EN219 - CAS 380351-29-1

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.

E1/E2/E3 Enzyme, Others

Others, Ubiquitination

380321

C17H13Br2ClN2O

456.56

O=C(N1N=C(C=2C=CC(Br)=CC2)CC1C3=CC=C(Br)C=C3)CCl

-20°C

Ice Packs

Small Compound