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Merck

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:
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SMILES string

O=C1C(C(C2=C1C=CC=C2)=O)=CC3=CN=CC=C3

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

InChI key

OMHZFEWYVFWVLI-UHFFFAOYSA-N

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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