SP2509

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SP2509

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Cat No: 15487

Biochemicals - Small Molecule Inhibitors

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 ef...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

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

Correlated keywords:

1287421-04-8 inhibitor LSD1 biochemical cancer epigenetic gene regulation histone modification intracellular signaling lysine-specific demethylase 1 SP-2509 HCI2509

Product Overview:
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}

Size	1 mg
Shipping	dry ice
CAS Number	1423715-09-6
Molecular Formula	C₁₉H₂₀ClN₃O₅S
SMILES	O=S(C1=CC(C(N/N=C(C)/C2=C(O)C=CC(Cl)=C2)=O)=CC=C1)(N3CCOCC3)=O
Molecular Weight	437,9
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2903.99
UNSPSC code	12352100

Technical File

MSDS

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.