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GSK-LSD1

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

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 SizePriceAvailabilityQuantity
1 mg$30In Stock
5 mg$65In Stock
10 mg$94In Stock
25 mg$156In Stock
50 mg$229In Stock
100 mg$343In Stock
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Purity:99.59%
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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
Storage & Solubility Information
StorageShipping with blue ice.

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