PROTAC G9a/GLP degrader 1
Based on 1 Customer Validation
PROTAC G9a/GLP degrader 1 is a G9a/GLP PROTAC degrader with DC50s of 336 nM (G9a) and 988 nM (GLP). PROTAC G9a/GLP degrader 1 exhibits inhibitory activity against G9a with an IC50 of 98 nM. PROTAC G9a/GLP degrader 1 effectively inhibits the migration of breast cancer MCF-7 cells without inhibiting cell proliferation. PROTAC G9a/GLP degrader 1 can be used for the study of breast cancer (Pink: G9a/GLP ligand (HY-152775); Blue: VHL ligand (HY-125845); Black: Linker (HY-140468)).
(Pink: G9a ligand (HY-152775) and G9a ligand (HY-152775); Blue: VHL ligand (HY-125845) and VHL ligand (HY-125845); Black: linker (HY-140468) and linker (HY-140468)).
For research use only. We do not sell to patients.
- Purity: 98.22%
- Formula: C57H76N8O11S
- Molecular Weight:1081.33
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Storage: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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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G9a 336 nM (DC50) |
GLP 988 nM (DC50) |
VHL |
PROTAC G9a/GLP degrader 1 (Compound 4) (0.03-10 μM, 0-72 h) exhibits potent and persistent G9a/GLP degrading ability and effectively reduces the level of the catalytic product H3K9me2 of G9a in breast cancer MCF-7 cells[1].
PROTAC G9a/GLP degrader 1 (0.1-10 μM, 24-72 h) significantly inhibits the migration ability of MCF-7 cells, but does not significantly affect the viability of MCF-7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 cells
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Concentration:0.03, 0.1, 0.3, 1, 3 and 10 μM
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Incubation Time:0, 3, 6, 12, 24, 48 and 72 h
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Result:Initiated the degradation of G9a/GLP within 6 hours and persisted for at least 72 hour.
Effectively reduced the level of the catalytic product H3K9me2 of G9a.
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Cell Line:MCF-7 cells
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Concentration:0.1, 0.3, 1, 3 and 10 μM
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Incubation Time:72 h
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Result:Did not reduce the MCF-7 cell viability.
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Cell Line:MCF-7 cells
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Concentration:3 μM
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Incubation Time:24 h
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Result:Suppressed the migration of MCF-7 cells.
Chemical Information
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Appearance Solid
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Molecular Weight 1081.33
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Formula C57H76N8O11S
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Color White to light yellow
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SMILES
O=C(CCOCCOCCOCCNC(C1=CC=C(C=C1)NC([C@H](CCC2CC2)NC(C3=C(C4=C(N3)CC(C)(C)CC4=O)C)=O)=O)=O)N[C@H](C(N5[C@@H](C[C@H](C5)O)C(NCC6=CC=C(C=C6)C7=C(N=CS7)C)=O)=O)C(C)(C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (92.48 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. 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)
Purity & Documentation
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Data Sheet (271 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. 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 | 0.9248 mL | 4.6239 mL | 9.2479 mL | 23.1197 mL |
| 5 mM | 0.1850 mL | 0.9248 mL | 1.8496 mL | 4.6239 mL | |
| 10 mM | 0.0925 mL | 0.4624 mL | 0.9248 mL | 2.3120 mL | |
| 15 mM | 0.0617 mL | 0.3083 mL | 0.6165 mL | 1.5413 mL | |
| 20 mM | 0.0462 mL | 0.2312 mL | 0.4624 mL | 1.1560 mL | |
| 25 mM | 0.0370 mL | 0.1850 mL | 0.3699 mL | 0.9248 mL | |
| 30 mM | 0.0308 mL | 0.1541 mL | 0.3083 mL | 0.7707 mL | |
| 40 mM | 0.0231 mL | 0.1156 mL | 0.2312 mL | 0.5780 mL | |
| 50 mM | 0.0185 mL | 0.0925 mL | 0.1850 mL | 0.4624 mL | |
| 60 mM | 0.0154 mL | 0.0771 mL | 0.1541 mL | 0.3853 mL | |
| 80 mM | 0.0116 mL | 0.0578 mL | 0.1156 mL | 0.2890 mL |
PROTAC G9a/GLP degrader 1 Related Classifications
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