SP2509

SP2509

Author: ApexBio

spu:

B4894

CAS:

1423715-09-6

purity:

0.9959

shortsummary:

Demethylase 1 (LSD1) antagonist, novel Lysine-specific

staurosporine solubility

Formula:

C19H20ClN3O5S

M.Wt:

437.90

Chemical Name:

(E)-N'-(1-(5-chloro-2-hydroxyphenyl)ethylidene)-3-(morpholinosulfonyl)benzohydrazide

SMILES:

OC1=CC=C(Cl)C=C1/C(C)=N/NC(C2=CC=CC(S(=O)(N3CCOCC3)=O)=C2)=O

Solubility:

insoluble in H2O; insoluble in EtOH; ≥19.45 mg/mL in DMSO

Storage:

Store at -20°C

Physical Appearance:

A solid

DeliveryTime:

In stock

JMJD2 inhibitor Description

ShippingType:

Blue ice

description:

SP2509 is a novel Lysine specific demethylase 1 (LSD1) antagonist (IC50 = 13nM) with no effect on MAO-A and MAO-B. [1]
LSD1 demethylates mono-/di-methylated lysine 4 on histone H3. High expression of LSD1 is associated with poor prognosis in cancer. [2]
In cultured human AML cells, SP2590 inhibited LSD1 activity, deplete colony growth and elicit apoptosis. SP2590 also inhibited the LSD1 binding to CoREST, increase promoter-specific H3K4Me3 and induces p53, p21 and C/EBPα in AML cells. Moreover, SP2590 promotes differentiated of cultured and primary AML cell. [1]
In mice carrying AML xenografts, SP2590 treatment alone significantly improved the survival of mice and co-treatment with an-HDAC inhibitor (HDI) panobinostat (PS) exhibited superior in vivo activity. [1]
References:
1. Fiskus W, Sharma S, Shah B, Portier BP, Devaraj SG, Liu K, Iyer SP, Bearss D, Bhalla KN. Highly effective combination of LSD1 (KDM1A) antagonist andpan-histone deacetylase inhibitor against human AML cells. Leukemia. 2014 Nov;28(11):2155-64.
2. Zhao ZK, Yu HF, Wang DR, Dong P, Chen L, Wu WG, Ding WJ, Liu YB.
Overexpression of lysine specific demethylase 1 predicts worse prognosis in primary hepatocellular carcinoma patients. World J Gastroenterol. 2012 Dec 7;18(45):6651-6.

related websites:

APExBIO Technology LLC is a premier provider of Small Molecule Inhibitors/Activators, Compound Libraries, Peptides, Assay Kits, Fluorescent Labels, Enzymes, Modified Nucleotides, mRNA synthesis and various tools for Molecular Biology. We carry a broad product line in over 4451 different research areas such as cancer, immunology, neurosciences, apoptosis and epigenetics etc. Based in USA (Houston, Texas), we have been serving the needs of customers across the world.