P60-L3-VHL
Based on 1 Customer Validation
P60-L3-VHL is a PROTAC degrader targeting Foxp3. P60-L3-VHL triggers the ubiquitination modification of Foxp3 by conjugating the Foxp3-targeting peptide P60 with the VHL E3 ubiquitin ligase ligand via a long linker, and mediates protein degradation through the proteasome pathway. P60-L3-VHL blocks the nuclear translocation of Foxp3, relieves the transcriptional inhibition of IL2 and IFN-γ, and inhibits the differentiation of iTreg cells. P60-L3-VHL is applicable to cancer-related research.
(Pink: FOXP3 ligand (HY-162946); Blue: VHL ligand (HY-125845); Black: linker (HY-162947)).
For research use only. We do not sell to patients.
- Purity: 99.84%
- Formula: C135H189N33O27S3
- Molecular Weight:2802.35
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Storage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All PROTACs Isoforms
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Biological Activity
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FOXP3 |
IL-2 |
P60-L3-VHL (compound L3) (10-1000 nM; 24 h) reduces the expression level of Foxp3 protein in Foxp3-transfected HEK293T cells, and significant protein degradation is observed after treatment with 1 μM for 24 h[1].
P60-L3-VHL (1 μM; 24 h) inhibits the nuclear translocation of HA-Foxp3 in transfected HeLa cells[1].
P60-L3-VHL (3 μM; 12-48 h) reduces Foxp3 protein levels in Foxp3-transfected HEK293T cells; it mediates Foxp3 degradation in Foxp3-transfected HEK293T cells via the proteasome pathway, as combined treatment with 10 μM MG132 (HY-13259) reverses Foxp3 downregulation[1].
P60-L3-VHL (1-3 μM; 24 h) inhibits the nuclear translocation of HA-Foxp3 in transfected HEK293T cells, with potency comparable to that of 100 μM P60 peptide (HY-P1684)[1].
P60-L3-VHL (1-4 μM; 48-72 h) suppresses Foxp3 expression in in vitro activated mouse Treg cells in a dose-dependent manner[1].
P60-L3-VHL (72 h) reduces Foxp3 mRNA expression and upregulates IL2 and IFN-g mRNA expression in activated mouse iTreg cells in vitro[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T cells (transfected with Foxp3 plasmid)
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Concentration:10, 50, 100, 500, 1000 nM
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Incubation Time:24 h
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Result:Decreased Foxp3 protein levels in cells treated with 500 nM P60-L3-VHL.
Showed significant reduction of Foxp3 protein levels at the 1 μM concentration.
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Cell Line:HEK293T cells (transfected with Foxp3 plasmid)
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Concentration:3 μM
10 μM (MG132) -
Incubation Time:12, 24, 48 h
4 h (MG132) -
Result:Lowered Foxp3 protein levels compared to control levels at 24 h.
Sustained reduced Foxp3 protein levels through 48 h.
Reduced Foxp3 levels over time in cells treated with P60-L3-VHL alone.
Increased Foxp3 expression compared to P60-L3-VHL alone when co-treated with MG132.
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Cell Line:Treg cells
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Concentration:1, 2, 3, 4 μM
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Incubation Time:72 h
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Result:Suppressed Foxp3 expression in in vitro activated mouse Treg cells in a dose-dependent manner.
Chemical Information
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Appearance Solid
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Molecular Weight 2802.35
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Formula C135H189N33O27S3
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Color White to off-white
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SMILES
O=C(NCC1=CC=C(C=C1)C2=C(N=CS2)C)[C@@H]3C[C@H](CN3C([C@@H](NC(COCCOCCNC(CCCCCN4C=C(N=N4)CCCC(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@@H](CO)C(N[C@H](C(N[C@@H](CCCNC(N)=N)C(N[C@H](C(N[C@H](C(N[C@H](C(N5CCC[C@H]5C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N)=O)CCSC)=O)C)=O)CC6=CC=CC=C6)=O)CC7=CC=CC=C7)=O)=O)CC8=CNC9=C8C=CC=C9)=O)CCSC)=O)CCCCN)=O)=O)CC%10=CC=CC=C%10)=O)=O)CCC(N)=O)=O)CC%11=CC=CC=C%11)=O)CC(O)=O)=O)CCCNC(N)=N)=O)=O)=O)C(C)(C)C)=O)O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H2O : 100 mg/mL (35.68 mM; Need ultrasonic)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (282 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 (sealed storage, away from moisture). 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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| H2O | 1 mM | 0.3568 mL | 1.7842 mL | 3.5684 mL | 8.9211 mL |
| 5 mM | 0.0714 mL | 0.3568 mL | 0.7137 mL | 1.7842 mL | |
| 10 mM | 0.0357 mL | 0.1784 mL | 0.3568 mL | 0.8921 mL | |
| 15 mM | 0.0238 mL | 0.1189 mL | 0.2379 mL | 0.5947 mL | |
| 20 mM | 0.0178 mL | 0.0892 mL | 0.1784 mL | 0.4461 mL | |
| 25 mM | 0.0143 mL | 0.0714 mL | 0.1427 mL | 0.3568 mL | |
| 30 mM | 0.0119 mL | 0.0595 mL | 0.1189 mL | 0.2974 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
P60-L3-VHL Related Classifications
HY-162943 Related Classifications
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