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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).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

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

Primary Target: LSD1
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
1423715-09-6C₁₉H₂₀ClN₃O₅S

Products

Catalog NumberPackaging Qty/Pack
5.09703.0001 Glass bottle 10 mg
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
Catalog Number GTIN
5.09703.0001 04055977241037

Documentation

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