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Cell Signaling Kits & MAPmates™
Choose fixed kits that allow you to explore entire pathways or processes. Or design your own kits by choosing single plex MAPmates™, following the provided guidelines.
The following MAPmates™ should not be plexed together:
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48-602MAG
Buffer Detection Kit for Magnetic Beads
1 Kit
Space Saver Option Customers purchasing multiple kits may choose to save storage space by eliminating the kit packaging and receiving their multiplex assay components in plastic bags for more compact storage.
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509703
Sigma-AldrichLSD1 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).
More>>A cell-permeable, potent, selective, reversible inhibitor of Lysine-Specific Demethylase 1 (LSD1; IC₅₀ = 13 nM; Ki = 31 nM). Less<<
MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
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Description
Overview
A 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).
Fiskus, W., et al. 2014. Leukemia28, 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.
A 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).
Form
Off-white solid
Intert gas (Yes/No)
Packaged under inert gas
CAS number
1423715-09-6
Chemical formula
C₁₉H₂₀ClN₃O₅S
Structure formula
Purity
≥98% by HPLC
Solubility
DMSO (100 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity
Standard Handling
References
Fiskus, W., et al. 2014. Leukemia28, 2155. Sorna, V., et al. 2013. J. Med. Chem.56, 9496.
