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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 | Availability | Quantity |
---|---|---|---|
1 mg | $30 | In Stock | |
5 mg | $65 | In Stock | |
10 mg | $94 | In Stock | |
25 mg | $156 | In Stock | |
50 mg | $229 | In Stock | |
100 mg | $343 | 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 | Shipping with blue ice. |
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