531662 JHDM Inhibitor VIII, SD70 - Calbiochem

531662
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₈H₁₈N₂O₃

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.31662.0001
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          Glass bottle 25 mg
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          Description
          OverviewA 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 = 30 µM). 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 (~ 5 µM) and also inhibits their growth in a prostate cancer xenograft murine model (10 mg/kg, i.p.daily).

          Please note that the molecular weight for this compound is batch-specific due to variable water content.
          Catalogue Number531662
          Brand Family Calbiochem®
          SynonymsN-(Furan-2-yl(8-hydroxyquinolin-7-yl)methyl)isobutyramide, N-(2-Furyl(8-hydroxy-7-quinolinyl)methyl)-2-methylpropanamide, Histone Lysine Demethylase Inhibitor XV, SD-70
          References
          ReferencesJin, C., et al. 2014. Proc. Natl. Acad. Sci. USA 111, 9235.
          Product Information
          FormOff-white powder
          Hill FormulaC₁₈H₁₈N₂O₃
          Chemical formulaC₁₈H₁₈N₂O₃
          ReversibleY
          Applications
          Biological Information
          Primary TargetJMJD2C/KDM4C
          Purity≥97% by HPLC
          Physicochemical Information
          Cell permeableY
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Ambient Temperature Only
          Toxicity Standard Handling
          Storage +2°C to +8°C
          Protect from Light Protect from light
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          JHDM Inhibitor VIII, SD70 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Jin, C., et al. 2014. Proc. Natl. Acad. Sci. USA 111, 9235.

          Brochure

          Title
          NPI Flyer- Epigenetics and Nuclear Function Feature (EMD)
          New Products - Antibodies, Small Molecule, Inhibitors

          Technical Info

          Title
          White Paper: Further considerations of antibody validation and usage. (EMD)
          Data Sheet

          Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

          Revision19-December-2014 JSW
          SynonymsN-(Furan-2-yl(8-hydroxyquinolin-7-yl)methyl)isobutyramide, N-(2-Furyl(8-hydroxy-7-quinolinyl)methyl)-2-methylpropanamide, Histone Lysine Demethylase Inhibitor XV, SD-70
          DescriptionA cell-permeable compound with a Fe(II)-chelating 8-hydroxyquinoline (8HQ) moiety is reported to inhibit KDM4C (IC50 = 30 µM against calf thymus histone H3K9me2 demethylation; [FeSO4] = 50 µM & [α-ketoglutarate] = 1 mM) and possibly other JMJD2/KDM4 members of Jumonji domain-containing histone demethylases (JHDM). Effectively suppresses androgen receptor (AR) target genes expression in human prostate adenocarcinoma LNCaP cultures upon 100 nM DHT stimulation as well as in CWR22Rv1 cells with constitutively active AR (10 µM) without affecting topoisomerase activity of E. coli Topo I or human Topo II. Shown to prevent AR/genotoxic stress-induced TMPRSS2 chromosomal translocation and gene fusions in LNCaP cells (1/100 & 1/13 of control TMPRSS2ETV1 and TMPRSS2ERG induction level, respectively; 10 µM SD70 dosed 2 h prior to 24 h 50 Gy irradiation & 100 nM DHT) and exhibit anti-proliferation activity against CWR22Rv1 both in cultures (97% decreased vs. 260% increased viable cell number on d6 by MTS assay with or without 10 µM SD70 ) in vitro and in mice (84% growth retardation on d10; 10 mg/4 mL/kg/d i.p.) in vivo without apparent animal toxicity. LNCaP genomic binding sites analyses utilizing Chem-seq with Biotin-derivatized SD70 as well as antibody-based ChIP reveal that 46% of genes upregulated by >1.5-fold upon DHT stimulation have both AR enhancer and SD70-binding sites within 500 kb of the coding gene promoter and 42% of all SD70-suppressed genes in DHT-treated LNCaP cells are DHT-induced genes. Likewise, increased KDM4C binding upon DHT treatment is observed on AR enhancers coocuppied by SD70.
          FormOff-white powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₈H₁₈N₂O₃
          Purity≥97% by HPLC
          SolubilityDMSO (50 mg/ml)
          Storage +2°C to +8°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesJin, C., et al. 2014. Proc. Natl. Acad. Sci. USA 111, 9235.