| CAS NO: | 1781835-13-9 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| Cas No. | 1781835-13-9 |
| 别名 | LSD1 Inhibitor IV |
| 化学名 | RN-1, monohydrochloride |
| Canonical SMILES | CN1CCN(C(CN[C@@H]2[C@@H](C3=CC=C(OCC4=CC=CC=C4)C=C3)C2)=O)CC1.Cl.Cl |
| 分子式 | C23H29N3O2o 2HCl |
| 分子量 | 452.4 |
| 溶解度 | ≤0.3mg/ml in DMSO |
| 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 | RN-1 (hydrochloride) is a brain-penetrant, potent and irreversible LSD1 inhibitor with IC50 values of 10-70 nM [1]. Lysine-specific demethylase 1 (LSD1) is a flavin-dependent monoamine oxidase that demethylate mono- and di-methylated lysines, specifically histone 3, lysines 4 and 9 (H3K4 and H3K9) [2]. RN-1 (hydrochloride) is a potent and irreversible LSD1 inhibitor with IC50 values of 10-70 nM. However, RN-1 is much less effective against MAO-A and MAO-B with IC50 values of 0.51 and 2.785 μM, respectively [1]. In ovarian cancer lines, RN-1 also induced cytotoxicity, which was correlated with the LSD1 inhibitory potential [3]. Following intraperitoneal administration in mice, RN-1 penetrated the blood-brain barrier and the brain/plasma exposure ratio was 88.9. In mice, RN-1 significantly impaired long-term memory but not short-term memory. And long-term memory impairment was due to a brain-specific effect [1]. In a sickle cell disease (SCD) mouse model, RN-1 induced HbF synthesis and increased frequencies of HbF-positive cells and mature erythrocytes, as well as reduced reticulocytes and sickle cells. And the RN-1 treated mice did not exhibit the necrotic lesions in the liver and spleen [4]. References: |
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