1361227-90-8

1361227-90-8 structure
1361227-90-8 structure
  • Name: JH-RE-06
  • Chemical Name: JH-RE-06
  • CAS Number: 1361227-90-8
  • Molecular Formula: C20H16Cl3N3O4
  • Molecular Weight: 468.72
  • Catalog: Signaling Pathways Cell Cycle/DNA Damage DNA/RNA Synthesis
  • Create Date: 2019-08-03 18:26:59
  • Modify Date: 2024-01-11 16:30:49
  • 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].

Name JH-RE-06
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

[1]. Wojtaszek JL, et al. A Small Molecule Targeting Mutagenic Translesion Synthesis Improves Chemotherapy. Cell. 2019 Jun 27;178(1):152-159.e11.

Molecular Formula C20H16Cl3N3O4
Molecular Weight 468.72
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