EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114. It binds to cysteine 8 (C8) in the intrinsically disordered region of RNF114 (RNF114-C8; IC50 = 470 nM) and inhibits RNF114-induced autoubiquitination and p21 ubiquitination in a cell-free assay when used at a concentration of 50 µM. EN219 (1 µM) also interacts with cysteine residues in the tubulin β1 chain (TUBB1), heat shock protein 60 (Hsp60), also known as Hsp family D member 1 (HspD1), and histone H3.1 (HIST1H3A) in 231MFP human breast cancer cells in a proteomic profiling assay. It has been linked to the bromodomain and extra terminal domain (BET) inhibitor ligand (+)-JQ1 for use as a proteolysis-targeting chimera (PROTAC) to degrade bromodomain-containing protein 4 (BRD4) in 231MFP cells.
MedKoo Cat#: 464832
Name: EN219
CAS#: 380351-29-1
Chemical Formula: C17H13Br2ClN2O
Exact Mass: 453.9083
Molecular Weight: 456.56
Elemental Analysis: C, 44.72; H, 2.87; Br, 35.00; Cl, 7.76; N, 6.14; O, 3.50
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMF | 10.0 | 21.90 | |
| DMSO | 5.0 | 10.95 | |
| Ethanol | 1.0 | 2.19 |
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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
