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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).

Synonym(s):

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

Empirical Formula (Hill Notation):
C23H29N3O2 · 2HCl
Molecular Weight:
452.42
UNSPSC Code:
12352208
NACRES:
NA.28

Quality Level

200

Assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)
protect from light

color

yellow

solubility

DMSO: 2.5 mg/mL
water: 2.5 mg/mL

shipped in

wet ice

storage temp.

−20°C

General description

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.).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 2

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Listings

Regulatory Listings are mainly provided for chemical products. Only limited information can be provided here for non-chemical products. No entry means none of the components are listed. It is the user’s obligation to ensure the safe and legal use of the product.

JAN Code

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

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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
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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
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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
Cellular population dynamics shape the route to human pluripotency.
Panariello, et al.
Nature Communications, 14, 2829-2829 (2023)

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