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SP2509

Name: SP2509
Brand: Selleck Chemicals
SKU: S7680
Rating: 5 (27 reviews)

Synonyms: HCI-2509

Catalog No.S7680 Purity:99.99%

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.

SP2509 Chemical Structure

CAS No. 1423715-09-6

Purity & Quality Control

Batch: Purity: 99.99%

99.99

SP2509 Related Products

Related Targets	KDM1 KDM2 KDM3 KDM4 KDM5 KDM6	Click to Expand
Related Products	GSK J4 HCl CPI-455 HCl Iadademstat (ORY-1001) 2HCl GSK-LSD1 2HCl JIB-04 OG-L002 ML324 IOX1 GSK J1 CP2 CPI-455	Click to Expand
Related Compound Libraries	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Highly Selective Inhibitor Library	Click to Expand

Signaling Pathway

Histone Demethylase Signaling Pathway

Cell Data

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
U87	Growth inhibition assay	96 h	Growth inhibition of human U87 cells after 96 hrs by ATPlite luminescence assay IC50=1.16 μM	24237195
SK-N-MC	Growth inhibition assay	96 h	Growth inhibition of human SK-N-MC cells after 96 hrs by ATPlite luminescence assay IC50=0.329 μM	24237195
T47D	Growth inhibition assay	96 h	Growth inhibition of human T47D cells after 96 hrs by ATPlite luminescence assay IC50=0.649 μM	24237195
PC3	Growth inhibition assay	96 h	Growth inhibition of human PC3 cells after 96 hrs by ATPlite luminescence assay IC50=2.16 μM	24237195
PANC1	Growth inhibition assay	96 h	Growth inhibition of human PANC1 cells after 96 hrs by ATPlite luminescence assay IC50=1.104 μM	24237195
MIAPaCa2	Growth inhibition assay	96 h	Growth inhibition of human MIAPaCa2 cells after 96 hrs by ATPlite luminescence assay IC50=0.468 μM	24237195
MDA-MB-468	Growth inhibition assay	96 h	Growth inhibition of human MDA-MB-468 cells after 96 hrs by ATPlite luminescence assay IC50=2.73 μM	24237195
MDA-MB-435	Growth inhibition assay	96 h	Growth inhibition of human MDA-MB-435 cells after 96 hrs by ATPlite luminescence assay IC50=1.44 μM	24237195
MDA-MB-231	Growth inhibition assay	96 h	Growth inhibition of human MDA-MB-231 cells after 96 hrs by ATPlite luminescence assay IC50=1.04 μM	24237195
MCF7	Growth inhibition assay	96 h	Growth inhibition of human MCF7 cells after 96 hrs by ATPlite luminescence assay IC50=0.637 μM	24237195
HT-29	Growth inhibition assay	96 h	Growth inhibition of human HT-29 cells after 96 hrs by ATPlite luminescence assay IC50=0.429 μM	24237195
Hs	Growth inhibition assay	96 h	Growth inhibition of human Hs 578T cells after 96 hrs by ATPlite luminescence assay IC50=1.7 μM	24237195
HER218	Growth inhibition assay	96 h	Growth inhibition of human HER218 cells after 96 hrs by ATPlite luminescence assay IC50=0.612 μM	24237195
HCT116	Growth inhibition assay	96 h	Growth inhibition of human HCT116 cells after 96 hrs by ATPlite luminescence assay IC50=0.614 μM	24237195
BT20	Growth inhibition assay	96 h	Growth inhibition of human BT20 cells after 96 hrs by ATPlite luminescence assay IC50=0.489 μM	24237195
BT549	Growth inhibition assay	96 h	Growth inhibition of human BT549 cells after 96 hrs by ATPlite luminescence assay IC50=1.01 μM	24237195
AN3CA	Growth inhibition assay	96 h	Growth inhibition of human AN3CA cells after 96 hrs by ATPlite luminescence assay IC50=0.356 μM	24237195
HCT116	Antiproliferative assay	96 hrs	Antiproliferative activity against human HCT116 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay, IC50 = 0.33 μM.	27524309
MCF7	Antiproliferative assay	72 hrs	Antiproliferative activity against human MCF7 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 0.44 μM.	27524309
DU145	Antiproliferative assay	96 hrs	Antiproliferative activity against human DU145 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay, IC50 = 0.62 μM.	27524309
HCT116	Antiproliferative assay	72 hrs	Antiproliferative activity against human HCT116 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 0.65 μM.	27524309
