| CAS NO: | 2102933-95-7 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Cas No. | 2102933-95-7 |
| 化学名 | N-[(1R,2S)-2-phenylcyclopropyl]-4-piperidinamine, dihydrochloride |
| Canonical SMILES | [C@H]1(C2=CC=CC=C2)[C@H](NC3CCNCC3)C1.Cl.Cl |
| 分子式 | C14H20N2o 2HCl |
| 分子量 | 289.2 |
| 溶解度 | ≤0.1mg/ml in ethanol;25mg/ml in DMSO;1mg/ml in dimethyl formamide |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | GSK-LSD1 (hydrochloride) is a potent, irreversible and mechanism-based inhibitor of LSD1 [1]. Lysine specific demethylase 1 (LSD1) is a histone H3K4me1/2 demethylase existed in many transcriptional co-repressor complexes. LSD1 mediates H3K4 demethylation, causes a repressive chromatin environment which results in gene expression silence and has been shown to play a role in hematopoietic differentiation. It has been demonstrated that LSD1 is overexpressed in multiple tumor types [2]. In vitro: GSK-LSD1 inhibited the activity of LSD1 with an IC50 of 16 nM that is >1,000-fold selective over the closely related FAD-utilizing enzymes, such as LSD2, MAO-A, and MAO-B. GSK-LSD1 inhibited cell proliferation by inducing gene expression changes in various cancer cell lines, the EC50s were< 5 nM [1]. In vivo: In mice bearing LX44 or LX48, daily treatment with 1.5 mg/kg GSK-LSD1 showed 69% and 74% TGI, respectively [3]. References: |
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