Name: SP2509
Price: 268.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    SP2509 is a novel Lysine specific demethylase 1 (LSD1) antagonist (IC50 = 13nM) with no effect on MAO-A and MAO-B. [1]LSD1 demethylates mono-/di-methylated lysine 4 on histone H3. High expression of LSD1 is associated with poor prognosis in cancer. [2] In cultured human AML cells, SP2590 inhibited LSD1 activity, deplete colony growth and elicit apoptosis. SP2590 also inhibited the LSD1 binding to CoREST, increase promoter-specific H3K4Me3 and induces p53, p21 and C/EBPα in AML cells. Moreover, SP2590 promotes differentiated of cultured and primary AML cell. [1] In mice carrying AML xenografts, SP2590 treatment alone significantly improved the survival of mice and co-treatment with an-HDAC inhibitor (HDI) panobinostat (PS) exhibited superior in vivo activity. [1]
    
    1. Fiskus W, Sharma S, Shah B, Portier BP, Devaraj SG, Liu K, Iyer SP, Bearss D, Bhalla KN. Highly effective combination of LSD1 (KDM1A) antagonist andpan-histone deacetylase inhibitor against human AML cells. Leukemia. 2014 Nov;28(11):2155-64.
    2. Zhao ZK, Yu HF, Wang DR, Dong P, Chen L, Wu WG, Ding WJ, Liu YB.Overexpression of lysine specific demethylase 1 predicts worse prognosis in primary hepatocellular carcinoma patients. World J Gastroenterol. 2012 Dec 7;18(45):6651-6.
- Properties
  - Categories
    
    Demethylase 1 (LSD1) antagonist, novel Lysine-specific
    
    Alternative Name
    
    (E)-N'-(1-(5-chloro-2-hydroxyphenyl)ethylidene)-3-(morpholinosulfonyl)benzohydrazide
    
    CAS Number
    
    1423715-09-6
    
    Molecular Formula
    
    C19H20ClN3O5S
    
    Molecular Weight
    
    437.90
    
    Appearance
    
    A solid
    
    Purity
    
    99.59%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥19.45 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    OC1=CC=C(Cl)C=C1/C(C)=N/NC(C2=CC=CC(S(=O)(N3CCOCC3)=O)=C2)=O
    
    * For Research Use Only
- Reference
  - 1. Amjad Ali, Jasmin Shafarin, et al. "Co-targeting BET bromodomain BRD4 and RAC1 suppresses growth, stemness and tumorigenesis by disrupting the c-MYC-G9a-FTH1axis and downregulating HDAC1 in molecular subtypes of breast cancer." Int J Biol Sci. 2021 Oct 25;17(15):4474-4492. PMID:34803511

Documents

COA (Certificate Of Analysis)

HPLC

NMR (Nuclear Magnetic Resonance)

MSDS (Material Safety Data Sheet)

Datasheet

SP2509

SP2509

Background

Documents

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