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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $30 | In Stock | In Stock | |
| 5 mg | $65 | In Stock | In Stock | |
| 10 mg | $94 | In Stock | In Stock | |
| 25 mg | $156 | In Stock | In Stock | |
| 50 mg | $229 | In Stock | In Stock | |
| 100 mg | $343 | In Stock | In Stock |
| 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] |
| Molecular Weight | 216.32 |
| Formula | C14H20N2 |
| Cas No. | 1431368-48-7 |
| Smiles | N([C@H]1[C@@H](C1)C2=CC=CC=C2)C3CCNCC3 |
| Storage | In 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
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Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
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 ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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