MDA-MB-231	Antiproliferative assay	96 hrs	Antiproliferative activity against human MDA-MB-231 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay, IC50 = 0.75 μM.	27524309
A2780	Antiproliferative assay	96 hrs	Antiproliferative activity against human A2780 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay, IC50 = 0.77 μM.	27524309
A549	Antiproliferative assay	96 hrs	Antiproliferative activity against human A549 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay, IC50 = 0.83 μM.	27524309
MDA-MB-231	Antiproliferative assay	72 hrs	Antiproliferative activity against human MDA-MB-231 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 1.4 μM.	27524309
NCI-H1299	Antiproliferative assay	96 hrs	Antiproliferative activity against human NCI-H1299 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay, IC50 = 1.73 μM.	27524309
A2780	Antiproliferative assay	72 hrs	Antiproliferative activity against human A2780 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 2.14 μM.	27524309
A549	Antiproliferative assay	72 hrs	Antiproliferative activity against human A549 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 2.69 μM.	27524309
NCI-H1299	Antiproliferative assay	72 hrs	Antiproliferative activity against human NCI-H1299 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 3.01 μM.	27524309
PC3	Antiproliferative assay	96 hrs	Antiproliferative activity against human PC3 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay, IC50 = 4.45 μM.	27524309
SMMC7721	Antiproliferative assay	96 hrs	Antiproliferative activity against human SMMC7721 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay, IC50 = 5.36 μM.	27524309
DU145	Antiproliferative assay	72 hrs	Antiproliferative activity against human DU145 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 13.08 μM.	27524309
LSD1	Antiproliferative assay	72 hrs	Antiproliferative activity against human SMMC7721 over-expressing LSD1 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 15.75 μM.	27524309
PC3	Antiproliferative assay	72 hrs	Antiproliferative activity against human PC3 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 19.72 μM.	27524309
H460	Antiproliferative assay	48 to 72 hrs	Antiproliferative activity against human H460 cells after 48 to 72 hrs by MTT assay, IC50 = 0.47 μM.	29754076
MCF7	Antiproliferative assay	48 to 72 hrs	Antiproliferative activity against human MCF7 cells after 48 to 72 hrs by MTT assay, IC50 = 0.62 μM.	29754076
Raji	Antiproliferative assay	48 to 72 hrs	Antiproliferative activity against human Raji cells after 48 to 72 hrs by MTT assay, IC50 = 0.98 μM.	29754076
Click to View More Cell Line Experimental Data

Biological Activity

Description

Targets

LSD1 ^[1]
(Cell-free assay)

13 nM

In vitro
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.
Kinase Assay	SP2509 activity assays
Kinase Assay	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 Research	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.

References

[1] Fiskus W, et al. Leukemia. 2014, 28(11), 2155-2164.

Chemical Information & Solubility

Molecular Weight	437.90	Formula	C₁₉H₂₀ClN₃O₅S
CAS No.	1423715-09-6	SDF	Download SP2509 SDF
Smiles	CC(=NNC(=O)C1=CC(=CC=C1)S(=O)(=O)N2CCOCC2)C3=C(C=CC(=C3)Cl)O
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 83 mg/mL ( (189.54 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	7.000mg/ml (15.99mM)	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.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	10%DMSO 1 90%Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (11.42mM)	Taking the 1 mL working solution as an example, add 100 μL of 50 mg/ml clear DMSO stock solution to 900 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.500mg/ml (7.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 70 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.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

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