PROTAC TG2 degrader-2
Based on 1 Customer Validation
PROTAC TG2 degrader-2 (compound 7) is a selective, competitive degrader targeting Transglutaminase 2 (TG2), with Kd > 100 μM. PROTAC TG2 degrader-2 inhibits the cell migration and decreases the level of TG2 in ovarian cancer cells. PROTAC TG2 degrader-2 can be used for ovarian cancer study.
(Pink: TGM2 ligand (HY-128595); Blue: VHL ligand (HY-125845); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.15%
- CAS No.: 3033465-51-6
- Formula: C47H57N9O6S
- Molecular Weight:876.08
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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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Metabolism/Protease Compound Library
HY-L012
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Anti-Cancer Compound Library
HY-L025
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Glutamine Metabolism Compound Library
HY-L064
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Anti-Cancer Metabolism Compound Library
HY-L083
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Mitochondria-Targeted Compound Library
HY-L089
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Cuproptosis Compound Library
HY-L133
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Metabolic Enzyme Compound Library
HY-L146
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PROTAC Library
HY-L151
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Anti-Ovarian Cancer Compound Library
HY-L173
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Amino Acid Metabolism Compound Library
HY-L189
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High-Throughput Bioactive Compound Library
HY-L205
All PROTACs Isoforms
More
Biological Activity
> 100 μM (TG2)
PROTAC TG2 degrader-2 (Compound 7) (10 μΜ, up to 24h) inhibits the migration of OVCAR5 and SKOV3 cell lines in both wound-healing assays and transwell migration assays[1].
PROTAC TG2 degrader-2 (10 μΜ) reduces the adhesion of OVCAR5 and SKOV3 cells to fibronectin[1].
PROTAC TG2 degrader-2 (up to 10 μΜ, 6 h) reduces the level of Transglutaminase 2(TG2) within 6 h in a concentration-dependent manner in both OVCAR5 and SKOV3 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:OVCAR5 and SKOV3 cells
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Concentration:10 μΜ
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Incubation Time:Wound-healing assay: 24 h (OVCAR5 cells) and 12 h (OVCAR5 cells) (SKOV3 cells)
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Result:Inhibited the migration.
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Cell Line:OVCAR5 and SKOV3 cells
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Concentration:0.1, 1 and 10 μΜ (OVCAR5 cells), 1 and 10 μΜ (OVCAR5 cells) (SKOV3 cells)
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Incubation Time:6 h and 24 h
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Result:Reduced the level of TG2.
Chemical Information
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CAS No. 3033465-51-6
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Appearance Solid
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Molecular Weight 876.08
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Formula C47H57N9O6S
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Color White to off-white
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SMILES
O=C(CCOCCN(C1=CC(C)=NC(NC2=CC=C(NC(CC3=CC=CC=C3)=O)C=C2)=N1)C)N[C@@H](C(C)(C)C)C(N4[C@H](C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)C[C@@H](O)C4)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : ≥ 100 mg/mL (114.14 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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). 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). 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 (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Valdivia A, el at. Discovery and Characterization of PROTACs Targeting Tissue Transglutaminase (TG2). J Med Chem. 2023;66(14):9445-9465. doi:10.1021/acs.jmedchem.2c01859Valdivia A, Vagadia PP, Guo G, O'Brien E, Matei D, Schiltz GE. Discovery and Characterization of PROTACs Targeting Tissue Transglutaminase (TG2). J Med Chem. 2023;66(14):9445-9465. doi:10.1021/acs.jmedchem.2c01859 [Content Brief]
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). 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 | 1.1414 mL | 5.7072 mL | 11.4145 mL | 28.5362 mL |
| 5 mM | 0.2283 mL | 1.1414 mL | 2.2829 mL | 5.7072 mL | |
| 10 mM | 0.1141 mL | 0.5707 mL | 1.1414 mL | 2.8536 mL | |
| 15 mM | 0.0761 mL | 0.3805 mL | 0.7610 mL | 1.9024 mL | |
| 20 mM | 0.0571 mL | 0.2854 mL | 0.5707 mL | 1.4268 mL | |
| 25 mM | 0.0457 mL | 0.2283 mL | 0.4566 mL | 1.1414 mL | |
| 30 mM | 0.0380 mL | 0.1902 mL | 0.3805 mL | 0.9512 mL | |
| 40 mM | 0.0285 mL | 0.1427 mL | 0.2854 mL | 0.7134 mL | |
| 50 mM | 0.0228 mL | 0.1141 mL | 0.2283 mL | 0.5707 mL | |
| 60 mM | 0.0190 mL | 0.0951 mL | 0.1902 mL | 0.4756 mL | |
| 80 mM | 0.0143 mL | 0.0713 mL | 0.1427 mL | 0.3567 mL | |
| 100 mM | 0.0114 mL | 0.0571 mL | 0.1141 mL | 0.2854 mL |
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