-
Alternative_name
N-((1R,2S)-2-phenylcyclopropyl)piperidin-4-amine dihydrochloride
-
Description
GSK-LSD1 is a potent and selective inhibitor of lysine specific demethylase 1 (LSD1). GSK-LSD1 2HCl irreversibly inhibits LSD1 with IC₅₀ value of 16 nM and is > 1000 fold selective over LSD2, MAO-A and MAO-B, which were related to FAD utilizing enzymes. GSK-LSD1 potently inhibits proliferation of varies cancer cell lines by changing gene expression patterns.
-
CAS Number
1431368-48-7 (free base)
-
Structure Available
Yes
-
Salt Form
No
-
Molecular Formula
C14H22Cl2N2
-
Molecular Weight
289.24
-
Cell Permeable
Yes
-
Purity
≥98% by HPLC
-
Solubilities
H₂O (>20 mg/ml)
-
Handling
Protect from air and moisture
-
Tag Line
A potent and selective lysine specific demethylase 1 (LSD1)inhibitor
-
Storage Condition
-20°C
-
Shipping Condition
gel pack
-
Shelf Life
36 months
-
PubChem CID
71522234
-
-
SMILES
C1CNCCC1NC2CC2C3=CC=CC=C3
-
InChi
InChI=1S/C14H20N2/c1-2-4-11(5-3-1)13-10-14(13)16-12-6-8-15-9-7-12/h1-5,12-16H,6-10H2/t13-,14+/m0/s1
-
InChi Key
BASFYRLYJAZPPL-UONOGXRCSA-N
-
-
MSDS Available
Yes
-
Gene
Lysine-specific demethylase 1 (LSD1), the first identified histone demethylase, was belonged to the superfamily of the Flavin adenine dinucleotide (FAD)-dependent amine oxidases. LSD1 specifically demethylates mono- or dimethylated dimethylated histone H3 lysine4 (H3K4) and H3 lysine 9 (H3K9) via a redox process. Recently evidences showed that LSD1 played an important role in a broad spectrum of biological processes, including cell proliferation, adipogenesis, spermatogenesis, chromosome segregation and embryonic development. Furthermore, LSD1 also could promote progress of tumor by inhibiting the tumor suppressor activity of p53. To date, as a potential drug for discovering anti-tumor drugs, the medical significance of LSD1 inhibitors have been greatly appreciated. Here, we reviewed the remarkable progress being made in understanding of LSD1, mainly on its structure, basic function and medical application in tumor therapy.
