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Product Details

SP-2509 | LSD1 inhibitor

SP2509 (1423715-09-6) is a potent (IC50 = 13 nM) and reversible inhibitor of the histone demethylase LSD1 (KDM1A).1 It is inactive against the closely related flavin enzymes MAO A,B as well as lactate dehydrogenase, several CYP’s and hERG. LSD1 regulates the balance between self-renewal and differentiation of stem cells and is highly expressed in various cancers.2-6 SP2509 promotes autophagy in neuroblastoma cells.7

References/Citations

1) Sorna, et al. (2013), High-Throughput Virtual Screening Identifies Novel N’-(1-Phenylethylidene)-benzohydrazides as Potent, Specific, and Reversible LSD1 Inhibitors; J. Med. Chem. 56 9496
2) Hosseini and Minucci (2017) A comprehensive review of lysine-specific demethylase 1 and its roles in cancer; Epigenomics 9 1123
3) Fiskus et al. (2014), Highly effective combination of LSD1 (KDM1A) antagonist and pan-histone deacetylase inhibitor against human AML cells; Leukemia 28 2155
4) Wen et al. (2018), Novel combination of histone methylation modulators with therapeutic synergy against acute myeloid leukemia in vitro and in vivo; Cancer Lett. 413 35
5) Tsai et al. (2018), Stress-induced phosphoprotein 1 acts as a scaffold protein for glycogen synthase kinase-3 beta-mediated phosphorylation of lysine-specific demethylase 1; Oncogenesis 7 31
6) Lu et al. (2018), Hypoxia Promotes Resistance to EGFR Inhibition in NSCLC Cells via the Histone Demethylases LSD1 and PLU-1; Mol. Cancer Epub ahead of print June 22, 2018
7) Ambrosio et al. (2017), Lysine-specific demethylase LSD1 regulates autophagy in neuroblastoma through SESN2-dependent pathway; Oncogene 36 36701

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Catalog#  10-4019-0005

$70.00
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Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
1423715-09-6
Catalog Number:
10-4019
Activity:
LSD1 inhibitor
Chemical Name:
(E)-N’-(1-(5-Chloro-2-hydroxyphenyl)ethylidene)-3-(morpholinosulfonyl)benzohydrazide
Molecular Weight:
437.90
Molecular Formula:
C19H20ClN3O5S
Solubility:
Soluble in DMSO (up to at least 25 mg/ml)
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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