JH-RE-06

CAS No. 1361227-90-8

JH-RE-06( —— )

Catalog No. M22367 CAS No. 1361227-90-8

JH-RE-06 disrupts mutagenic translesion synthesis (TLS) by preventing the recruitment of mutagenic POLζ. JH-RE-06 is an effective REV1-REV7 interface inhibitor (IC50=0.78 μM; Kd=0.42 μM), which targets REV1 that interacts with the REV7 subunit of POLζ. JH-RE-06 also improves chemotherapy.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    JH-RE-06
  • Note
    Research use only, not for human use.
  • Brief Description
    JH-RE-06 disrupts mutagenic translesion synthesis (TLS) by preventing the recruitment of mutagenic POLζ. JH-RE-06 is an effective REV1-REV7 interface inhibitor (IC50=0.78 μM; Kd=0.42 μM), which targets REV1 that interacts with the REV7 subunit of POLζ. JH-RE-06 also improves chemotherapy.
  • Description
    JH-RE-06 disrupts mutagenic translesion synthesis (TLS) by preventing the recruitment of mutagenic POLζ. JH-RE-06 is an effective REV1-REV7 interface inhibitor (IC50=0.78 μM; Kd=0.42 μM), which targets REV1 that interacts with the REV7 subunit of POLζ. JH-RE-06 also improves chemotherapy. JH-RE-06 unexpectedly causes dimerization of the REV1 CTD at its REV7-binding surface. It also blocks the REV1-REV7 interaction. In mice, co-administration of JH-RE-06 with cisplatin inhibits the growth of xenograft human melanomas. JH-RE-06 suppresses mutagenic TLS and increases cisplatin-induced toxicity in cultured human and mouse cell lines.
  • In Vitro
    JH-RE-06 unexpectedly induces dimerization of the REV1 CTD at its REV7-binding surface and blocks the REV1-REV7 interaction.
  • In Vivo
    JH-RE-06 inhibits mutagenic TLS and enhances cisplatin-induced toxicity in cultured human and mouse cell lines. Co-administration of JH-RE-06 with cisplatin suppresses the growth of xenograft human melanomas in mice.
  • Synonyms
    ——
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    DNA/RNA Synthesis
  • Recptor
    REV1-REV7
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1361227-90-8
  • Formula Weight
    468.72
  • Molecular Formula
    C20H16Cl3N3O4
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:5 mg/mL (10.67 mM; Need ultrasonic)
  • SMILES
    O=C1C(C(CC(C)C)=O)=C(NC2=CC=C(Cl)C=C2Cl)NC3=C1C([N+]([O-])=O)=CC=C3Cl
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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