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SP2509

13 Cited Publications

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Based on 13 publication(s) in Google Scholar

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

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Pureté: 99.50%
CAS No.: 1423715-09-6
Formule: C₁₉H₂₀ClN₃O₅S
Masse moléculaire:437.90

Stockage:

4°C, protect from light

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

SP2509 Chemical Structure

CAS No.: 1423715-09-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (13)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

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

Voir tous les produits spécifiques à Isoform Histone Demethylase :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.77 μM Compound: RC, Reference compound	Antiproliferative activity against human A2780 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay Antiproliferative activity against human A2780 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay	[PMID: 27524309]
A2780	IC₅₀	2.14 μM Compound: RC, Reference compound	Antiproliferative activity against human A2780 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human A2780 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 27524309]
A549	IC₅₀	0.83 μM Compound: RC, Reference compound	Antiproliferative activity against human A549 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay Antiproliferative activity against human A549 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay	[PMID: 27524309]
A549	IC₅₀	2.69 μM Compound: RC, Reference compound	Antiproliferative activity against human A549 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 27524309]
AGS	IC₅₀	6.19 μM Compound: SP-2509	Antiproliferative activity against human AGS cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human AGS cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 33957387]
AN3-CA	IC₅₀	0.356 μM Compound: 12	Growth inhibition of human AN3CA cells after 96 hrs by ATPlite luminescence assay Growth inhibition of human AN3CA cells after 96 hrs by ATPlite luminescence assay	[PMID: 24237195]
BGC-823	IC₅₀	8.08 μM Compound: SP-2509	Antiproliferative activity against human BGC-823 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human BGC-823 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 33957387]
BT-20	IC₅₀	0.489 μM Compound: 12	Growth inhibition of human BT20 cells after 96 hrs by ATPlite luminescence assay Growth inhibition of human BT20 cells after 96 hrs by ATPlite luminescence assay	[PMID: 24237195]
BT-549	IC₅₀	1.01 μM Compound: 12	Growth inhibition of human BT549 cells after 96 hrs by ATPlite luminescence assay Growth inhibition of human BT549 cells after 96 hrs by ATPlite luminescence assay	[PMID: 24237195]
DU-145	IC₅₀	0.62 μM Compound: RC, Reference compound	Antiproliferative activity against human DU145 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay Antiproliferative activity against human DU145 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay	[PMID: 27524309]
DU-145	IC₅₀	13.08 μM Compound: RC, Reference compound	Antiproliferative activity against human DU145 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human DU145 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 27524309]
HCT-116	IC₅₀	0.33 μM Compound: RC, Reference compound	Antiproliferative activity against human HCT116 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay Antiproliferative activity against human HCT116 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay	[PMID: 27524309]
HCT-116	IC₅₀	0.614 μM Compound: 12	Growth inhibition of human HCT116 cells after 96 hrs by ATPlite luminescence assay Growth inhibition of human HCT116 cells after 96 hrs by ATPlite luminescence assay	[PMID: 24237195]
HCT-116	IC₅₀	0.65 μM Compound: RC, Reference compound	Antiproliferative activity against human HCT116 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 27524309]
Hs-578T	IC₅₀	1.7 μM Compound: 12	Growth inhibition of human Hs 578T cells after 96 hrs by ATPlite luminescence assay Growth inhibition of human Hs 578T cells after 96 hrs by ATPlite luminescence assay	[PMID: 24237195]
HT-29	IC₅₀	0.429 μM Compound: 12	Growth inhibition of human HT-29 cells after 96 hrs by ATPlite luminescence assay Growth inhibition of human HT-29 cells after 96 hrs by ATPlite luminescence assay	[PMID: 24237195]
MCF7	IC₅₀	0.19 μM Compound: RC, Reference compound	Antiproliferative activity against human MCF7 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay Antiproliferative activity against human MCF7 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay	[PMID: 27524309]
MCF7	IC₅₀	0.44 μM Compound: RC, Reference compound	Antiproliferative activity against human MCF7 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 27524309]
MCF7	IC₅₀	0.62 μM Compound: SP2509; 4	Antiproliferative activity against human MCF7 cells after 48 to 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 to 72 hrs by MTT assay	[PMID: 29754076]
MCF7	IC₅₀	0.637 μM Compound: 12	Growth inhibition of human MCF7 cells after 96 hrs by ATPlite luminescence assay Growth inhibition of human MCF7 cells after 96 hrs by ATPlite luminescence assay	[PMID: 24237195]
