PROTAC(H-PGDS)-7
Based on 1 Customer Validation
PROTAC (H-PGDS)-7 is a selective, linker-free H-PGDS PROTAC degrader with a DC50 of 17.3 pM. PROTAC (H-PGDS)-7 binds to CRBN and forms a ternary complex with H-PGDS, inducing the degradation of H-PGDS via the ubiquitin-proteasome system through polyubiquitination and proteasomal degradation processes. PROTAC (H-PGDS)-7 inhibits the upregulated expression of TNFα, IL-1β, TGFβ1 and CD11b in mice with cardiac hypertrophy models. PROTAC (H-PGDS)-7 can be used in studies related to Duchenne muscular dystrophy and allergic diseases.
(Pink: H-PGDS ligand (HY-110167); Blue: Cereblon ligand (HY-41547); Black: linker).
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- Pureté: 99.42%
- CAS No.: 2761281-50-7
- Formule: C40H38N8O7
- Masse moléculaire:742.78
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Stockage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
Cereblon |
IL-1β |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KU812 cell line | DC50 |
26.3 pM
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Half-maximal degradation of H-PGDS protein in human chronic myelogenous leukemia KU812 cells after 6 h incubation, measured via Western blot relative to β-actin.
Half-maximal degradation of H-PGDS protein in human chronic myelogenous leukemia KU812 cells after 6 h incubation, measured via Western blot relative to β-actin.
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34652145 |
| KU812 cell line | DC50 |
17.3 pM
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Half-maximal degradation of H-PGDS protein in human chronic myelogenous leukemia KU812 cells after 24 h incubation, measured via Western blot relative to β-actin.
Half-maximal degradation of H-PGDS protein in human chronic myelogenous leukemia KU812 cells after 24 h incubation, measured via Western blot relative to β-actin.
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34652145 |
| KU812 cell line | DC50 |
0.094 nM
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Half-maximal degradation of H-PGDS protein in human chronic myelogenous leukemia KU812 cells assessed via western blot after 24 h incubation.
Half-maximal degradation of H-PGDS protein in human chronic myelogenous leukemia KU812 cells assessed via western blot after 24 h incubation.
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40937104 |
| KU812 cell line | DC50 |
18.7 pM
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Degradation of H-PGDS protein in human chronic myelogenous leukemia KU812 cells assessed via western blotting after 24 h incubation.
Degradation of H-PGDS protein in human chronic myelogenous leukemia KU812 cells assessed via western blotting after 24 h incubation.
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36561070 |
In Vitro
PROTAC(H-PGDS)-7 (0-10000 pM; 6-24 h) potently and selectively degrades H-PGDS protein in KU812 cells via the ubiquitin-proteasome system, with a DC50 of 17.3 pM after 24 h incubation[1].
PROTAC(H-PGDS)-7 (30-3000 pM; 6 h) potently suppresses PGD2 production in KU812 cells, with greater efficacy than non-degrading H-PGDS inhibitors[1].
PROTAC(H-PGDS)-7 (24 h) induces concentration-dependent degradation of H-PGDS in KU812 cells with a DC50 of 0.094 nM after 24 h incubation[2].
PROTAC(H-PGDS)-7 (5-200 pM; 24 h) potently degrades H-PGDS in KU812 cells with a DC50 of 18.7 pM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human chronic myelogenous leukemia KU812 cells
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Concentration:0-10000 pM (24 h incubation: 0,10,30,100 pM; 6 h incubation: 0,10,100,1000,10000 pM)
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Incubation Time:6 h, 24 h
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Result:Showed potent dose-dependent reduction of H-PGDS protein levels in KU812 cells.
Achieved a half-maximal degradation concentration (DC50) of 26.3 pM after 6 h of incubation and 17.3 pM after 24 h of incubation.
Reduced H-PGDS protein levels to ~30.8% of vehicle control levels at 100 pM with 6 h treatment.
Reduced H-PGDS protein levels to ~12.9% of vehicle control levels at 10 nM with 6 h treatment.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:mdx mice (male, 9-12 weeks old, dystrophin-deficient, cardiac hypertrophy induced by subcutaneous injection of 2 mg/kg/day T3 for 14 days)[1]
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Dosage:45 mg/kg
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Administration:s.c.; daily; 14 days
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Result:Suppressed the T3-induced upregulation of cardiac mRNA levels of TNFα, IL-1β, TGFβ1, and CD11b.
Chemical Information
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CAS No. 2761281-50-7
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Appearance Solid
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Masse moléculaire 742.78
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Formule C40H38N8O7
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Color Light yellow to yellow
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SMILES
O=C(C1CCN(C2=CC=C(NC(C3=CN=C(OC4=CC=CC=C4)N=C3)=O)C=C2)CC1)N5CCN(C6=C(C(N(C7CCC(NC7=O)=O)C8=O)=O)C8=CC=C6)CC5
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (134.63 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 (sealed storage, away from moisture and 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 (sealed storage, away from moisture and 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)
Pureté et documentation
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Fiche technique (279 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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Instruction de manipulation (2659 KB)
Références
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 and 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 | 1.3463 mL | 6.7315 mL | 13.4629 mL | 33.6573 mL |
| 5 mM | 0.2693 mL | 1.3463 mL | 2.6926 mL | 6.7315 mL | |
| 10 mM | 0.1346 mL | 0.6731 mL | 1.3463 mL | 3.3657 mL | |
| 15 mM | 0.0898 mL | 0.4488 mL | 0.8975 mL | 2.2438 mL | |
| 20 mM | 0.0673 mL | 0.3366 mL | 0.6731 mL | 1.6829 mL | |
| 25 mM | 0.0539 mL | 0.2693 mL | 0.5385 mL | 1.3463 mL | |
| 30 mM | 0.0449 mL | 0.2244 mL | 0.4488 mL | 1.1219 mL | |
| 40 mM | 0.0337 mL | 0.1683 mL | 0.3366 mL | 0.8414 mL | |
| 50 mM | 0.0269 mL | 0.1346 mL | 0.2693 mL | 0.6731 mL | |
| 60 mM | 0.0224 mL | 0.1122 mL | 0.2244 mL | 0.5610 mL | |
| 80 mM | 0.0168 mL | 0.0841 mL | 0.1683 mL | 0.4207 mL | |
| 100 mM | 0.0135 mL | 0.0673 mL | 0.1346 mL | 0.3366 mL |
PROTAC(H-PGDS)-7 Related Classifications
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