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EN219
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Catalog No. T36800Cas No. 380351-29-1
Alias EN 219
EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114 and binds specifically to cysteine 8 (C8) within its intrinsically disordered region, exhibiting an IC50 of 470 nM. EN219 inhibits RNF114-induced autoubiquitination and p21 ubiquitination in cell-free assays at 50 μM. At 1 μM, EN219 interacts with multiple proteins including the tubulin β1 chain (TUBB1), heat shock protein 60 (Hsp60/HspD1), and histone H3.1 (HIST1H3A) in 231MFP breast cancer cells. Furthermore, EN219 has been linked to the bromodomain inhibitor (+)-JQ1 for the creation of a PROTAC capable of degrading BRD4 in 231MFP cells.
EN219
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Purity: 99.46%
Catalog No. T36800Alias EN 219Cas No. 380351-29-1
EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114 and binds specifically to cysteine 8 (C8) within its intrinsically disordered region, exhibiting an IC50 of 470 nM. EN219 inhibits RNF114-induced autoubiquitination and p21 ubiquitination in cell-free assays at 50 μM. At 1 μM, EN219 interacts with multiple proteins including the tubulin β1 chain (TUBB1), heat shock protein 60 (Hsp60/HspD1), and histone H3.1 (HIST1H3A) in 231MFP breast cancer cells. Furthermore, EN219 has been linked to the bromodomain inhibitor (+)-JQ1 for the creation of a PROTAC capable of degrading BRD4 in 231MFP cells.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $49 | - | In Stock | |
| 5 mg | Preferential | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $299 | - | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.46%
Appearance:Solid
Color:White to Red
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114 and binds specifically to cysteine 8 (C8) within its intrinsically disordered region, exhibiting an IC50 of 470 nM. EN219 inhibits RNF114-induced autoubiquitination and p21 ubiquitination in cell-free assays at 50 μM. At 1 μM, EN219 interacts with multiple proteins including the tubulin β1 chain (TUBB1), heat shock protein 60 (Hsp60/HspD1), and histone H3.1 (HIST1H3A) in 231MFP breast cancer cells. Furthermore, EN219 has been linked to the bromodomain inhibitor (+)-JQ1 for the creation of a PROTAC capable of degrading BRD4 in 231MFP cells. |
| Targets&IC50 | RNF114:470 nM |
| In vitro | Isotope tandem orthogonal proteolysis ABPP (isoTOP-ABPP) analysis demonstrated that EN219 (1 μM, 90 minutes) interacts with RNF114 C8, TUBB1 C201, HSPD1 C442, and HIST1H3A C97. [1] |
| Synonyms | EN 219 |
| Molecular Weight | 456.56 |
| Formula | C17H13Br2ClN2O |
| Cas No. | 380351-29-1 |
| Smiles | O=C(N1N=C(C=2C=CC(Br)=CC2)CC1C3=CC=C(Br)C=C3)CCl |
| Storage | keep away from moisture,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||||||||||||
| Solubility Information | DMF: 10 mg/mL (21.9 mM), Sonication is recommended. Ethanol: 1 mg/mL (2.19 mM), Sonication is recommended. DMSO: 50 mg/mL (109.51 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||||||||||||
Ethanol/DMF/DMSO
DMF/DMSO
DMSO
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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