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Merck
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資料

安全性情報

489479

Sigma-Aldrich

LSD1 Inhibitor IV, RN-1, 2HCl

LSD1 Inhibitor IV, RN-1, HCl, is a cell-permeable potent, irreversible inhibitor of lysine specific demethylase 1 (LSD1; IC₅₀ = 70 nM in a HRP-coupled assay using H3K4Me2 peptide substrate).

別名:

LSD1 Inhibitor IV, RN-1, 2HCl, LSD Inhibitor IV, Histone Lysine Demethylase Inhibitor VI, MOA Inhibitor III, 2-(1R,2S)-2-(4-(Benzyloxy)phenyl)cyclopropylamino)-1-(4-methylpiperazin-1-yl)ethanone, HCl, BHC110 Inhibitor IV, KDM1 Inhibitor IV, LSD Inhibitor IV, KDM1 Inhibitor IV, Histone Lysine Demethylase Inhibitor VI, MOA Inhibitor III, 2-(1R,2S)-2-(4-(Benzyloxy)phenyl)cyclopropylamino)-1-(4-methylpiperazin-1-yl)ethanone, HCl, BHC110 Inhibitor IV

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About This Item

実験式(ヒル表記法):
C23H29N3O2 · 2HCl
分子量:
452.42
UNSPSCコード:
12352208
NACRES:
NA.28

品質水準

アッセイ

≥97% (HPLC)

形状

solid

メーカー/製品名

Calbiochem®

保管条件

OK to freeze
desiccated (hygroscopic)
protect from light

yellow

溶解性

DMSO: 2.5 mg/mL
water: 2.5 mg/mL

輸送温度

wet ice

保管温度

−20°C

詳細

A cell-permeable tranylcypromine (parnate; Cat. No. 616431) analog that acts as a potent, irreversible inhibitor of lysine specific demethylase 1 (LSD1; IC50 = 70 nM in a HRP-coupled assay using H3K4Me2 peptide substrate). Forms a covalent adduct with flavin adenine dinucleotide (FAD). Shown to cross the blood brain barrier. Exhibits moderate selectivity over amine oxidases MAO-A and MAO-B (IC50 = 0.51 and 2.785 µM, respectively). Displays desirable pharmacokinetic properties (brain/plasma exposure ratio of 88.9), and impairs long-term memory without affecting short-term memory in mice (10 mg/kg, i.p.).
A cell-permeable tranylcypromine (parnate; Cat. No. 616431) analog that acts as a potent, irreversible inhibitor of lysine specific demethylase 1 (LSD1; IC50 = 70 nM in a HRP-coupled assay using H3K4Me2 peptide substrate). Forms a covalent adduct with flavin adenine dinucleotide (FAD). Shown to cross the blood brain barrier. Exhibits moderate selectivity over amine oxidases MAO-A and MAO-B (IC50 = 0.51 and 2.785 µM, respectively). Displays desirable pharmacokinetic properties (brain/plasma exposure ratio of 88.9), and impairs long-term memory without affecting short-term memory in mice (10 mg/kg, i.p.).

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

その他情報

Neelamegam, R., et al. 2011. ACS Chem. Neurosci.3, 120.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

保管分類コード

11 - Combustible Solids

WGK

WGK 2

引火点(°F)

Not applicable

引火点(℃)

Not applicable


適用法令

試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。

Jan Code

489479-1GM:
489479-0GM:
489479-10MG:
489479-MG:


試験成績書(COA)

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文書ライブラリにアクセスする

Ramesh Neelamegam et al.
ACS chemical neuroscience, 3(2), 120-128 (2012-07-04)
Modulation of histone modifications in the brain may represent a new mechanism for brain disorder therapy. Post-translational modifications of histones regulate gene expression, affecting major cellular processes such as proliferation, differentiation, and function. An important enzyme involved in one of
Brennan D Johnson et al.
ACS bio & med chem Au, 2(2), 161-170 (2022-07-28)
The flavin adenine dinucleotide containing Endoplasmic Reticulum Oxidoreductase-1 α (ERO1α) catalyzes the formation of de novo disulfide bond formation of secretory and transmembrane proteins and contributes towards proper protein folding. Recently, increased ERO1α expression has been shown to contribute to
Xiaoying Zhou et al.
Frontiers in cell and developmental biology, 10, 861916-861916 (2022-08-09)
Commensal microbes cross talk with their colonized mucosa. We show that microbes and their cell wall components induce an inflammatory response in cultured human mucosal cells derived from the nonmalignant nasopharyngeal epithelium (NNE) cells in vitro. NNE cells show significant
Cellular population dynamics shape the route to human pluripotency.
Panariello, et al.
Nature Communications, 14, 2829-2829 (2023)
Amanda Holley et al.
Physiology & behavior, 196, 78-83 (2018-08-24)
Although female rats are typically described as having a promiscuous mating strategy, if sexually naïve females have their formative sexually rewarding experiences paired with the same male, they will recognize that male and display mate-guarding behavior towards him in the

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