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

A cell-permeable, potent, selective, reversible inhibitor of Lysine-Specific Demethylase 1 (LSD1; IC₅₀ = 13 nM; Ki = 31 nM).

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Synonyme: BHC110 Inhibitor VII, Histone Lysine Demethylase Inhibitor XIV, KIAA1718 Inhibitor VII, LSD Inhibitor VII, SP-2509

Primary Target: LSD1
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509703
Preis & Verfügbarkeit

Übersicht

Replacement Information

Key Spec Table

CAS #Empirical Formula
1423715-09-6C₁₉H₂₀ClN₃O₅S

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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
      Quality LevelMQ100
      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
      Global Trade Item Number
      Bestellnummer GTIN
      5097030001 04055977241037

      Documentation

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

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

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

      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 Protect from light
      +2°C to +8°C
      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.