JH-RE-06
Names
[ CAS No. ]:
1361227-90-8
[ Name ]:
JH-RE-06
Biological Activity
[Description]:
JH-RE-06, a potent REV1-REV7 interface inhibitor (IC50=0.78 μM; Kd=0.42 μM), targets REV1 that interacts with the REV7 subunit of POLζ. JH-RE-06 disrupts mutagenic translesion synthesis (TLS) by preventing recruitment of mutagenic POLζ. JH-RE-06 sensitizes mouse and human cell lines to Cisplatin, and suppresses tumor progression in mice and prolongs animal survival[1].
[Related Catalog]:
[Target]
IC50: 0.78 μM (REV1-REV7)[1] Kd: 0.42 μM (REV1-REV7)[1]
[In Vitro]
JH-RE-06 unexpectedly induces dimerization of the REV1 CTD at its REV7-binding surface and blocks the REV1-REV7 interaction[1].
[In Vivo]
JH-RE-06 inhibits mutagenic TLS and enhances cisplatin-induced toxicity in cultured human and mouse cell lines[1]. Co-administration of JH-RE-06 with cisplatin suppresses the growth of xenograft human melanomas in mice[1].
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C20H16Cl3N3O4
[ Molecular Weight ]:
468.72