203630
Bmi1-Ring1A E3 Ligase Inhibitor, PRT4165
Synonym(s):
PRT4165, 2-(3-Pyridinylmethylene)-1H-indene-1,3(2H)-dione; 2-(3-Pyridylmethylene)-1,3-indandione, NSC 600157
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About This Item
Empirical Formula (Hill Notation):
C15H9NO2
CAS Number:
Molecular Weight:
235.24
MDL number:
InChI key
OMHZFEWYVFWVLI-UHFFFAOYSA-N
InChI
1S/C15H9NO2/c17-14-11-5-1-2-6-12(11)15(18)13(14)8-10-4-3-7-16-9-10/h1-9H
SMILES string
O=C1C(C(C2=C1C=CC=C2)=O)=CC3=CN=CC=C3
Biochem/physiol Actions
PRT4165 is a potent inhibitor of PRC1 (polycomb-repressive complex 1)-mediated histone H2A ubiquitylation in vivo and in vitro. PRT4165 inhibits the in vitro histone H2A E3 ubiquitin ligase activity of PRC1 components RING1, RNF2, and a BMI1/RNF2 complex. PRT4165 also inhibits DNA double-strand breaks induced ubiquitylation of histone H2AX.
PRT4165 is a potent inhibitor of PRC1 (polycomb-repressive complex 1)-mediated histone H2A ubiquitylation in vivo and in vitro.
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