Demethylase 1 (LSD1) antagonist, novel Lysine-specific
CAS：1423715-09-6
分子式：C19H20ClN3O5S
分子量：437.9
纯度：98%
存储：Store at -20°C

Background:

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]
参考文献:
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.