| Name | GSK-LSD1 |
| 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] |
| Storage | Powder: -20°C for 3 years | 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)
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| Keywords | LSD1 | HistoneDemethylase | Histone Demethylase | Apoptosis |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Formamide | Dimethyl phthalate | Alginic acid | Sodium Molybdate | Sildenafil citrate |
| Related Compound Libraries | Apoptosis Compound Library | Histone Modification Compound Library | Bioactive Compound Library | Epigenetics Compound Library | Anti-Breast Cancer Compound Library | Post-Translational Modification Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
