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EN219

Name: EN219
Brand: TargetMol
SKU: T36800
Rating: 4.5 (1 reviews)

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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

🥰Excellent

Catalog No. T36800Alias EN 219Cas No. 380351-29-1

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Product Introduction

Bioactivity

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

Chemical Properties

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
Color	White
Appearance	Solid

Storage & Solubility Information

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

	1mg	5mg	10mg	50mg
1 mM	2.1903 mL	10.9515 mL	21.9029 mL	109.5146 mL

DMF/DMSO

	1mg	5mg	10mg	50mg
5 mM	0.4381 mL	2.1903 mL	4.3806 mL	21.9029 mL
10 mM	0.2190 mL	1.0951 mL	2.1903 mL	10.9515 mL
20 mM	0.1095 mL	0.5476 mL	1.0951 mL	5.4757 mL

DMSO

	1mg	5mg	10mg	50mg
50 mM	0.0438 mL	0.2190 mL	0.4381 mL	2.1903 mL
100 mM	0.0219 mL	0.1095 mL	0.2190 mL	1.0951 mL

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DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

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