GSK2879552CAS号： 1401966-69-5分子式： C23H28N2O2分子量： 364.48描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 描述 |
GSK2879552 is an orally available, irreversible, inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.
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| 纯度 |
>98%
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| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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| 基本信息 | |
| 别名 |
GSK-2879552,GSK 2879552
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| 外观 |
Powder
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| 可溶性/溶解性 |
Water 44 mg/mL (100.59 mM)
DMSO 29 mg/mL (66.3 mM) |
| 生物活性 | |
| 靶点 |
Histone Demethylase
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| In vitro(体外研究) |
GSK2879552 inhibits KDM1A histone demethylase activity, inducing differentiation of sorafenib-resistant cells and attenuates stemness properties. GSK2879552 derepresses the transcription of Wnt antagonists and downregulates β-catenin signaling activity in sorafenib-resistant cells. GSK2879552 is 280-fold selective over D-amino acid oxidase, allowing for direct comparison of inactivation efficiency (KIapp=520 ± 170 μM, kinact=0.12 ± 0.01 min−1, kinact/KIapp=2.3×10-4 ± 1.31×10-5 min-1 μM-1). GSK2879552 inhibits the growth of 9/28 small cell lung carcinoma (SCLC) lines and 20/29 AML lines, with EC50 of 2-240 nM.
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| In vivo(体内研究) |
GSK2879552 (1.5 mg/kg, p.o.) treatment exhibits tumor growth inhibition in SCLC xenograft bearing mice. There is 57% and 83% tumor growth inhibition (TGI) in NCI-H526 and NCI-H1417 tumor bearing mice respectively. NCI-H510 and NCI-H69 tumor bearing mice also demonstrate partial TGI (38% and 49% respectively) in response to GSK2879552, while no significant TGI is observed for SHP77 bearing mice.
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分子结构图
