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489477 LSD1 Inhibitor II, S2101 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₆H₁₆ClF₂NO

Products

Catalog NumberPackaging Qty/Pack
489477-5MG Glass bottle 5 mg
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®
SynonymsLSD Inhibitor II, S2101, 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
Global Trade Item Number
Catalog Number GTIN
489477-5MG 04055977273373

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
SynonymsLSD Inhibitor II, S2101, 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.