An RNF114 recruiter
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EN219

Item No. 33957

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[3,5-bis(4-bromophenyl)-4,5-dihydro-1H-pyrazol-1-yl]-2-chloro-ethanone
CAS Number
380351-29-1
Molecular Formula
C17H13Br2ClN2O
Formula Weight
456.6
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 5 mg/mlEthanol: 1 mg/ml
λmax
224, 295, 305 nm
SMILES
BrC(C=C1)=CC=C1C2N(C(CCl)=O)N=C(C3=CC=C(Br)C=C3)C2
InChi Code
InChI=1S/C17H13Br2ClN2O/c18-13-5-1-11(2-6-13)15-9-16(22(21-15)17(23)10-20)12-3-7-14(19)8-4-12/h1-8,16H,9-10H2
InChi Key
CXRHMHAKZPJNKS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $37

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    5 mg

    $168

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    10 mg

    $315

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    25 mg

    $653

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    Cayman Chemical
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    Product Description

    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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Luo, M., Spradlin, J.N., Boike, L., et al. Chemoproteomics-enabled discovery of covalent RNF114-based degraders that mimic natural product function. Cell Chem. Biol. 28(4), 559-566 (2021).