EN219
Product Specifications
CAS Number
380351-29-1
Target
E1/E2/E3 Enzyme, Others
Related Pathways
Others, Ubiquitination
Bioactivity
EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114 and binds specifically to cysteine 8 (C8) within its intrinsically disordered region, exhibiting an IC50 of 470 nM. EN219 inhibits RNF114-induced autoubiquitination and p21 ubiquitination in cell-free assays at 50 μM. At 1 μM, EN219 interacts with multiple proteins including the tubulin β1 chain (TUBB1), heat shock protein 60 (Hsp60/HspD1), and histone H3.1 (HIST1H3A) in 231MFP breast cancer cells. Furthermore, EN219 has been linked to the bromodomain inhibitor (+) -JQ1 for the creation of a PROTAC capable of degrading BRD4 in 231MFP cells.
Smiles
O=C(N1N=C(C=2C=CC(Br)=CC2)CC1C3=CC=C(Br)C=C3)CCl
Molecular Formula
C17H13Br2ClN2O
Molecular Weight
456.56
Shipping Conditions
Ice Packs
Storage Temperature
-20°C
Available Sizes
Frequently Asked Questions
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