SK2188
Based on 1 Customer Validation
SK2188 (JB325) is a selective AURKA PROTAC degrader with a DC50 of 3.9 nM. SK2188 recruits CRBN E3 ubiquitin ligase to target and degrade AURKA, abrogating both its catalytic and non-kinase functions, which leads to the destabilization and degradation of the oncogenic protein MYCN, ultimately inducing replication stress, DNA damage and apoptosis. SK2188 is applicable to research related to neuroblastoma.
(Pink: Aurora A ligand (HY-13252); Blue: Cereblon ligand (HY-14658); Black: linker (HY-W008005)).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.87%
- CAS No.: 3038446-94-2
- 화학식: C43H46ClFN6O10S
- 분자량:893.38
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보관: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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
Aurora A 3.90 nM (DC50) |
Caspase 3 |
Caspase-7 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| IMR-32 | IC50 |
21.5 nM
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Half-maximal cell growth inhibition in human IMR-32 neuroblastoma cells after 48 h incubation, assessed by Incucyte Live-Cell confluency assay normalized to DMSO controls.
Half-maximal cell growth inhibition in human IMR-32 neuroblastoma cells after 48 h incubation, assessed by Incucyte Live-Cell confluency assay normalized to DMSO controls.
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36549117 |
| SK-N-AS | IC50 |
6693.0 nM
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Half-maximal cell growth inhibition in human SK-N-AS neuroblastoma cells after 48 h incubation, assessed by Incucyte Live-Cell confluency assay normalized to DMSO controls.
Half-maximal cell growth inhibition in human SK-N-AS neuroblastoma cells after 48 h incubation, assessed by Incucyte Live-Cell confluency assay normalized to DMSO controls.
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36549117 |
In Vitro
SK2188 (JB325) (0.1 nM-1 μM; 3-24 h) potently and selectively degrades AURKA in NGP neuroblastoma cells, with a DC50 of 3.9 nM[1].
SK2188 (0.1 nM-1 μM; 24 h) induces apoptosis, specifically degrades AURKA, reduces MYCN, and upregulates pCHK1, pRPA32 and yH2AX to trigger replication stress and DNA damage in NGP cells[1].
SK2188 (500 nM; 1-72 h) induces rapid and sustained degradation of AURKA protein in NGP cells, accompanied by time-dependent downregulation of MYCN protein[1].
SK2188 (10 nM-10 μM; 48-120 h) potently inhibits the growth of MYCN-amplified NGP and IMR-32 neuroblastoma cells with IC50 values of 31.9 nM and 21.5 nM, respectively, but shows limited activity in N206 and SK-N-AS cells. It also potently reduces the cell viability of NB067 and NB139 neuroblastoma organoids with IC50 values of 26.4 nM and 131.3 nM, respectively, but exhibits limited activity in 000GKX and NB059 organoids[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NGP
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Concentration:0.1, 1, 10, 100, 500, 1000 nM
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Incubation Time:1, 3, 6, 24, 48, 72 h
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Result:Potently degraded AURKA protein in a dose-dependent manner.
Rapidly degraded AURKA protein, followed by a time-dependent decrease in MYCN protein expression.
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Cell Line:NGP, IMR-32, SK-N-AS, N206, derived organoids NB059, 000GKX, NB139, NB067
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Concentration:10, 100, 1000, 10000 nM (logarithmic gradients)
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Incubation Time:48, 120 h
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Result:Inhibited cell proliferation and growth across multiple cell lines.
Reduced the cell viability of derived organoids, exhibiting anti-proliferative activity
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Cell Line:NGP
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Concentration:10, 100, 1000 nM
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Incubation Time:24 h
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Result:Significantly increased caspase 3/7 activity, inducing cell apoptosis.
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Cell Line:NGP
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Concentration:10, 100, 1000 nM
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Incubation Time:24 h
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Result:Specifically downregulated AURKA and MYCN proteins, while concurrently upregulating levels of replicative stress and DNA damage markers (pCHK1, pRPA32, and yH2AX).
Chemical Information
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CAS No. 3038446-94-2
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Appearance Solid
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분자량 893.38
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
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)
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: ≥ 2.5 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.
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.
순도&문서
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Data Sheet (284 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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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, 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 |
SK2188 Related Classifications
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