|N-((1R,2S)-2-苯基环丙基)哌啶-4-胺二盐酸盐|CsnPharm

CAS No.: 1821798-25-7

N-((1R,2S)-2-Phenylcyclopropyl)piperidin-4-amine dihydrochloride Catalog No. CSN19201

Synonyms: GSK-LSD1 HCl;GSK-LSD1

GSK-LSD1 2HCl is a selective LSD1 inhibitor with IC50 of 16 nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 KDM1A

IC50:16nM
描述Lysine specific demethylase 1 (LSD1) is a histone demethylase involved in embryonic stem cell differentiation and hematopoiesis. GSK-LSD1 dihydrochloride is an irreversible inhibitor of LSD1 with an IC50 value of 16nM. It displays > 1000-fold selectivity over LSD2, monoamine oxidase A and monoamine oxidase B. GSK-LSD1 was able to regulate gene expression in cancer cell lines with an average EC50 of < 5nM. It also inhibited cancer cell line growth with an average EC50 of < 5nM.^[2] The inhibition of histone H3K4 demethylase KDM1A/LSD1 by GSK-LSD1 (200μM for 12 hours) induced autophagy in U2OS cells.^[3]
作用机制GSK-LSD1 dihydrochloride is a potent, selective, irreversible inhibitor of LSD1.^[2]
参考文献

[1] Alsaqer SF, Tashkandi MM, et al. Inhibition of LSD1 epigenetically attenuates oral cancer growth and metastasis. Oncotarget. 2017 Jul 27;8(43):73372-73386.
[2] GSK-LSD1 A chemical probe for LSD1
[3] Wang Z, Long QY, Chen L, Fan JD, Wang ZN, Li LY, Wu M, Chen X. Inhibition of H3K4 demethylation induces autophagy in cancer cell lines. Biochim Biophys Acta Mol Cell Res. 2017 Dec;1864(12):2428-2437

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.4573 mL
- 17.2864 mL
- 34.5729 mL
- 5 mM
- 0.6915 mL
- 3.4573 mL
- 6.9146 mL
- 10 mM
- 0.3457 mL
- 1.7286 mL
- 3.4573 mL

技术信息

CAS号

1821798-25-7

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H22Cl2N2

运输

蓝冰

分子量

289.24

别名

GSK-LSD1 HCl;GSK-LSD1

溶解度

DMSO	55.0 mg/mL (190.2 mM) warming

动物实验配方

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N-((1R,2S)-2-Phenylcyclopropyl)piperidin-4-amine dihydrochloride Catalog No. CSN19201

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