RN-1 (hydrochloride)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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:
[1]. Neelamegam R, Ricq EL, Malvaez M, et al. Brain-penetrant LSD1 inhibitors can block memory consolidation. ACS Chem Neurosci. 2012 Feb 15;3(2):120-128.
[2]. Shi Y, Lan F, Matson C, et al. Histone demethylation mediated by the nuclear amine oxidase homolog LSD1. Cell. 2004 Dec 29;119(7):941-53.
[3]. Konovalov S, Garcia-Bassets I. Analysis of the levels of lysine-specific demethylase 1 (LSD1) mRNA in human ovarian tumors and the effects of chemical LSD1 inhibitors in ovarian cancer cell lines. J Ovarian Res. 2013 Oct 29;6(1):75.
[4]. 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 Jul 16;126(3):386-96.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 452.4 |
Cas No. | 1781835-13-9 |
Formula | C23H29N3O2·2HCl |
Synonyms | LSD1 Inhibitor IV |
Solubility | insoluble in EtOH; ≥2.7 mg/mL in DMSO with ultrasonic; ≥8.47 mg/mL in H2O |
Chemical Name | RN-1, monohydrochloride |
SDF | Download SDF |
Canonical SMILES | CN1CCN(C(CN[C@@H]2[C@@H](C3=CC=C(OCC4=CC=CC=C4)C=C3)C2)=O)CC1.Cl.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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