| Identification | Back Directory | [Name]
1-[3,5-bis(4-bromophenyl)-3,4-dihydropyrazol-2-yl]-2-chloroethanone | [CAS]
380351-29-1 | [Synonyms]
EN219
1-[3,5-bis(4-bromophenyl)-3,4-dihydropyrazol-2-yl]-2-chloroethanone | [Molecular Formula]
C17H13Br2ClN2O | [MDL Number]
MFCD02989881 | [MOL File]
380351-29-1.mol | [Molecular Weight]
456.56 |
| Chemical Properties | Back Directory | [Boiling point ]
510.5±60.0 °C(Predicted) | [density ]
1.70±0.1 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
DMF: 10 mg/ml,DMSO: 5 mg/ml,Ethanol: 1 mg/ml | [form ]
A crystalline solid | [pka]
-2.09±0.70(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Biological Activity]
EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114.1 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. | [storage]
-20°C | [References]
1.Luo, M., Spradlin, J.N., Boike, L., et al.Chemoproteomics-enabled discovery of covalent RNF114-based degraders that mimic natural product functionCell Chem. Biol.28(4)559-566(2021)
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PHARMEKS Ltd.
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+7 (495) 702-9648 |
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www.pharmeks.com |
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