MDA-MB-231	IC₅₀	0.75 μM Compound: RC, Reference compound	Antiproliferative activity against human MDA-MB-231 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay	[PMID: 27524309]
MDA-MB-231	IC₅₀	1.04 μM Compound: 12	Growth inhibition of human MDA-MB-231 cells after 96 hrs by ATPlite luminescence assay Growth inhibition of human MDA-MB-231 cells after 96 hrs by ATPlite luminescence assay	[PMID: 24237195]
MDA-MB-231	IC₅₀	1.4 μM Compound: RC, Reference compound	Antiproliferative activity against human MDA-MB-231 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 27524309]
MDA-MB-435	IC₅₀	1.44 μM Compound: 12	Growth inhibition of human MDA-MB-435 cells after 96 hrs by ATPlite luminescence assay Growth inhibition of human MDA-MB-435 cells after 96 hrs by ATPlite luminescence assay	[PMID: 24237195]
MDA-MB-468	IC₅₀	2.73 μM Compound: 12	Growth inhibition of human MDA-MB-468 cells after 96 hrs by ATPlite luminescence assay Growth inhibition of human MDA-MB-468 cells after 96 hrs by ATPlite luminescence assay	[PMID: 24237195]
MIA PaCa-2	IC₅₀	0.468 μM Compound: 12	Growth inhibition of human MIAPaCa2 cells after 96 hrs by ATPlite luminescence assay Growth inhibition of human MIAPaCa2 cells after 96 hrs by ATPlite luminescence assay	[PMID: 24237195]
MKN-1	IC₅₀	8.98 μM Compound: SP-2509	Antiproliferative activity against human MKN-1 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MKN-1 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 33957387]
MKN-45	IC₅₀	26.7 μM Compound: SP-2509	Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 33957387]
NCI-H1299	IC₅₀	1.73 μM Compound: RC, Reference compound	Antiproliferative activity against human NCI-H1299 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay Antiproliferative activity against human NCI-H1299 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay	[PMID: 27524309]
NCI-H1299	IC₅₀	3.01 μM Compound: RC, Reference compound	Antiproliferative activity against human NCI-H1299 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1299 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 27524309]
NCI-H460	IC₅₀	0.47 μM Compound: SP2509; 4	Antiproliferative activity against human H460 cells after 48 to 72 hrs by MTT assay Antiproliferative activity against human H460 cells after 48 to 72 hrs by MTT assay	[PMID: 29754076]
NCI-N87	IC₅₀	10.54 μM Compound: SP-2509	Antiproliferative activity against human NCI-N87 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human NCI-N87 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 33957387]
PANC-1	IC₅₀	1.104 μM Compound: 12	Growth inhibition of human PANC1 cells after 96 hrs by ATPlite luminescence assay Growth inhibition of human PANC1 cells after 96 hrs by ATPlite luminescence assay	[PMID: 24237195]
PC-3	IC₅₀	19.72 μM Compound: RC, Reference compound	Antiproliferative activity against human PC3 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human PC3 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 27524309]
PC-3	IC₅₀	2.16 μM Compound: 12	Growth inhibition of human PC3 cells after 96 hrs by ATPlite luminescence assay Growth inhibition of human PC3 cells after 96 hrs by ATPlite luminescence assay	[PMID: 24237195]
PC-3	IC₅₀	4.45 μM Compound: RC, Reference compound	Antiproliferative activity against human PC3 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay Antiproliferative activity against human PC3 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay	[PMID: 27524309]
Raji	IC₅₀	0.98 μM Compound: SP2509; 4	Antiproliferative activity against human Raji cells after 48 to 72 hrs by MTT assay Antiproliferative activity against human Raji cells after 48 to 72 hrs by MTT assay	[PMID: 29754076]
SK-N-MC	IC₅₀	0.329 μM Compound: 12	Growth inhibition of human SK-N-MC cells after 96 hrs by ATPlite luminescence assay Growth inhibition of human SK-N-MC cells after 96 hrs by ATPlite luminescence assay	[PMID: 24237195]
SMMC-7721	IC₅₀	15.75 μM Compound: RC, Reference compound	Antiproliferative activity against human SMMC7721 over-expressing LSD1 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human SMMC7721 over-expressing LSD1 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 27524309]
SMMC-7721	IC₅₀	5.36 μM Compound: RC, Reference compound	Antiproliferative activity against human SMMC7721 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay Antiproliferative activity against human SMMC7721 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay	[PMID: 27524309]
SNU1	IC₅₀	8.03 μM Compound: SP-2509	Antiproliferative activity against human SNU1 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human SNU1 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 33957387]
T47D	IC₅₀	0.649 μM Compound: 12	Growth inhibition of human T47D cells after 96 hrs by ATPlite luminescence assay Growth inhibition of human T47D cells after 96 hrs by ATPlite luminescence assay	[PMID: 24237195]
U-87MG ATCC	IC₅₀	1.16 μM Compound: 12	Growth inhibition of human U87 cells after 96 hrs by ATPlite luminescence assay Growth inhibition of human U87 cells after 96 hrs by ATPlite luminescence assay	[PMID: 24237195]

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.

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.

