509703 LSD1 Inhibitor VII, SP-2509 - CAS 1423715-09-6 - Calbiochem

509703
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₉H₂₀ClN₃O₅S 1423715-09-6

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      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.09703.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable phenethylidene-benzohydrazide compound that acts as a potent, selective, reversible, and non-competitive inhibitor of Lysine-Specific Demethylase 1 (LSD1; IC50 = 13 nM; Ki = 31 nM). Exhibits excellent selectivity over monoamine oxidases A and B (IC50 > 300 µM), lactate dehydrogenase, glucose oxidase, hERG, CYP1A2, CYP2D6 (IC50 ≥ 10 µM), CYP2C9 (IC50 = 8.04 µM) and CYP2C19 (IC50 = 9.76 µM). Inhibits CYP3A4 only at >200-fold higher concentration. Reduces the proliferation of several cancer cell lines, including AN3 Ca, BT-20, MCF-7, T-47D, HT29, MIA PaCa-2 and SK-N-MC (IC50 = 356, 489, 637, 649, 429, 468 and 329 nM, respectively).
          Catalogue Number509703
          Brand Family Calbiochem®
          SynonymsBHC110 Inhibitor VII, Histone Lysine Demethylase Inhibitor XIV, KIAA1718 Inhibitor VII, LSD Inhibitor VII, SP-2509
          References
          ReferencesFiskus, W., et al. 2014. Leukemia 28, 2155.
          Sorna, V., et al. 2013. J. Med. Chem. 56, 9496.
          Product Information
          CAS number1423715-09-6
          FormOff-white solid
          Hill FormulaC₁₉H₂₀ClN₃O₅S
          Chemical formulaC₁₉H₂₀ClN₃O₅S
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetLSD1
          Purity≥98% 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

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Fiskus, W., et al. 2014. Leukemia 28, 2155.
          Sorna, V., et al. 2013. J. Med. Chem. 56, 9496.
          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.

          Revision28-February-2014 JSW
          SynonymsBHC110 Inhibitor VII, Histone Lysine Demethylase Inhibitor XIV, KIAA1718 Inhibitor VII, LSD Inhibitor VII, SP-2509
          DescriptionA cell-permeable, lysine-specific demethylase 1 (LSD1) active site-targeting phenethylidene-benzohydrazide that inhibits LSD1 activity (IC50 = 13 nM) in a reversible and substrate non-competitive (Ki = 34 nM) manner, while inhibiting CYP3A4 only at much higher concentrations (IC50 = 2.61 µM) and displaying little or no potency towards CYP1A2/2C9/2C19/2D6. MAO-A/B, D-lactate dehydrogenase, glucose oxidase, and hERG (IC50 ≥8.0 µM). Shown to enhance histone H3 Lys9 dimethylation (H3K9me2) in androgen-dependent prostate cancer VCaP cultures (1 to 10 µM) and effectively inhibits LSD1-dependent cancer growth (IC50 in nM = 329/SK-N-MC, 356/AN3 Ca, 429/HT29, 468/MIA PaCa-2, 489/BT-20, 612/HER218, 614/HCT 116, 637/MCF-7, 649/T-47D; 96 h).
          FormOff-white solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number1423715-09-6
          Chemical formulaC₁₉H₂₀ClN₃O₅S
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityDMSO (100 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
          ReferencesFiskus, W., et al. 2014. Leukemia 28, 2155.
          Sorna, V., et al. 2013. J. Med. Chem. 56, 9496.