EN1033
Based on 1 Customer Validation
EN1033 is a covalent immune regulatory transcription factor 5/8 (IRF5/8) molecular glue degrader. EN1033 degrades IRF5 in a proteasome-dependent manner. EN1033 engages and degrades IRF8 more robustly and rapidly. EN1033 covalently targets C28 and C223 to destabilize and degrade IRF5 and IRF8 respectively, thereby inhibiting their pro-inflammatory transcriptional activity. EN1033 serves as a promising tool for the study of autoimmune and inflammatory disorders.
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- Purity: 99.96%
- CAS No.: 2193367-28-9
- 화학식: C15H18N2O
- 분자량:242.32
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보관:
-20°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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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
EN1033 (6.25-100 μM) does not exhibit cytotoxicity in THP1 macrophage leukemia cancer cells, nor does it induce stress granules formation[1].
EN1033 (1-µM, 24 h) induces on-pathway inhibition of IRF5 transcriptional activity[1].
EN1033 (100 μM, 18 h) degrades IRF8 in THP1 cells, which is proteasome-dependent[1].
EN1033 (12.5-100 μM, 2-24 h) degrades both IRF8 and IRF5, in a dose-responsive and time-dependent manner[1].
EN1033 (100 μM, 6 h) engages IRF8 more robustly than IRF5, while EN1033 and its analog TH3-189 exert only moderate effects across the proteome[1].
EN1033 (50 μM, 18-24 h) causes the degradation of IRF5 and IRF8 by targeting C28 and C223, respectively[1].
EN1033 (12.5-100 μM, 24 h) degrades IRF8 in IRF5 Knockout cells, suggesting IRF5 does not regulate IRF8. In contrast, IRF8 knockdown markedly reduces IRF5 levels, indicating IRF8 regulates IRF5 in THP1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP1 cells
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Concentration:12.5, 25, 50, 75, 100 μM
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Incubation Time:24 h
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Result:Decreased the levels of IRF8 and IRF5 gradually as the concentration increased.
Triggered the most prominent degradation of IRF8 and IRF5 at a concentration of 100 μM.
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Cell Line:THP1 cells
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Concentration:100 μM
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Incubation Time:0, 2, 4, 8, 20, 24 h
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Result:Induced the degradation of IRF8 and IRF5 starting at 8 h, and this effect was gradually strengthened over time.
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Cell Line:HEK293T cells
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Concentration:50 μM
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Incubation Time:18, 24 h
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Result:Induced IRF5 degradation, which was fully rescued in C28S and C28S/C121S variants, but not in the C121S mutant.
Triggered IRF8 loss, which was fully rescued in C223S and C223S/C385S IRF8 mutants, but not in the C385S mutant-expressing cells.
Chemical Information
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CAS No. 2193367-28-9
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Appearance Solid-Liquid Mixture
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분자량 242.32
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화학식 C15H18N2O
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Color Light yellow to yellow
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SMILES
C=CC(N1C2=CC=CC=C2CN3C(CCC3)C1)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
용액&용해도
DMSO : 100 mg/mL (412.68 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 (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)
순도&문서
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Data Sheet (277 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)
- 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 (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 | 4.1268 mL | 20.6339 mL | 41.2677 mL | 103.1694 mL |
| 5 mM | 0.8254 mL | 4.1268 mL | 8.2535 mL | 20.6339 mL | |
| 10 mM | 0.4127 mL | 2.0634 mL | 4.1268 mL | 10.3169 mL | |
| 15 mM | 0.2751 mL | 1.3756 mL | 2.7512 mL | 6.8780 mL | |
| 20 mM | 0.2063 mL | 1.0317 mL | 2.0634 mL | 5.1585 mL | |
| 25 mM | 0.1651 mL | 0.8254 mL | 1.6507 mL | 4.1268 mL | |
| 30 mM | 0.1376 mL | 0.6878 mL | 1.3756 mL | 3.4390 mL | |
| 40 mM | 0.1032 mL | 0.5158 mL | 1.0317 mL | 2.5792 mL | |
| 50 mM | 0.0825 mL | 0.4127 mL | 0.8254 mL | 2.0634 mL | |
| 60 mM | 0.0688 mL | 0.3439 mL | 0.6878 mL | 1.7195 mL | |
| 80 mM | 0.0516 mL | 0.2579 mL | 0.5158 mL | 1.2896 mL | |
| 100 mM | 0.0413 mL | 0.2063 mL | 0.4127 mL | 1.0317 mL |
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