EN 219

Pricing Availability   Qty
Description: Covalent RNF114 ligand
Chemical Name: 1-[3,5-bis(4-Bromophenyl)-4,5-dihydro-1H-pyrazol-1-yl]-2-chloroethanone
Purity: ≥98% (HPLC)
Literature (3)

Biological Activity for EN 219

EN 219 is a covalent RNF114 inhibitor (IC50 = 470 nM). In vitro EN 219 mimics the mechanism of action of Nimbolide (Cat. No. 7289) by binding to RNF114 and inhibiting ubiquitination of its endogenous substrate, the tumor suppressor p21.

Technical Data for EN 219

M. Wt 456.56
Formula C17H13Br2ClN2O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 380351-29-1
PubChem ID 3413196
Smiles ClCC(N1N=C(C2=CC=C(C=C2)Br)CC1C3=CC=C(C=C3)Br)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for EN 219

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 45.66 100
ethanol 9.13 20

Preparing Stock Solutions for EN 219

The following data is based on the product molecular weight 456.56. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.19 mL 10.95 mL 21.9 mL
5 mM 0.44 mL 2.19 mL 4.38 mL
10 mM 0.22 mL 1.1 mL 2.19 mL
50 mM 0.04 mL 0.22 mL 0.44 mL

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References for EN 219

References are publications that support the biological activity of the product.

Luo et al (2021) Chemoproteomics-enabled discovery of covalent RNF114-based degraders that mimic natural product function. Cell Chem.Biol. 28 559 PMID: 33513350

If you know of a relevant reference for EN 219, please let us know.

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Keywords: EN 219, EN 219 supplier, EN219, ligase, RNF114, e3, inhibitors, inhibits, ligands, targeted, protein, TPD, Degrader, Degraders, Ubiquitin, E3, Ligases, 7476, Tocris Bioscience

Citations for EN 219

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Literature in this Area

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