2. PROTAC Immunology/Inflammation
  3. Molecular Glues IFNAR
  4. EN1033

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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EN1033

EN1033 Chemical Structure

CAS No. : 2193367-28-9

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

EN1033 Related Antibodies

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Description

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[1].

In Vitro

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.

EN1033 Related Antibodies

Western Blot Analysis[1]

Cell Line: THP1 cells
Concentration: 12.5, 25, 50, 75, 100 μM
Incubation Time: 24 h
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.

Western Blot Analysis[1]

Cell Line: THP1 cells
Concentration: 100 μM
Incubation Time: 0, 2, 4, 8, 20, 24 h
Result: Induced the degradation of IRF8 and IRF5 starting at 8 h, and this effect was gradually strengthened over time.

Western Blot Analysis[1]

Cell Line: HEK293T cells
Concentration: 50 μM
Incubation Time: 18, 24 h
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.
Molecular Weight

242.32

Formula

C15H18N2O
CAS No.
Appearance

Liquid (Density: 1.178±0.10 g/cm3)

Color

Colorless to light yellow

SMILES

C=CC(N1C2=CC=CC=C2CN3C(CCC3)C1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.1268 mL 20.6339 mL 41.2677 mL
5 mM 0.8254 mL 4.1268 mL 8.2535 mL
View the 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.

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Purity & Documentation

Purity: 99.96%

SDS (252 KB)

COA (254 KB) HNMR (264 KB) RP-HPLC (249 KB) LCMS (181 KB)

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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EN1033 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EN10332193367-28-9EN 1033EN-1033Molecular GluesIFNARInterferon-α/β receptorInterferon-alpha/beta receptorImmune regulatory transcription factor 5/8IRF5/8Pro-inflammatory transcriptionalAutoimmune and inflammatory diseasescytokineschemokinescovalentdegradersTHP1Inhibitorinhibitorinhibit

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