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RN 1 dihydrochloride
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
RN 1 dihydrochloride图片
CAS NO:1781835-13-9
包装与价格：
包装价格(元)
10mg电议
50mg电议

产品介绍
RN 1 dihydrochloride 是一种有效的、脑渗透性的、不可逆的和选择性的赖氨酸特异性去甲基化酶 1 (LSD1) 抑制剂，IC50 为 70 nM。
Cas No.1781835-13-9
化学名2-(((1R,2S)-2-(4-(benzyloxy)phenyl)cyclopropyl)amino)-1-(4-methylpiperazin-1-yl)ethanone dihydrochloride
Canonical SMILESCN1CCN(C(CN[C@]2([H])C[C@@]2([H])C3=CC=C(OCC4=CC=CC=C4)C=C3)=O)CC1.Cl.Cl
分子式C23H29N3O2.2HCl
分子量452.42
溶解度<9.05mg/ml in Water;<9.05mg/ml in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

RN 1 dihydrochloride is a potent and selective inhibitor of LSD1 with IC50 value of 70 nM [1].

Lysine (K) -specific demethylase 1A (LSD1) is a flavin-dependent histone demethylase that demethylates mono- and di-methylated lysines and plays an important role in oocyte growth, embryogenesis and tissue-specific differentiation. LSD1 plays a role in acute myeloid leukemia (AML).

RN 1 dihydrochloride is a potent and selective LSD1 inhibitor. RN-1 inhibited monoamine oxidase MAO A and MAO B with IC50 values of 0.51 and 2.79 μM, respectively [1]. In baboon erythroid progenitor cells, RN-1 increased γ-globin expression [2].

In mice, RN-1 significantly impairs long-term memory but didn’t affect short-term memory [1]. In sickle cell disease (SCD) mice, RN-1 induced the expression of γ-globin and increased amounts of F cells and F reticulocytes [2]. In SCD mouse model, RN-1 induced HbF synthesis and increased amounts of mature erythrocytes and HbF-positive cells. Also, RN-1 reduced sickle cells and reticulocytes in the peripheral blood [3].

References:
[1].  Neelamegam R, Ricq EL, Malvaez M, et al. Brain-penetrant LSD1 inhibitors can block memory consolidation. ACS Chem Neurosci, 2012, 3(2): 120-128.
[2].  Rivers A, Vaitkus K, Ruiz MA, et al. RN-1, a potent and selective lysine-specific demethylase 1 inhibitor, increases γ-globin expression, F reticulocytes, and F cells in a sickle cell disease mouse model. Exp Hematol, 2015, 43(7): 546-553.e3.
[3].  Cui S, Lim KC, Shi L, et al. The LSD1 inhibitor RN-1 induces fetal hemoglobin synthesis and reduces disease pathology in sickle cell mice. Blood, 2015, pii: blood-2015-02-626259.