A reversible inhibitor of LSD1 (IC50 = 13 nM); allows increased methylation of H3K4

SP2509 – 1 mg

Brand:
Cayman
CAS:
1423715-09-6
Storage:
-20
UN-No:
Non-Hazardous - /

Lysine-specific demethylase 1 (LSD1) is a protein lysine demethylase that specifically demethylates histone H3 lysine 4 (H3K4), resulting in transcriptional repression.{14724} SP2509 is a reversible inhibitor of LSD1 (IC50 = 13 nM).{28684} It has no effect on monoamine oxidases A and B. SP2509 attenuates the binding of LSD1 to CoREST, allowing increased methylation of H3K4 and driving increased expression of p21, p27, and CCAAT/enhancer binding protein α in cultured acute myeloid leukemia (AML) cells.{28684,28685} It improves survival of mice with AML xenografts when given (25 mg/kg biweekly via intraperitoneal injection) for three weeks.{28684} Co-treatment of SP2509 with the pan-HDAC inhibitor panobinostat (Item No. 13280) synergistically kills AML cells in vitro and improves survival of mice engrafted with AML cells.{28684,28685}  

 

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Description

A reversible inhibitor of LSD1 (IC50 = 13 nM); allows increased methylation of H3K4, driving increased expression of p21, p27 and CCAAT/enhancer binding protein α in cultured AML cells; improves survival alone and synergizes with panobinostat in improving survival of mice engrafted with AML cells

Formal name: 3-(4-morpholinylsulfonyl)-benzoic acid (2E)-2-[1-(5-chloro-2-hydroxyphenyl)ethylidene]hydrazide

Synonyms:  HCI-2509|LSD1 Inhibitor VII

Molecular weight: 437.9

CAS: 1423715-09-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Demethylases||Research Area|Epigenetics, Transcription, & Translation|Erasers|Histone Demethylation

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