Home Epigenetics Histone Demethylase inhibitor - LSD1 inhibitor - Apoptosis related activator - Autophagy activator SP2509 For research use only.

SP2509

Synonyms: HCI-2509

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

SP2509 Chemical Structure

CAS: 1423715-09-6

Selleck's SP2509 has been cited by 25 Publications

1 Customer Review

Purity & Quality Control

Batch: Purity: 99.99%
99.99

SP2509 Related Products

Signaling Pathway

Histone Demethylase Signaling Pathways

Histone Demethylase Signaling Pathway

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation 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 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 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]
Kinase Assay 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 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.
In Vivo
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.
Animal Research Animal Models NOD/SCID mice bearing OCI-AML3 xenografts
Dosages 20% Cremaphor, 20% DMSO, 60% sterile water
Administration i.p.

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)

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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

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