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GSK-LSD1

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Catalog No. T82254Cas No. 1431368-48-7

GSK-LSD1 is a selective LSD1 inhibitor with potential anticancer activity that attenuates the expression of CTGF/CCN2, MMP13, LOXL4, and waveform proteins in cancer cells.GSK-LSD1 regulates the cell cycle, induces apoptosis, and can be used to study breast cancer.

GSK-LSD1

GSK-LSD1

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Purity: 99.59%
Catalog No. T82254Cas No. 1431368-48-7
GSK-LSD1 is a selective LSD1 inhibitor with potential anticancer activity that attenuates the expression of CTGF/CCN2, MMP13, LOXL4, and waveform proteins in cancer cells.GSK-LSD1 regulates the cell cycle, induces apoptosis, and can be used to study breast cancer.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$30In StockIn Stock
5 mg$65In StockIn Stock
10 mg$94In StockIn Stock
25 mg$156In StockIn Stock
50 mg$229In StockIn Stock
100 mg$343In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.59%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
GSK-LSD1 is a selective LSD1 inhibitor with potential anticancer activity that attenuates the expression of CTGF/CCN2, MMP13, LOXL4, and waveform proteins in cancer cells.GSK-LSD1 regulates the cell cycle, induces apoptosis, and can be used to study breast cancer.
In vitro
METHODS: LDH activity was measured at 24 and 48 h in HSC-3 cells treated with different concentrations of GSK-LSD1 (0.1, 1, 10 μM). To assess the cytotoxicity and any nonspecific effects of GSK-LSD1, a lactate dehydrogenase (LDH) assay was performed.
RESULTS: The 0.1 μM and 1 μM doses did not affect LDH release. However, the 10 μM dose increased LDH activity at 48 h. GSK-LSD1 inhibited phosphorylated AKT, -ERK1/2, and -NF-κB-p65 in HSC-3 cells. [3]
In vivo
METHODS: A PDX model was established. GSK-LSD1 (10 mg/kg) was injected into mice with xenografts grown for 16 weeks every two weeks, and the growth of tumors and the expression of related proteins in the mice were observed.
RESULTS: GSK-LSD1 inhibited further xenograft growth; GSK-LSD1 inhibited the expression of CCN2/CTGF, MMP13, LOXL4 and vimentin in tumor xenografts derived from patients with tonsillar squamous cell carcinoma, while the expression of the tumor suppressor E-cadherin was increased; in addition, GSK-LSD1 inhibited the expression of CTGF in PDXs. [3]
Chemical Properties
Molecular Weight216.32
FormulaC14H20N2
Cas No.1431368-48-7
SmilesN([C@H]1[C@@H](C1)C2=CC=CC=C2)C3CCNCC3
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 13.78 mg/mL (63.7 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM4.6228 mL23.1139 mL46.2278 mL231.1391 mL
5 mM0.9246 mL4.6228 mL9.2456 mL46.2278 mL
10 mM0.4623 mL2.3114 mL4.6228 mL23.1139 mL
20 mM0.2311 mL1.1557 mL2.3114 mL11.5570 mL
50 mM0.0925 mL0.4623 mL0.9246 mL4.6228 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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