PROTAC Mcl1 degrader-1
Based on 1 publication(s) in Google Scholar
PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC) based on Cereblon ligand, is a potently and selectively Mcl-1 (Bcl-2 family member) inhibitor with an IC50 of 0.78 μM. PROTAC Mcl1 degrader-1 inhibits Bcl-2 with an IC50 of 0.54 μM.
(Pink: Bcl-2 Family ligand (HY-129701); Blue: Cereblon ligand (HY-10984); Black: linker (HY-W010505)).
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- Reinheit: 98.13%
- CAS. Nr.: 2163793-38-0
- Formel: C45H45BrN6O8S
- Molecular Weight:909.84
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Speicherung:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) PROTAC Mcl1 degrader-1
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Biologische Aktivität
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Mcl-1 0.78 μM (IC50) |
Bcl-2 0.54 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HeLa | DC50 |
0.7 μM
Compound: C3
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Induction of CRBN-mediated Mcl-1 degradation in human HeLa cells assessed as Mcl-1 removal activity measured at 12 hrs by Western blot analysis
Induction of CRBN-mediated Mcl-1 degradation in human HeLa cells assessed as Mcl-1 removal activity measured at 12 hrs by Western blot analysis
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[PMID: 31389699] |
PROTAC Mcl1 degrader-1 (compound C3) induces the ubiquitination and proteasomal degradation of Mcl-1 by introducing the E3 ligase cereblon (CRBN)-binding ligand Pomalidomide (HY-10984) to Mcl-1 inhibitor S1-6 with μM-range affinity[1].
PROTAC Mcl1 degrader-1 (0-10 μM; 0-24 h) induces selective depletion of Mcl-1 or Bcl-2 protein in HeLa cells in a time- and concentration-dependent manner[1].
PROTAC Mcl1 degrader-1 (0-2 μM; 24 h) shows cytotoxicity against H23 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells and H23 cells
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Concentration:0.3, 1.0, 3.0 and 10 μM
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Incubation Time:0-24 h
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Result:Induced time- and concentration-dependent selective depletion of Mcl-1 or Bcl-2 protein in HeLa cells. Induced Mcl-1 depletion and PARP cleavage in H23 cells (0-10 μM; 12 h).
Chemical Information
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CAS. Nr. 2163793-38-0
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Appearance Solid
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Molecular Weight 909.84
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Formel C45H45BrN6O8S
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Color Light yellow to yellow
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SMILES
O=C(C1=CC=CC(NCCCCCCNC(CCCCC(NCCN2C(C3=C4C(C2=O)=CC=C(C4=CC=C3)SC5=CC=C(C=C5)Br)=O)=O)=O)=C1C6=O)N6C7CCC(NC7=O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (1)
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Journal Impact Factor
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Most Recent
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Structure
PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. [Abstract]2024 Dec 5;32(12):2352-2363.e8. PMID: 39389062
Lösungsmittel & Löslichkeit
DMSO : 50 mg/mL (54.95 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 (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 (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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (2.75 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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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.
Reinheit & Dokumentation
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Data Sheet (273 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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Handling Instructions (2659 KB)
Verweise
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 (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 |
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| DMSO | 1 mM | 1.0991 mL | 5.4955 mL | 10.9909 mL | 27.4774 mL |
| 5 mM | 0.2198 mL | 1.0991 mL | 2.1982 mL | 5.4955 mL | |
| 10 mM | 0.1099 mL | 0.5495 mL | 1.0991 mL | 2.7477 mL | |
| 15 mM | 0.0733 mL | 0.3664 mL | 0.7327 mL | 1.8318 mL | |
| 20 mM | 0.0550 mL | 0.2748 mL | 0.5495 mL | 1.3739 mL | |
| 25 mM | 0.0440 mL | 0.2198 mL | 0.4396 mL | 1.0991 mL | |
| 30 mM | 0.0366 mL | 0.1832 mL | 0.3664 mL | 0.9159 mL | |
| 40 mM | 0.0275 mL | 0.1374 mL | 0.2748 mL | 0.6869 mL | |
| 50 mM | 0.0220 mL | 0.1099 mL | 0.2198 mL | 0.5495 mL |
PROTAC Mcl1 degrader-1 Related Classifications
HY-125877 Related Classifications
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