Chemical Information

CAS No. 1423715-09-6
Appearance Solid
Masse moléculaire 437.90
Formule C₁₉H₂₀ClN₃O₅S
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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light

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

Publications (13)

All Histological Imaging/StainingIFWBCell Proliferation/Viability Assay

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Journal Impact Factor

Cancer Discov

Iron-(Fe3+) dependent reactivation of telomerase drives colorectal cancers. [Abstract]

2024 Oct 4;14(10):1940-1963. PMID: 38885349
Acta Pharm Sin B

LSD1 inhibition suppresses the growth of clear cell renal cell carcinoma via upregulating P21 signaling. [Abstract]

2019 Mar;9(2):324-334. PMID: 30972280
J Exp Clin Cancer Res

The PRMT5-LSD1 axis confers Slug dual transcriptional activities and promotes breast cancer progression. [Abstract]

2022 Jun 2;41(1):191. PMID: 35655230
Cell Death Dis

KDM1A epigenetically enhances RAD51 expression to suppress the STING-associated anti-tumor immunity in esophageal squamous cell carcinoma. [Abstract]

2024 Dec 6;15(12):882. PMID: 39638799
Cell Death Discov

Lysine-specific demethylase 1 inhibition enhances autophagy and attenuates early-stage post-spinal cord injury apoptosis. [Abstract]

2021 Apr 6;7(1):69. PMID: 33824301

SP2509 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2021 Apr 6;7(1):69. [Abstract]

Representative H&E stained transverse sections treated with SP2509 (25 mg/kg, i.p.).

SP2509 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2021 Apr 6;7(1):69. [Abstract]

Nissl staining for testing survival neurons to indicate each group’s motor neuron amount treated with SP2509 (25 mg/kg, i.p.).

SP2509 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2021 Apr 6;7(1):69. [Abstract]

Sample pictures of TUNEL-positive cells from the sham, SCI, and SCI + SP2509 (25 mg/kg, i.p.) groups at 1 week following injury.

SP2509 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2021 Apr 6;7(1):69. [Abstract]

SP2509 (25 mg/kg, i.p.) decreased the ratio of Bax to Bcl-2 and for cleaved caspase3 to caspase3 by Western blot.

SP2509 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2021 Apr 6;7(1):69. [Abstract]

CCK-8’s measurement of a quantitative analysis of relative cell viability treated with SP2509 (0, 4, 8, 16, 32, 64 μM).
Molecules

Modulatory Effect of Curcumin on Expression of Methyltransferase/Demethylase in Colon Cancer Cells: Impact on wt p53, mutp53 and c-Myc. [Abstract]

2025 Jul 22;30(15):3054. PMID: 40807229
Clin Exp Med

Corin: a dual inhibitor for KDM1A/HDAC1, suppresses hepatocellular carcinoma by triggering cuproptosis. [Abstract]

2025 Nov 25;26(1):33. PMID: 41286164
Brain Res Bull

Lysine-specific Demethylase 1 in Primary Sensory Neurons Participates in Chronic Compression of Dorsal Root Ganglion-induced Neuropathic Pain. [Abstract]

2022 Dec:191:30-39. PMID: 36240908
Biochim Biophys Acta Mol Cell Res

The yin and yang interplay between HDAC6 and KDM1 regulates the lysosomal degradation of mutp53 in colon cancer cells undergoing TG-induced ER stress. [Abstract]

2026 Jun;1873(5):120164. PMID: 42203131
ACS Pharmacol Transl Sci

Comprehensive in Vitro Characterization of the LSD1 Small Molecule Inhibitor Class in Oncology. [Abstract]

2021 Nov 12;4(6):1818-1834. PMID: 34927013
bioRxiv

2025 Sep 21.
Boston University

2025.
Oncotarget

Lysine-specific demethylase 1 (LSD1) destabilizes p62 and inhibits autophagy in gynecologic malignancies. [Abstract]

2017 Aug 10;8(43):74434-74450. PMID: 29088798

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.

Solvant et solubilité

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2836 mL

11.4181 mL

22.8363 mL

5 mM

0.4567 mL

2.2836 mL

4.5673 mL

10 mM

0.2284 mL

1.1418 mL

2.2836 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
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Saline +

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).

Working solution concentration: 0.22 mg/mL

Protocole

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.

MedChemExpress (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.

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (275 KB)
SDS (393 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Fiskus W, et al. Highly effective combination of LSD1 (KDM1A) antagonist and pan-histone deacetylase inhibitor against human AML cells. Leukemia. 2014 Nov;28(11):2155-64. [Content Brief]

[2]. Inui K, et al. Stepwise assembly of functional C-terminal REST/NRSF transcriptional repressor complexes as a drug target. Protein Sci. 2017 Feb 20 [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

SP2509

13 Cited Publications

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SP2509

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Cysteine Targeted Covalent Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Apoptosis Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Publications Citing Use of MedChemExpress (MCE) SP2509

Voir tous les produits spécifiques à Isoform Histone Demethylase

Activité biologique

Chemical Information

Publications (13)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

SP2509

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Cysteine Targeted Covalent Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Apoptosis Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Publications Citing Use of MedChemExpress (MCE) SP2509

Voir tous les produits spécifiques à Isoform Histone Demethylase

Activité biologique

Chemical Information

Publications (13)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

SP2509 Related Classifications

HY-12635 Related Classifications