JH-RE-06

For research use only.

Catalog No.S8850

JH-RE-06 Chemical Structure

CAS No. 1361227-90-8

JH-RE-06 is a potent REV1-REV7 interface inhibitor with an IC50 of 0.78 μM and Kd value of 0.42 μM, disrupting REV1-POL ζ-mediated mutagenic translesion synthesis (TLS).

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Biological Activity

Description JH-RE-06 is a potent REV1-REV7 interface inhibitor with an IC50 of 0.78 μM and Kd value of 0.42 μM, disrupting REV1-POL ζ-mediated mutagenic translesion synthesis (TLS).
Targets
REV1-REV7 [1]
(Cell-free assay)
REV1-REV7 [1]
(Cell-free assay)
0.42 μM(Kd) 0.78 μM
In vitro

JH-RE-06 disrupts mutagenic TLS by preventing recruitment of mutagenic POL ζ. Remarkably, JH-RE-06 targets a nearly featureless surface of REV1 that interacts with the REV7 subunit of POL ζ. Binding of JH-RE-06 induces REV1 dimerization, which blocks the REV1-REV7 interaction and POL ζ recruitment. JH-RE-06 inhibits mutagenic TLS and enhances cisplatin-induced-toxicity in cultured human and mouse cell lines.[1]

In vivo

JH-RE-06 improves tumor cell response to cisplatin in vivo. Co-administration of JH-RE-06 with cisplatin suppresses the growth of xenograft human melanomas in mice, establishing a framework for developing TLS inhibitors as a novel class of chemotherapy adjuvants.[1]

Protocol

Cell Research:

[1]

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  • Cell lines: HT1080 cells, A375 cells, KP cells, MEF, LNCap cells, AG01522 cells.
  • Concentrations: 1.5 μM
  • Incubation Time: 24 h
  • Method:

    Clonogenic survival assay—300 cells are plated in triplicate in 6-well plates for 24 hours. Cisplatin is added to relevant wells for 24 hours. All plates are incubated at 37℃ for 24 hours. Media are changed the next day and in fresh media JH-RE-06 (at 1.5 μM concentration) is added to untreated or cisplatin-treated cells for another 24 hours. Media are changed at the end of these combination treatments, and cells are allowed to recover for 7 days. To stain the resulting colonies, media are aspirated and the fixative (50% methanol and 10% glacial acetic acid) is added for 10 minutes, followed by the addition of 0.02% Coomassie brilliant blue R-250 stain in methanol: acetic acid: water in a ratio of 46.5:7:46.5 (v/v/v). Colonies that stained blue and contained at least 40 cells are counted. Relative cell survival or colony formation is calculated by dividing colony counts from treated samples by the DMSO or untreated controls.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: 6–8-week-old NCRNU-F (nude) female mice
  • Dosages: 1.6 mg/kg
  • Administration: intra tumor injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 12 mg/mL (25.6 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 468.72
Formula

C20H16Cl3N3O4

CAS No. 1361227-90-8
Storage powder
in solvent
Synonyms N/A
Smiles CC(C)CC(=O)C1=C(NC2=C(C=CC(=C2C1=O)[N+](=O)[O-])Cl)NC3=C(C=C(C=C3)Cl)Cl

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID