SP2509

生物活性体外研究体内研究生物活性靶点体外研究体内研究 SP2509 试剂级价格

SP2509

CAS号:1423715-09-6
英文名:SP2509
中文名:SP2509
CBNumber:CB22734796
分子式:C19H20ClN3O5S
分子量:437.9
MOL File:1423715-09-6.mol

SP2509化学性质

密度 :1.44±0.1 g/cm3(Predicted)
储存条件 :+2C to +8C
溶解度 :Soluble in DMSO (up to at least 25 mg/ml)
形态 :Off-white solid
酸度系数(pKa) :7.96±0.43(Predicted)
颜色 :White
稳定性 :Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

SP2509性质、用途与生产工艺

生物活性 SP2509是一种选择性histone demethylase LSD1抑制剂，IC50为 13 nM，对MAO-A，MAO-B，乳酸脱氢酶和葡萄糖氧化酶没有活性。
体外研究 In AML cells, SP2509 inhibits the association of LSD1 with CoREST, increases promoter-specific H3K4Me3 and induces p53, p21 and C/EBPα. SP2509 also significantly inhibits the colony growth and induces apoptosis of OCI-AML3. In addition, SP2509 induces differentiation of cultured and primary AML cells, and exerts synergistic lethal activity when used in combination with panobinostat.
体内研究 In mice bearing OCI-AML3 xenografts, SP2509 (25 mg/kg i.p.) significantly improved the survival of the mice, while co-treatment with SP2509 and panobinostat exerts superior in vivo activity.
生物活性 SP2509 (HCI-2509)是一种选择性histone demethylase LSD1抑制剂，IC50为 13 nM，对MAO-A，MAO-B，乳酸脱氢酶和葡萄糖氧化酶没有活性。SP2509 可诱导凋亡并促进自噬。
靶点
Target Value
LSD1
(Cell-free assay) 13 nM
体外研究
在AML细胞中，SP2509抑制LSD1与CoREST联合，增加启动子特异性H3K4Me3，并诱导p53，p21和C/EBPα。SP250也显著抑制菌落生长，并诱导OCI-AML3的细胞凋亡。此外，SP2509诱导培养的和原代AML细胞的增殖，并且与panobinostat结合使用时，发挥协同致死性。
体内研究在负荷OCI-AML3异种移植物的小鼠体内，SP2509 (25 mg/kg i.p.)显著提高小鼠的存活率，与SP2509和panobinostat联合治疗发挥出优良的体内活性。