MilliporeSigma™ Calbiochem™ JHDM Inhibitor VIII, SD70

Description

A cell-permeable, bioavailable, non-toxic 8-hydroxyquinolinyl based compound that binds to and colocalizes with androgen receptor (AR) at both ligand-dependent and independent transcriptional regulatory elements

A cell-permeable, bioavailable, non-toxic 8-hydroxyquinolinyl based compound that binds to and colocalizes with androgen receptor (AR) at both ligand-dependent and independent transcriptional regulatory elements. Acts as an inhibitor of dihydotestosterone-regulated gene expression. Shown to inhibit prostate cancer cell transcription by blocking the activity of histone lysine demethylase KDM4C (IC₅₀ = 30μM). Increases total H3K9me2 levels in 293 T cells in enhancer and promoter regions and causes a slight diminution in the levels of methylated H3K36. Does not affect the activity of DNA/RNA polymerase or topoisomerase I and II activities in any significant manner. Blocks the proliferation of hormone-independent CWR22Rv1 cells in culture (∽ 5μM) and also inhibits their growth in a prostate cancer xenograft murine model (10mg/kg, i.p.daily).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Specifications

• Color: Off-white
• Description: 97% by HPLC
• Target Proteins: JMJD2C/KDM4C
• Molecular Formula: C₁₈H₁₈N₂O₃
• Solubility: DMSO
• Content And Storage: Protect from light
• Form: Powder
• Quantity: 25 mg