性能参数

产品名称

RN-1 (hydrochloride)

规格

1mg  5mg 10mg

货号

GOY-Y3629

 含量

>98.00%

CAS

1781835-13-9

别名

LSD1 Inhibitor IV

化学名

RN-1, monohydrochloride

分子式

C23H29N3O2 ? 2HCl

分子量

分子量 452.4

溶解度

≤0.3mg/ml in DMSO

储存条件

Store at -20°C

General tips

用途

仅供科研

价格

电询

详细内容

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].

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