PROTAC G9a/GLP degrader 1
Based on 1 Customer Validation
PROTAC G9a/GLP degrader 1 is a PROTAC degrader targeting G9a/GLP histone methyltransferases, with DC50 values of 336 nM and 988 nM against G9a and GLP, respectively. PROTAC G9a/GLP degrader 1 reduces H3K9me2 levels, inhibits breast cancer cell migration, and has no effect on cell viability. PROTAC G9a/GLP degrader 1 can be used in breast cancer-related research.
(Pink: G9a ligand (HY-152775); Blue: VHL ligand (HY-125845); Black: 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
Description
IC50 & Target
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G9a 190.4 nM (DC50) |
GLP 988 nM (DC50) |
VHL |
In Vitro
PROTAC G9a/GLP degrader 1 (Compound 4) inhibits the catalytic activity of recombinant G9a, with an IC50 of 190.4 nM[1].
PROTAC G9a/GLP degrader 1 (0.03-3 μM; 0-72 h) induces dose- and time-dependent degradation of G9a and GLP in MCF-7 cells, with a G9a DC50 of 336 nM and a GLP DC50 of 988 nM[1].
PROTAC G9a/GLP degrader 1 (1 μM; 24 h) induces the degradation of G9a/GLP in MCF-7 cells via the canonical PROTAC mechanism, a process that requires simultaneous binding to both G9a/GLP and VHL and is dependent on the ubiquitin-proteasome system[1].
PROTAC G9a/GLP degrader 1 (3 μM; 24 h) selectively degrades G9a and its scaffold chaperone protein WIZ in MCF-7 cells, with minimal reduction of off-target proteins[1].
PROTAC G9a/GLP degrader 1 (1-10 μM; 72 h) reduces the level of H3K9me2 in MCF-7 cells and effectively inhibits the catalytic function of intracellular G9a[1].
PROTAC G9a/GLP degrader 1 (0.1-10 μM; 72 h) does not inhibit the viability of MCF-7 cells[1].
PROTAC G9a/GLP degrader 1 (3 μM; 24 h) increases the phosphorylation level of Smad1/5 in MCF-7 cells, and this mechanism is associated with its anti-migratory effect[1].
PROTAC G9a/GLP degrader 1 (3 μM; 24 h) inhibits the migration 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 human breast cancer cells
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Concentration:0.03, 0.1, 0.3, 1 and 3 μM (dose-dependent assay); 3 μM (time-course assay)
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Incubation Time:24 h (dose-dependent assay); 0, 3, 6, 12, 24, 48 and 72 h (time-course assay)
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Result:Induced dose-dependent degradation of G9a and GLP, with a G9a DC50 of 336 nM and GLP DC50 of 988 nM, and maximum degradation (D_max) of 89% for G9a and 71% for GLP.
Reduced G9a/GLP levels after 6 h of exposure, with sustained low levels maintained for at least 72 h.
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Cell Line:MCF-7 human breast cancer cells
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Concentration:1 μM (compound alone); 1 μM plus 10-200 μM RK-701 (HY-152775) or VHL ligand; 1 μM plus Bortezomib (HY-10227)
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Incubation Time:24 h (compound alone, compound plus RK-701/VHL ligand); 22.5 h compound exposure with 1.5 h Bortezomib pretreatment
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Result:Induced degradation of G9a/GLP only when administered alone; neither RK-701 nor VHL ligand alone, nor their combination, reduced G9a/GLP levels.
Inhibited G9a/GLP degradation induced by the compound when co-exposed with RK-701 or VHL ligand.
Blocked G9a/GLP degradation induced by the compound when pretreated with Bortezomib.
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Cell Line:MCF-7 human breast cancer cells
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Concentration:1 and 10 μM
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Incubation Time:72 h
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Result:Significantly decreased H3K9me2 levels in MCF-7 cells, an effect comparable to the parent inhibitor RK-701, correlating with G9a degradation.
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Cell Line:MCF-7 human breast cancer 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 MCF-7 cell viability at any tested concentration.
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Cell Line:MCF-7 human breast cancer cells
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Concentration:3 μM
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Incubation Time:24 h
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Result:Inhibited MCF-7 cell migration more strongly than the parent inhibitor RK-701, with a level of inhibition superior to reference inactive control compounds.
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Cell Line:MCF-7 human breast cancer cells
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Concentration:3 μM
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Incubation Time:24 h
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Result:Increased Smad1/5 phosphorylation in MCF-7 cells, recapitulating the effect of G9a siRNA knockdown.
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
In Vitro:
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 (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. 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 | 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
HY-178065 Related Classifications
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