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SP2509

SP2509 是一种选择性 LSD1拮抗剂，IC50值为 13 nM。

CAS号

1423715-09-6

分子式

C19H20ClN3O5S

主要靶点

Histone Demethylase|Apoptosis

仅限科研使用

Cat No : CM04540

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Synonyms

HCI-2509

验证数据展示

  • CAS No.: 1423715-09-6

    SP2509
    CAS#: 1423715-09-6

产品信息

SP2509 is a specific histone demethylase LSD1 inhibitor(IC50 =13 nM).

CAS号 1423715-09-6
分子式 C19H20ClN3O5S
主要靶点 Histone Demethylase|Apoptosis
主要通路 表观遗传|凋亡
分子量 437.9
纯度 99.49%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 HCI-2509

靶点活性

LSD1:13 nM

体内活性

在OCI-AML3中,SP250能够抑制集落形成,诱导细胞凋亡。在AML细胞中,SP2509能够抑制LSD1与CoREST作用,增加启动子特异性H3K4Me3,同时诱导p53,p21和C/EBPα。在原代AML细胞中,SP2509诱导细胞的增殖。

体外活性

在负荷OCI-AML3异种移植物的小鼠中,SP2509（25 mg/kg i.p. ）,能够抑制肿瘤生长,延迟动物的存活.

溶解度

H2O:<1 mg/mL,DMSO:36 mg/mL (82.2 mM),Ethanol:<1 mg/mL

细胞实验

Cultured AML cells are treated with SP2509 and/or PS for 96?h. At the end of treatment, cells are washed free of the drugs and 500 cells per condition are plated in methylcellulose and incubated at 37?°C. Colony formation is measured 7–10 days after plating.(Only for Reference)

参考文献

1.Fiskus W, et al. Leukemia. 2014, 28(11), 2155-2164.

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