For research use only.

Catalog No.S7680 Synonyms: HCI-2509

14 publications

SP2509 Chemical Structure

CAS No. 1423715-09-6

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.

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Selleck's SP2509 has been cited by 14 publications

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  • Cells were exposed to drugs for 48 h or for the indicated times. Cell death and Dwm dissipation were determined by flow cytometric analyses of propidium iodide uptake or DiOC6(3) staining, respectively. Caspase 3/7 activity was determined using the fluorogenic substrate Ac-DEVD-AMC; relative caspase 3/7 activities are the ratio of treated cells to untreated cells.

    Br J Haematol, 2017, doi: 10.1111/bjh.14983. SP2509 purchased from Selleck.

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Choose Selective Histone Demethylase Inhibitors

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.
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. In addition, SP2509 induces differentiation of cultured and primary AML cells, and exerts synergistic lethal activity when used in combination with panobinostat. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U87 M4nTRmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmjsPVYhcA>? NXnp[Yt1T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hXTh5IHPlcIx{KGGodHXyJFk3KGi{czDifUBCXFCuaYTlJIx2dWmwZYPj[Y5k\SCjc4PhfUBKSzVyPUGuNVYh|ryP M1npNlI1OjN5MUm1
SK-N-MC NEOzeINIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2TjWlk3KGh? MorpS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gV2suVi2PQzDj[YxteyCjZoTldkA6PiCqcoOgZpkhSVSSbHn0[UBtfW2rbnXzZ4Vv[2ViYYPzZZkhUUN3ME2wMlMzQSEQvF2= NGHrSJEzPDJ|N{G5OS=>
T47D MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYW1V|F[QTZiaB?= NXi1c|EyT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hXDR5RDDj[YxteyCjZoTldkA6PiCqcoOgZpkhSVSSbHn0[UBtfW2rbnXzZ4Vv[2ViYYPzZZkhUUN3ME2wMlY1QSEQvF2= NFfGR3gzPDJ|N{G5OS=>
PC3 NIrRdYpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVHzeJVHQTZiaB?= NVXmTHpmT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hWEN|IHPlcIx{KGGodHXyJFk3KGi{czDifUBCXFCuaYTlJIx2dWmwZYPj[Y5k\SCjc4PhfUBKSzVyPUKuNVYh|ryP NXHzWJlMOjR{M{exPVU>
PANC1 Moj5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NETCc3Q6PiCq NGDLbm1Iem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBRSU6FMTDj[YxteyCjZoTldkA6PiCqcoOgZpkhSVSSbHn0[UBtfW2rbnXzZ4Vv[2ViYYPzZZkhUUN3ME2xMlExPCEQvF2= Mmr0NlQzOzdzOUW=
MIAPaCa2 M{X1Zmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWi5OkBp MnHES5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUWlCWGGFYUKgZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KEGWUHzpeIUhdHWvaX7ld4NmdmOnIHHzd4F6KEmFNUC9NE41PjhizszN NF;KeIczPDJ|N{G5OS=>
MDA-MB-468 NH\he3dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVnmdGI3QTZiaB?= M13tZ2dzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj20Olgh[2WubIOgZYZ1\XJiOU[gbJJ{KGK7IFHUVIxqfGVibIXtbY5me2OnbnPlJIF{e2G7IFnDOVA:Oi55MzFOwG0> MX:yOFI{PzF7NR?=
MDA-MB-435 NYW5foVOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1PTU|k3KGh? NEnuXZhIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBOTEFvTVKtOFM2KGOnbHzzJIFnfGW{IEm2JIhzeyCkeTDBWHBtcXSnIHz1cYlv\XOlZX7j[UBie3OjeTDJR|UxRTFwNESg{txO NFXyWlYzPDJ|N{G5OS=>
MDA-MB-231 NXHWe2VWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlvEPVYhcA>? MVTHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHmeIVzKDl4IHjyd{BjgSCDVGDsbZRmKGy3bXnu[ZNk\W6lZTDhd5NigSCLQ{WwQVEvODRizszN NWP0SVNEOjR{M{exPVU>
MCF7 M2\iXmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVK5OkBp MUTHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IEm2JIhzeyCkeTDBWHBtcXSnIHz1cYlv\XOlZX7j[UBie3OjeTDJR|UxRTBwNkO3JO69VQ>? MoHrNlQzOzdzOUW=
HT-29 MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mli3PVYhcA>? M{f1fWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGhVNTJ7IHPlcIx{KGGodHXyJFk3KGi{czDifUBCXFCuaYTlJIx2dWmwZYPj[Y5k\SCjc4PhfUBKSzVyPUCuOFI6KM7:TR?= NInLU4kzPDJ|N{G5OS=>
Hs MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGLne|A6PiCq NXKzWGJwT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUHNiNUe4WEBk\WyuczDh[pRmeiB7NjDodpMh[nliQWTQcIl1\SCudX3pcoV{[2WwY3WgZZN{[XliSVO1NF0yNjdizszN MViyOFI{PzF7NR?=
HER218 MX3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlrDPVYhcA>? M3HJOWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGhGWjJzODDj[YxteyCjZoTldkA6PiCqcoOgZpkhSVSSbHn0[UBtfW2rbnXzZ4Vv[2ViYYPzZZkhUUN3ME2wMlYyOiEQvF2= MUGyOFI{PzF7NR?=
HCT116 MYXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3Lyc|k3KGh? MWTHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgPVYhcHK|IHL5JGFVWGyrdHWgcJVucW6nc3PlcoNmKGG|c3H5JGlEPTB;MD62NVQh|ryP MYiyOFI{PzF7NR?=
BT20 MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mm\UPVYhcA>? NGDObFJIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBDXDJyIHPlcIx{KGGodHXyJFk3KGi{czDifUBCXFCuaYTlJIx2dWmwZYPj[Y5k\SCjc4PhfUBKSzVyPUCuOFg6KM7:TR?= NV\zVopNOjR{M{exPVU>
BT549 M{PZPWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHnD[ow6PiCq M3nJOGdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGJVPTR7IHPlcIx{KGGodHXyJFk3KGi{czDifUBCXFCuaYTlJIx2dWmwZYPj[Y5k\SCjc4PhfUBKSzVyPUGuNFEh|ryP NHHYfXUzPDJ|N{G5OS=>
AN3CA NUjLdXBmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV25OIhrQTZiaB?= NV\DXIRuT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hSU5|Q1GgZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KEGWUHzpeIUhdHWvaX7ld4NmdmOnIHHzd4F6KEmFNUC9NE4{PTZizszN NXSxcpNXOjR{M{exPVU>

... Click to View More Cell Line Experimental Data

In vivo In mice bearing OCI-AML3 xenografts, SP2509 (25 mg/kg i.p.) significantly improved the survival of the mice, while co-treatment with SP2509 and panobinostat exerts superior in vivo activity.


Kinase Assay:[1]
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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 Research:[1]
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  • 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.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: NOD/SCID mice bearing OCI-AML3 xenografts
  • Dosages: 20% Cremaphor, 20% DMSO, 60% sterile water
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 38 mg/mL (86.77 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
10% DMSO+corn oil
For best results, use promptly after mixing.

* 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.

Chemical Information

Molecular Weight 437.90


CAS No. 1423715-09-6
Storage powder
in solvent
Synonyms HCI-2509
Smiles CC(=NNC(=O)C1=CC(=CC=C1)S(=O)(=O)N2CCOCC2)C3=C(C=CC(=C3)Cl)O

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Histone Demethylase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID