SP2509

Catalog No.S7680 Synonyms: HCI-2509

SP2509 Chemical Structure

Molecular Weight(MW): 437.90

SP2509 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.

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Biological Activity

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

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.

Protocol

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
  • Formulation: 25 mg/kg twice per week
  • 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 individually and in order:
10% DMSO+corn oil
5mg/mL

* 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
Formula

C19H20ClN3O5S

CAS No. 1423715-09-6
Storage powder
Synonyms HCI-2509

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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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Related Antibodies

Histone Demethylase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID