SP2509

Catalog No.S7680 Batch:S768001

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Technical Data

Formula

C19H20ClN3O5S
Molecular Weight 437.90 CAS No. 1423715-09-6
Solubility (25°C)* In vitro DMSO 83 mg/mL (189.54 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
7.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 140 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description SP2509 (HCI-2509) is a selective histone demethylase LSD1 inhibitor with IC50 of 13 nM, showing no activity against MAO-A, MAO-B, lactate dehydrogenase and glucose oxidase. SP2509 induces apoptosis and promotes autophagy.
Targets
LSD1 [1]
(Cell-free assay)
13 nM
In vitro

In AML cells, SP2509 inhibits the association of LSD1 with CoREST, increases promoter-specific H3K4Me3 and induces p53, p21 and C/EBPα. SP2509 also significantly inhibits the colony growth and induces apoptosis of OCI-AML3.

Protocol (from reference)

Kinase Assay:

[1]
  • SP2509 activity assays

    Test compounds are diluted to 20 × the desired test concentration in 100% DMSO and 2.5 μL of the diluted drug sampleis added to a black 384-well plate. The LSD1 enzyme stock is diluted 17-fold with assay buffer and 40 μL of the diluted LSD1 enzyme is added to the appropriate wells. Substrate, consisting of horseradish peroxidase, dimethyl K4 peptide corresponding to the first 21 amino acids of the N-terminal tail of histone H3, and 10-acetyl-3,7-dihydroxyphenoxazine is then added to wells. Resorufin is analyzed on an Envision plate reader with an excitation wavelength of 530 nm and an emission wavelength of 595 nm. The activity of SP2509 on the other oxidases is determined by using commercially available kits. The glucose oxidase activity (which also noncovalently binds FAD in an elongate conformation), is determined using the glucose oxidase kit. The MAO assays are performed using the MAO-glo kit with MAO-A and MAO-B.
Cell Assay:

[1]
  • Cell lines

    OCI-AML3, MV4-11 and MOLM13 cells

  • Concentrations

    ~10 μM

  • Incubation Time

    96 hours

  • Method

    Cultured AML cells are treated with SP2509 and/or PS for 96 h. At the end of treatment, cells are washed free of the drugs and 500 cells per condition are plated in methylcellulose and incubated at 37 °C. Colony formation is measured 7–10 days after plating.
Animal Study:

[1]
  • Animal Models

    NOD/SCID mice bearing OCI-AML3 xenografts

  • Dosages

    20% Cremaphor, 20% DMSO, 60% sterile water

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , Br J Haematol, 2017, doi: 10.1111/bjh.14983]

Selleck's SP2509 has been cited by 27 publications

Transposable elements-mediated recruitment of KDM1A epigenetically silences HNF4A expression to promote hepatocellular carcinoma [ Nat Commun, 2024, 15(1):5631] PubMed: 38965210
Pharmacological inhibition of LSD1 suppresses growth of hepatocellular carcinoma by inducing GADD45B [ MedComm (2020), 2023, 4(3):e269] PubMed: 37250145
LSD1 promotes prostate cancer reprogramming by repressing TP53 signaling independently of its demethylase function [ JCI Insight, 2023, 8(15)e167440] PubMed: 37440313
LSD1 promotes prostate cancer reprogramming by repressing TP53 signaling independently of its demethylase function [ JCI Insight, 2023, 8(15)e167440] PubMed: 37440313
RAS and PP2A activities converge on epigenetic gene regulation [ Life Sci Alliance, 2023, 6(5)e202301928] PubMed: 36858798
Leveraging patient derived models of FGFR2 fusion positive intrahepatic cholangiocarcinoma to identify synergistic therapies [ NPJ Precis Oncol, 2022, 6(1):75] PubMed: 36274097
High-Throughput Drug Library Screening in Primary KMT2A-Rearranged Infant ALL Cells Favors the Identification of Drug Candidates That Activate P53 Signaling [ Biomedicines, 2022, 10(3)638] PubMed: 35327440
SP2509, a Selective Inhibitor of LSD1, Suppresses Retinoblastoma Growth by Downregulating β-catenin Signaling [ Invest Ophthalmol Vis Sci, 2022, 63(3):20] PubMed: 35297943
Targeting LSD1 suppresses stem cell-like properties and sensitizes head and neck squamous cell carcinoma to PD-1 blockade [ Cell Death Dis, 2021, 12(11):993] PubMed: 34689153
KRT6A Promotes Lung Cancer Cell Growth and Invasion Through MYC-Regulated Pentose Phosphate Pathway [ Front Cell Dev Biol, 2021, 9:694071] PubMed: 34235156

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.