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GSK-LSD1 (hydrochloride)

Catalog No.
C4202
LSD1 inhibitor
Grouped product items
SizePriceStock Qty
5mg
$91.00
Ship with 5-10 days
10mg
$165.00
Ship with 5-10 days
25mg
$371.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

GSK-LSD1 (hydrochloride) is a potent, irreversible and mechanism-based inhibitor of LSD1 [1].

Lysine specific demethylase 1 (LSD1) is a histone H3K4me1/2 demethylase existed in many transcriptional co-repressor complexes. LSD1 mediates H3K4 demethylation, causes a repressive chromatin environment which results in gene expression silence and has been shown to play a role in hematopoietic differentiation. It has been demonstrated that LSD1 is overexpressed in multiple tumor types [2].

In vitro: GSK-LSD1 inhibited the activity of LSD1 with an IC50 of 16 nM that is >1,000-fold selective over the closely related FAD-utilizing enzymes, such as LSD2, MAO-A, and MAO-B. GSK-LSD1 inhibited cell proliferation by inducing gene expression changes in various cancer cell lines, the EC50s were < 5 nM [1].

In vivo: In mice bearing LX44 or LX48, daily treatment with 1.5 mg/kg GSK-LSD1 showed 69% and 74% TGI, respectively [3].

References:
[1] Epigenetics probes collection.  (2014).
[2] Smitheman K, Cusan M, Liu Y, et al.  Inhibition of LSD1 for the treatment of cancer[J]. 2015.
[3] Mohammad H P, Smitheman K N, Kamat C D, et al.  A DNA hypomethylation signature predicts antitumor activity of LSD1 inhibitors in SCLC[J]. Cancer Cell, 2015, 28(1): 57-69.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt289.2
FormulaC14H20N2·2HCl
Solubility≤0.1mg/ml in ethanol;25mg/ml in DMSO;1mg/ml in dimethyl formamide
Chemical NameN-[(1R,2S)-2-phenylcyclopropyl]-4-piperidinamine, dihydrochloride
SDFDownload SDF
Canonical SMILES[[email protected]]1(C2=CC=CC=C2)[[email protected]](NC3CCNCC3)C1.Cl.Cl
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

GSK-LSD1 (hydrochloride)