PROTAC MLKL Degrader-1
Based on 1 Customer Validation
PROTAC MLKL Degrader-1 is a selective MLKL PROTAC degrader with a DC50 of 2.4 μM. PROTAC MLKL Degrader-1 blocks necroptosis without modulating the phosphorylation of RIPK1 or RIPK3, and exhibits a linear correlation between MLKL levels and necroptotic cell death.
(Pink: Mixed Lineage Kinase ligand (HY-175705); Blue: Cereblon ligand (HY-W249500); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.76%
- CAS No.: 3032600-90-8
- Formula: C46H55F2N9O9S
- Molecular Weight:948.05
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Storage:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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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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All PROTACs Isoforms
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Biological Activity
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Cereblon |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-29 | EC50 |
1.2 μM
Compound: 36
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Protection against TSZ-induced necroptosis in human HT-29 cells assessed as cell viability incubated for 24 hrs by CellTiter Glo assay
Protection against TSZ-induced necroptosis in human HT-29 cells assessed as cell viability incubated for 24 hrs by CellTiter Glo assay
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[PMID: 37535857] |
PROTAC MLKL Degrader-1 (Compound 36) (0.1-10 μM; 2-24 h) dose-dependently degrades MLKL in HT29 cells, with a DC50 of 2.4 μM. It achieves a degradation rate of > 90% within 5 h at a concentration of 10 μM, and this effect lasts for up to 24 h[1].
PROTAC MLKL Degrader-1 (0.1-10 μM; 24 h) dose-dependently protects HT29 cells against TSZ-induced necroptosis, with an EC50 of 1.2 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT29 colon cancer cells
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Concentration:0.1, 0.3, 1, 3 and 10 μM
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Incubation Time:24 h
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Result:Protected cells from necroptosis in a dose-dependent manner, reaching 100% protection at 10 μM, with an EC50 of 1.2 μM.
Demonstrated anti-necroptotic efficacy that correlated linearly with the extent of MLKL degradation.
Chemical Information
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CAS No. 3032600-90-8
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Appearance Solid
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Molecular Weight 948.05
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Formula C46H55F2N9O9S
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Color Off-white to light yellow
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SMILES
O=C(C1=C(NN=C1C2=CC=C(C=C2)NS(C(F)F)(=O)=O)NC3=CC=CC(OCCCCCCCC(N4CCC5(CCN(CC5)C(C6=CC=C(C(N7CCC(NC7=O)=O)=C6)OC)=O)CC4)=O)=C3)N
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL (105.48 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, stored under nitrogen). 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, stored under nitrogen). 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 (270 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)
- 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, stored under nitrogen). 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 | 1.0548 mL | 5.2740 mL | 10.5480 mL | 26.3699 mL |
| 5 mM | 0.2110 mL | 1.0548 mL | 2.1096 mL | 5.2740 mL | |
| 10 mM | 0.1055 mL | 0.5274 mL | 1.0548 mL | 2.6370 mL | |
| 15 mM | 0.0703 mL | 0.3516 mL | 0.7032 mL | 1.7580 mL | |
| 20 mM | 0.0527 mL | 0.2637 mL | 0.5274 mL | 1.3185 mL | |
| 25 mM | 0.0422 mL | 0.2110 mL | 0.4219 mL | 1.0548 mL | |
| 30 mM | 0.0352 mL | 0.1758 mL | 0.3516 mL | 0.8790 mL | |
| 40 mM | 0.0264 mL | 0.1318 mL | 0.2637 mL | 0.6592 mL | |
| 50 mM | 0.0211 mL | 0.1055 mL | 0.2110 mL | 0.5274 mL | |
| 60 mM | 0.0176 mL | 0.0879 mL | 0.1758 mL | 0.4395 mL | |
| 80 mM | 0.0132 mL | 0.0659 mL | 0.1318 mL | 0.3296 mL | |
| 100 mM | 0.0105 mL | 0.0527 mL | 0.1055 mL | 0.2637 mL |
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