Home Epigenetics Histone Demethylase inhibitor - LSD1 inhibitor GSK-LSD1 2HCl For research use only.

GSK-LSD1 2HCl

GSK-LSD1 2HCl is an irreversible, and selective LSD1 inhibitor with IC50 of 16 nM, > 1000 fold selective over other closely related FAD utilizing enzymes (i.e. LSD2, MAO-A, MAO-B).

GSK-LSD1 2HCl Chemical Structure

GSK-LSD1 2HCl Chemical Structure

CAS No. 2102933-95-7

Purity & Quality Control

Batch: S757401 DMSO]57 mg/mL]false]Water]57 mg/mL]false]]]false Purity: 99.78%
99.78

GSK-LSD1 2HCl Related Products

Signaling Pathway

Histone Demethylase Signaling Pathways

Histone Demethylase Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A549 Function assay 10 uM 1 hr Binding affinity to LSD1 in human A549 cells assessed as increase in stability of cellular LSD1 protein at 10 uM pre-incubated for 1 hr followed by heating at 49 degC for 3 mins by Western blot-based CESTA 30780087
A549 Function assay 10 uM 1 hr Binding affinity to LSD1 in human A549 cells assessed as increase in stability of cellular LSD1 protein at 10 uM pre-incubated for 1 hr followed by heating at 52 degC for 3 mins by Western blot-based CESTA 30780087
A549 Function assay 96 hrs Down regulation of snail levels in human A549 cells up to 16 uM after 96 hrs by Western blot analysis 30780087
A549 Function assay 96 hrs Down regulation of N-cadherin levels in human A549 cells up to 16 uM after 96 hrs by Western blot analysis 30780087
A549 Function assay 96 hrs Down regulation of slug levels in human A549 cells up to 16 uM after 96 hrs by Western blot analysis 30780087
A549 Function assay 96 hrs Up regulation of claudin-1 levels in human A549 cells up to 16 uM after 96 hrs by Western blot analysis 30780087
A549 Function assay 96 hrs Up regulation of E-cadherin levels in human A549 cells up to 16 uM after 96 hrs by Western blot analysis 30780087
THP1 Function assay 4 uM 3 days Inhibition of LSD1 in human THP1 cells assessed as increase in CD86 expression at 4 uM incubated for 3 days by flow cytometric analysis 31096156
Click to View More Cell Line Experimental Data

Biological Activity

Description GSK-LSD1 2HCl is an irreversible, and selective LSD1 inhibitor with IC50 of 16 nM, > 1000 fold selective over other closely related FAD utilizing enzymes (i.e. LSD2, MAO-A, MAO-B).
Targets
LSD1 [1]
(Cell-free assay)
16 nM
In vitro
In vitro

GSK-LSD1 induces gene expression changes in cancer cell lines with average EC50 of < 5 nM and inhibits cancer cell line growth with average EC50 of < 5 nM. [1]
Cell Research Cell lines U2OS cells
Concentrations 200 μM
Incubation Time 12 h
Method

Cells were treated with indicated concentration of drug for 12 h.
Experimental Result Images Methods Biomarkers Images PMID
Western blot LSD1 / H3K4me2 29088714
In Vivo
In vivo

GSK-LSD1, a highly selective inhibitor of KDM1A, significantly inhibits thyroid cancer progression and enhances the sensitivity of thyroid cancer to chemotherapy.

Chemical Information & Solubility

Molecular Weight 289.24 Formula

C14H22Cl2N2
CAS No. 2102933-95-7 SDF Download GSK-LSD1 2HCl SDF
Smiles C1CNCCC1NC2CC2C3=CC=CC=C3.Cl.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 57 mg/mL ( (197.06 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 57 mg/mL


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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