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489477 LSD1 Inhibitor II, S2101 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₆H₁₆ClF₂NO

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489477-5MG
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      Description
      OverviewA cell-permeable, 2-PCPA derivative that elicits mechanism-based inhibition against LSD1 (IC50 = 0.99 µM, KI = 0.61 µM, and kinact/KI = 4560 M-1S-1), and displays much lower inhibition activity toward MAO-B (KI = 17 µM, kinact/KI = 18 M-1S-1) and MAO-A (KI = 110 µM, kinact/KI = 60 M-1S-1), with higher potency and selectivity compared with those of 2-PCPA (Cat. No. 616431) (IC50 = 184 µM, KI = 100 µM, kinact/KI = 58 M-1S-1 for LSD1, and K I = 26 µM, kinact/KI = 271 M-1S-1 for MAO-B, and K I = 5 µM,
      kinact/KI = 1050 M-1S-1 for MAO-A). The inhibition of LSD1 is further confirmed in a cell-based assay, the treatment of HEK293T human cells with S2101 results in a dose-dependent increase in the level of H3K4me2, and about 50-fold stronger inhibition compared with that of 2-PCPA.
      Catalogue Number489477
      Brand Family Calbiochem®
      SynonymsS2101, LSD Inhibitor II, BHC110 Inhibitor II, Histone Lysine Demethylase Inhibitor IV, KDM1 Inhibitor II, MOA Inhibitor II
      References
      ReferencesMimasu, S., et al. 2010. Biochemistry 49, 6494.
      Product Information
      FormWhite solid
      Hill FormulaC₁₆H₁₆ClF₂NO
      Chemical formulaC₁₆H₁₆ClF₂NO
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      ApplicationLSD1 Inhibitor II, S2101, is a cell-permeable, 2-PCPA derived mechanism-based inhibitor of LSD1 (IC50 = 0.99 µM, KI = 0.61 µM, and kinact/KI = 4560 M-1S-1).
      Biological Information
      Purity≥95% by HPLC
      Physicochemical Information
      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
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      LSD1 Inhibitor II, S2101 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      LSD1 Inhibitor II, S2101 - Calbiochem Certificates of Analysis

      TitleLot Number
      489477

      References

      Reference overview
      Mimasu, S., et al. 2010. Biochemistry 49, 6494.
      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.

      Revision23-February-2011 RFH
      SynonymsS2101, LSD Inhibitor II, BHC110 Inhibitor II, Histone Lysine Demethylase Inhibitor IV, KDM1 Inhibitor II, MOA Inhibitor II
      DescriptionA cell-permeable, 2-PCPA derivative that elicits mechanism based inhibition of LSD1 (IC50 = 0.99 µM, KI = 0.61 µM, and kinact/KI = 4560 (M-1S-1)), and displays much lower inhibition activity toward MAO-B (KI = 17 µM, kinact/KI = 18 (M-1S-1)) and MAO-A inhibition (KI = 110 µM, kinact/KI = 60 (M-1S-1)), with higher potency and selectivity compared with 2-PCPA, IC50 = 184 µM, KI = 100 µM, kinact/KI = 58 (M-1S-1)) for LSD1, and K I = 26 µM, kinact/KI = 271 (M-1S-1)) for MAO-B, and K I = 5 µM, kinact/KI = 1050 (M-1S-1)) for MAO-A). The inhibition of LSD1 is further confirmed in a cell based assay, the treatment of HEK293T human cells with S2101 results in a dose-dependent increase in the level of H3K4me2, and about 50-fold stronger inhibition compared with that of 2-PCPA.
      FormWhite solid
      Chemical formulaC₁₆H₁₆ClF₂NO
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (100 mg/ml) or H₂O (25 mg/ml)
      Storage +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 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesMimasu, S., et al. 2010. Biochemistry 49, 6494.