JH-RE-06

Catalog No.S8850

For research use only.

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).

JH-RE-06 Chemical Structure

CAS No. 1361227-90-8

Purity & Quality Control

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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 (from reference)

Cell Research:

[1]

  • 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.

Animal Research:

[1]

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

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 468.72
Formula

C20H16Cl3N3O4

CAS No. 1361227-90-8
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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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.

Handling Instructions

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