
Compound: SK2188
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Antiproliferative activity against human IMR-32 cells assessed as reduction in cell viability incubated for 48 hrs
Antiproliferative activity against human IMR-32 cells assessed as reduction in cell viability incubated for 48 hrs
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[PMID: 36549117] |
| SK-N-AS | IC50 |
6693 nM
Compound: SK2188
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Antiproliferative activity against human SK-N-AS cells assessed as reduction in cell viability incubated for 48 hrs
Antiproliferative activity against human SK-N-AS cells assessed as reduction in cell viability incubated for 48 hrs
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[PMID: 36549117] |
SK2188 (10-10000 nM, 48-120 h) efficiently inhibits proliferation in MYCN amplified cells and is effective in NB patient-derived organoids cells[1].
SK2188 (10-1000 nM, 24 h) inhibits cell growth by inducing apoptosis in NGP cells[1].
SK2188 (10-1000 nM, 24 h) degrades AURKA in NGP cells, triggering DNA damage and replication stress[1].
SK2188 (100-1000 nM, 3h) has high target selectivity and degradation specificity in NGP cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NGP cells, IMR-32 cells, N206 cells, SK-N-AS cells, NB patient-derived organoids cells
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Concentration:10 nM, 100 nM, 1000 nM, 10000 nM
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Incubation Time:48 h (NGP cells, IMR-32 cells, N206 cells, SK-N-AS cells); 120 h (NB patient-derived organoids cells)
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Result:Inhibited cell viability with IC50s of 31.9 nM and 21.5 nM in NGP and IMR-32 cells, respectively, which were significantly lower than those of the parent inhibitor MK-5108 (IC50s: 348.9 nM and 199.3 nM).
Inhibited cell viability with IC50s of 131.3 nM and 26.4 nM in MYCN-amplified organoids NB139 and NB067, respectively, which were significantly lower than those of the parent inhibitor MK-5108 (IC50s: 899.7 nM and 75.3 nM).
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Cell Line:NGP cells
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Concentration:10 nM, 100 nM, 1000 nM
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Incubation Time:24 h
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Result:Significantly activated Caspase 3/7 at 10 nM and exerted a stronger apoptosis-inducing effect than MK-5108 at 1000 nM.
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Cell Line:NGP neuroblastoma cells
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Concentration:10 nM, 100 nM, 500 nM, 1000 nM
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Incubation Time:1 h, 3 h, 6 h, 24 h, 48 h, 72 h
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Result:Induced 89 % AURKA degradation (DC50 = 3.9 nM) at 24 hours. Reduced MYCN protein levels (73 % degradation at 72 hours). Increased DNA damage markers (γH2AX, pCHK1)at 24 hours.
Chemical Information
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No. CAS 3038446-94-2
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Appearance Solid
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Peso molecular 893.38
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Fòrmula C43H46ClFN6O10S
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Color White to off-white
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SMILES
O=C(N1C2C(NC(CC2)=O)=O)C3=CC=CC(OCCOCCOCCOCCNC([C@@]4(CC[C@H](CC4)OC5=C(C(Cl)=CC=C5)F)CC6=CC=CC(NC7=NC=CS7)=N6)=O)=C3C1=O
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Synonyms
JB325
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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 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (111.93 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.5 mg/mL (2.80 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.1193 mL | 5.5967 mL | 11.1934 mL | 27.9836 mL |
| 5 mM | 0.2239 mL | 1.1193 mL | 2.2387 mL | 5.5967 mL | |
| 10 mM | 0.1119 mL | 0.5597 mL | 1.1193 mL | 2.7984 mL | |
| 15 mM | 0.0746 mL | 0.3731 mL | 0.7462 mL | 1.8656 mL | |
| 20 mM | 0.0560 mL | 0.2798 mL | 0.5597 mL | 1.3992 mL | |
| 25 mM | 0.0448 mL | 0.2239 mL | 0.4477 mL | 1.1193 mL | |
| 30 mM | 0.0373 mL | 0.1866 mL | 0.3731 mL | 0.9328 mL | |
| 40 mM | 0.0280 mL | 0.1399 mL | 0.2798 mL | 0.6996 mL | |
| 50 mM | 0.0224 mL | 0.1119 mL | 0.2239 mL | 0.5597 mL | |
| 60 mM | 0.0187 mL | 0.0933 mL | 0.1866 mL | 0.4664 mL | |
| 80 mM | 0.0140 mL | 0.0700 mL | 0.1399 mL | 0.3498 mL | |
| 100 mM | 0.0112 mL | 0.0560 mL | 0.1119 mL | 0.2798 mL |
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