1-[3,5-bis(4-bromophenyl)-3,4-dihydropyrazol-2-yl]-2-chloroethanone
![1-[3,5-bis(4-bromophenyl)-3,4-dihydropyrazol-2-yl]-2-chloroethanone Structure](CAS/20180720/GIF/380351-29-1.gif)
- CAS No.
- 380351-29-1
- Chemical Name:
- 1-[3,5-bis(4-bromophenyl)-3,4-dihydropyrazol-2-yl]-2-chloroethanone
- Synonyms
- EN219;3,5-bis(4-bromophenyl)-1-(chloroacetyl)-4,5-dihydro-1H-pyrazole;1-[3,5-bis(4-bromophenyl)-3,4-dihydropyrazol-2-yl]-2-chloroethanone;Ethanone, 1-[3,5-bis(4-bromophenyl)-4,5-dihydro-1H-pyrazol-1-yl]-2-chloro-
- CBNumber:
- CB34224922
- Molecular Formula:
- C17H13Br2ClN2O
- Molecular Weight:
- 456.56
- MDL Number:
- MFCD02989881
- MOL File:
- 380351-29-1.mol
| 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 |
1-[3,5-bis(4-bromophenyl)-3,4-dihydropyrazol-2-yl]-2-chloroethanone Chemical Properties,Uses,Production
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
Store at -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)
1-[3,5-bis(4-bromophenyl)-3,4-dihydropyrazol-2-yl]-2-chloroethanone Preparation Products And Raw materials
Raw materials
Preparation Products
1-[3,5-bis(4-bromophenyl)-3,4-dihydropyrazol-2-yl]-2-chloroethanone Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| Beijing Biocreative Technology Co., Ltd. | 15522676233 | 3007606172@qq.com | China | 1249 | 58 |
| Shanghai Easy CDMO Co.,Ltd | 021-61734564 | August@easycdmo.com | China | 10010 | 58 |
| Shanghai Yifei Biotechnology Co. , Ltd. | 021-65675885 18964387627 | customer_service@efebio.com | China | 8739 | 58 |
| Suzhou Meidi Senuo Pharmaceutical Technology Co., Ltd. | 13771642864 | snhuyu_2008@126.com | China | 1107 | 58 |
| Jilin Chinese Academy of Sciences-yanshen Technology | 18143011203 | ET-market@chemextension.com | China | 41844 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 28091 | 58 |