HGC652
Based on 1 Customer Validation
HGC652 is a molecular glue degrader targeting TRIM21 with a TRIM21-dependent nuclear membrane disruption effect. HGC652 binds to the PRY-SPRY domain of TRIM21 with high affinity (Ka=0.061 μM), mediates the interaction between TRIM21 and NUP98, and redirects E3 ligase activity. By triggering the polyubiquitination and proteasomal degradation of nucleoporins (such as NUP155 and GLE1), HGC652 disrupts nuclear membrane integrity, alters nuclear morphology, induces genomic instability, and thereby induces cancer cell death.
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- Pureza: 98.86%
- No. CAS: 3055558-98-7
- Fòrmula: C23H28FNO3S2
- Peso molecular:449.60
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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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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Oxygen Sensing Compound Library
HY-L045
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Ubiquitination Compound Library
HY-L050
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Molecular Glue Compound Library
HY-L137
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Metabolic Enzyme Compound Library
HY-L146
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Mitophagy Compound Library
HY-L180
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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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Cell Proliferation Compound Library
HY-L201
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High-Throughput Bioactive Compound Library
HY-L205
Actividad biológica
The IC50 of HGC652 for inhibiting the proliferation of PANC-1 pancreatic cancer cells is 0.094 μM (72 h)[1].
HGC652 (0.5-5 μM; 24 h) induces dose-dependent degradation of GLE1 and NUP155 in PANC-1 cells via a proteasome-dependent pathway[1].
HGC652 (0.05-5 μM; 24 h incubation) induces NUP155 degradation in PANC-1 cells, and this process is independent of GLE1; whereas the degradation of GLE1 depends on NUP155, indicating that NUP155 is its primary target[1].
HGC652 (0.01-25 μM; room temperature; 40 min) induces the formation of a concentration-dependent ternary complex between TRIM21PRY-SPRY and NUP98APD proteins[1].
HGC652 (0.5-15 μM; incubated on ice; 30 min; incubated with streptavidin agarose beads for 2 h) induces direct interaction between TRIM21 (124-475) and NUP98APD in cell-free Strep-tag pull-down assays[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PANC-1 pancreatic cancer cells
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Concentration:0.5 μM; 5 μM
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Incubation Time:24 h
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Result:Induced dose-dependent degradation of GLE1 and NUP155 proteins in PANC-1 cells.
Prevented degradation of GLE1 and NUP155 when cells were pre-treated with 5 μM proteasome inhibitor MG132, but not by autophagy-lysosome inhibitors 100 μM chloroquine or 0.1 μM bafilomycin A1.
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Cell Line:PANC-1 pancreatic cancer cells (TRIM21 siRNA-transfected)
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Concentration:0.020, 0.078, 0.313, 1.25, 5 μM
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Incubation Time:48 h (siRNA transfection); 24 h (compound incubation)
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Result:Completely abrogated degradation of GLE1 and NUP155 in TRIM21-knockdown PANC-1 cells, compared to control siRNA-transfected cells.
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Cell Line:PANC-1 pancreatic cancer cells (GLE1 or NUP155 siRNA-transfected)
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Concentration:0.05, 0.5, 5 μM
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Incubation Time:24 h (compound incubation, following siRNA transfection)
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Result:Allowed NUP155 degradation to persist in GLE1-knockdown PANC-1 cells. Completely abolished GLE1 degradation in NUP155-knockdown PANC-1 cells.
Chemical Information
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No. CAS 3055558-98-7
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Appearance Solid
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Peso molecular 449.60
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Fòrmula C23H28FNO3S2
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Color White to off-white
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SMILES
CN(C(C1=CC=C(C2=C(SC)C=C(F)C=C2)C=C1S(=O)(C)=O)=O)CC3CCCCC3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 62.5 mg/mL (139.01 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)
Pureza y Documentación
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Ficha de datos (275 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Li X, et al. Chemically Induced Nuclear Pore Complex Protein Degradation via TRIM21. ACS Chem Biol. 2025 May 16;20(5):1020-1028. [Content Brief]
[2]. Cheng Y, et al. TRIM21-NUP98 Interface Accommodates Structurally Diverse Molecular Glue Degraders. ACS Chem Biol. 2025 Apr 18;20(4):953-959. [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. 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 | 2.2242 mL | 11.1210 mL | 22.2420 mL | 55.6050 mL |
| 5 mM | 0.4448 mL | 2.2242 mL | 4.4484 mL | 11.1210 mL | |
| 10 mM | 0.2224 mL | 1.1121 mL | 2.2242 mL | 5.5605 mL | |
| 15 mM | 0.1483 mL | 0.7414 mL | 1.4828 mL | 3.7070 mL | |
| 20 mM | 0.1112 mL | 0.5560 mL | 1.1121 mL | 2.7802 mL | |
| 25 mM | 0.0890 mL | 0.4448 mL | 0.8897 mL | 2.2242 mL | |
| 30 mM | 0.0741 mL | 0.3707 mL | 0.7414 mL | 1.8535 mL | |
| 40 mM | 0.0556 mL | 0.2780 mL | 0.5560 mL | 1.3901 mL | |
| 50 mM | 0.0445 mL | 0.2224 mL | 0.4448 mL | 1.1121 mL | |
| 60 mM | 0.0371 mL | 0.1853 mL | 0.3707 mL | 0.9267 mL | |
| 80 mM | 0.0278 mL | 0.1390 mL | 0.2780 mL | 0.6951 mL | |
| 100 mM | 0.0222 mL | 0.1112 mL | 0.2224 mL | 0.5560 mL |
HGC652 Related Classifications
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