PROTAC Chk1 degrader-1
Based on 1 Customer Validation
PROTAC Chk1 degrader-1 is a Chk1-targeting PROTAC.PROTAC Chk1 degrader-1 recruits the Cereblon E3 ligase to induce ubiquitination and proteasomal degradation of Chk1.PROTAC Chk1 degrader-1 exhibits Chk1 degradation activity in malignant melanoma cells without showing a hook effect.PROTAC Chk1 degrader-1 can be used for the research of malignant melanoma.
(Pink: Chk1 Target protein ligand; Blue: Cereblon ligand (HY-103597); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.70%
- CAS No.: 2597167-34-3
- Formula: C43H44N14O9
- Molecular Weight:900.90
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
All PROTACs Isoforms
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Biological Activity
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Cereblon |
Chk1 |
PROTAC Chk1 degrader-1 (PROTAC-2) (1.5-12.5 μM; 18 h) reduces Chk1 protein levels in a concentration-dependent manner in A375 malignant melanoma cells following 18 h of treatment[1].
PROTAC Chk1 degrader-1 (PROTAC-2) (1-12 μM; 12 h) degrades Chk1 protein in A375 malignant melanoma cells with a DC50 of 1.33 μM following 12 h of treatment, without inducing a hook effect or complete degradation at tested concentrations[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A375 malignant melanoma cells
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Concentration:1.5 μM, 6.3 μM, 12.5 μM
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Incubation Time:18 h
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Result:Reduced Chk1 protein levels in a concentration-dependent manner.
Was the most efficient Chk1 degrader among the tested PROTAC series, with greater degradation observed at higher concentrations.
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Cell Line:A375 malignant melanoma cells
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Concentration:1 μM, 2 μM, 3 μM, 4 μM, 5 μM, 6 μM, 12 μM
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Incubation Time:12 h
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Result:Degraded Chk1 with a DC50 of 1.33 μM.
Did not induce complete Chk1 degradation even at the highest tested concentration of 12 μM.
Did not detect a hook effect.
Chemical Information
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CAS No. 2597167-34-3
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Appearance Solid
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Molecular Weight 900.90
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Formula C43H44N14O9
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Color White to off-white
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SMILES
N#CCC1=CC=C(NC2=NC(C(NCC3=CN(CCOCCOCCNC(COC4=C5C(C(N(C6C(NC(CC6)=O)=O)C5=O)=O)=CC=C4)=O)N=N3)=O)=CC(NC7=NNC(C8CC8)=C7)=N2)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 100 mg/mL (111.00 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 (protect from light). 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 (protect from light). 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)
Purity & Documentation
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Data Sheet (269 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 (protect from light). 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 | 1.1100 mL | 5.5500 mL | 11.1000 mL | 27.7500 mL |
| 5 mM | 0.2220 mL | 1.1100 mL | 2.2200 mL | 5.5500 mL | |
| 10 mM | 0.1110 mL | 0.5550 mL | 1.1100 mL | 2.7750 mL | |
| 15 mM | 0.0740 mL | 0.3700 mL | 0.7400 mL | 1.8500 mL | |
| 20 mM | 0.0555 mL | 0.2775 mL | 0.5550 mL | 1.3875 mL | |
| 25 mM | 0.0444 mL | 0.2220 mL | 0.4440 mL | 1.1100 mL | |
| 30 mM | 0.0370 mL | 0.1850 mL | 0.3700 mL | 0.9250 mL | |
| 40 mM | 0.0278 mL | 0.1388 mL | 0.2775 mL | 0.6938 mL | |
| 50 mM | 0.0222 mL | 0.1110 mL | 0.2220 mL | 0.5550 mL | |
| 60 mM | 0.0185 mL | 0.0925 mL | 0.1850 mL | 0.4625 mL | |
| 80 mM | 0.0139 mL | 0.0694 mL | 0.1388 mL | 0.3469 mL | |
| 100 mM | 0.0111 mL | 0.0555 mL | 0.1110 mL | 0.2775 mL |