2. Epigenetics Apoptosis
  3. Histone Demethylase Apoptosis
  4. SP2509

SP2509 is a potent and selective antagonist of lysine specific demethylase 1 (LSD1) with an IC50 of 13 nM.

For research use only. We do not sell to patients.

SP2509 Chemical Structure

SP2509 Chemical Structure

CAS No. : 1423715-09-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
1 mg USD 26 In-stock
5 mg USD 66 In-stock
10 mg USD 99 In-stock
50 mg USD 297 In-stock
100 mg USD 495 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 8 publication(s) in Google Scholar

SP2509 Related Antibodies

Top Publications Citing Use of Products

    SP2509 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Aug 10;8(43):74434-74450.  [Abstract]

    ARK2 and TOV112D cells are treated with an LSD1 inhibitor SP2509 (100 nM) for 24 h. Equal amounts of protein lysates are analyzed with western blots with appropriate antibodies. Increased levels of H3K4Me2 indicated an inhibition of LSD1. GAPDH is used to confirm that equal amounts of proteins are present in all lanes.

    View All Histone Demethylase Isoform Specific Products:

    View All Isoforms
    KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    SP2509 is a potent and selective antagonist of lysine specific demethylase 1 (LSD1) with an IC50 of 13 nM[1].

    IC50 & Target

    KDM1/LSD1

     

    In Vitro

    SP2509 (250, 500, 1000 nM) inhibits LSD1 activity, depletes colony growth and induces apoptosis and cell death of cultured human acute myeloid leukemia cells, and increases H3K4Me3 on the promoters of p57 Kip, KLF4, and p21 and induces mRNA expression of p57Kip, KLF4 and p21 in AML cells. SP2509 (250, 1000 nM) induces features of morphologic differentiation of cultured and primary AML cells. Besides, SP2509 in combination with PS exerts synergistic lethal activity against cultured and primary AML cells[1]. SP2509 does not destabilize the CoREST-LSD1 interaction, and has no major destabilizing effect on the CRC. SP2509 (1 or 10 µM) induces cell death, but there are no morphological changes at a low concertation of 0.1 µM. SP2509 likewise interferes with the viability of medulloblastoma cells[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    SP2509 Related Antibodies
    In Vivo

    Treatment with SP2509 (25 mg/kg) and/or PS (5 mg/kg) significantly enhances PS-mediated loss of viability of CD34+ primary AML cells and improves the survival of mice bearing AML xenografts and primagrafts[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    437.90

    Formula

    C19H20ClN3O5S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(N/N=C(C1=CC(Cl)=CC=C1O)\C)C2=CC=CC(S(=O)(N3CCOCC3)=O)=C2
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, protect from light

    *In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 33 mg/mL (75.36 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2836 mL 11.4181 mL 22.8363 mL
    5 mM 0.4567 mL 2.2836 mL 4.5673 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (4.75 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.90%

    COA (247 KB) LCMS (100 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    Daoy and D283 Med cells are used in the assay. ONS-76 cells used. All medulloblastoma cell lines are kept in an incubator at 37°C in a 5% CO2/5% O2/90% N2 atmosphere with maximum humidity. XTT assays are performed in triplicates (n = 3) with three replicates for each using 1×103 Daoy cells/well, 4×103 D283 Med cells/well, and 1×103 ONS-76 cells/well in 100 µL of medium at initial seeding in 96-well plates.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Female NOD/SCID mice are exposed to 2.5 Gy of radiation. The following day, 5 million OCI-AmL3 cells are injected into the lateral tail vein of the mice and the mice are monitored for 7 days. Following treatments are administered in cohorts of 8 mice for each treatment: vehicle alone, 25 mg/kg SP2509, 5 mg/kg LBH589 and SP2509 plus LBH589. Treatments are initiated on day 7 for OCI-AmL3 cells. SP2509 (formulated in solubilization buffer [20% Cremaphor, 20% DMSO, 60% sterile water]) is administered twice per week (Tues and Thurs) intraperitoneally (IP) for 3 weeks, and then discontinued. LBH589 (formulated in 5% DMSO/ 95% normal saline) is administered by IP injection 3 days per week (M-W-F) for 3 weeks and discontinued. The doses of PS utilized in these studies are determined to be safe and effective. A separate in vivo experiment is conducted utilizing NSG mice and primary AmL cells. Following engraftment of the AmL cells (presence of greater than 1% CD45+ cells in the peripheral blood), mice are treated with SP2509 and/or PS, for three weeks.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2836 mL 11.4181 mL 22.8363 mL 57.0907 mL
    5 mM 0.4567 mL 2.2836 mL 4.5673 mL 11.4181 mL
    10 mM 0.2284 mL 1.1418 mL 2.2836 mL 5.7091 mL
    15 mM 0.1522 mL 0.7612 mL 1.5224 mL 3.8060 mL
    20 mM 0.1142 mL 0.5709 mL 1.1418 mL 2.8545 mL
    25 mM 0.0913 mL 0.4567 mL 0.9135 mL 2.2836 mL
    30 mM 0.0761 mL 0.3806 mL 0.7612 mL 1.9030 mL
    40 mM 0.0571 mL 0.2855 mL 0.5709 mL 1.4273 mL
    50 mM 0.0457 mL 0.2284 mL 0.4567 mL 1.1418 mL
    60 mM 0.0381 mL 0.1903 mL 0.3806 mL 0.9515 mL
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    SP2509 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    SP25091423715-09-6SP 2509SP-2509Histone DemethylaseApoptosisInhibitorinhibitorinhibit

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