Gsk lsd1

Manufactured by Selleck Chemicals

Sourced in United States

GSK-LSD1 is a selective inhibitor of the LSD1 (Lysine-specific demethylase 1) enzyme. LSD1 is an epigenetic regulator that plays a role in the modulation of gene expression. GSK-LSD1 is a tool compound used in research to study the biological functions of LSD1.

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GSK-LSD1 2HCL (4 citations)

6 protocols using gsk lsd1

Multiple Myeloma Cell Lines and Compounds

Cited 2 times

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Cell lines (KMS11, OPM2, and ANBL6) were purchased from American Type Culture Collection (Manassas, VA, USA). MM.1S BzR cells were a gift from Dr. Brian Van Ness (U. of Minnesota) and have been described previously [25 (link)]. LTI6426 was provided by Leukogene Therapeutics, Inc. (Charleston, SC) with purity and identity that was confirmed by liquid chromatograph–mass spectrometry (LC–MS) and nuclear magnetic resonance (NMR) as shown previously [16 (link)]. Bortezomib (Catalog No. S1013), carfilzomib (Catalog No. S2853), panobinostat (Catalog No. S1030), vorinostat (Catalog No. S1047), ricolinostat (Catalog No. S8001), entinostat (Catalog No. S1053), romidepsin (Catalog No. S3020), tazmetostat (Catalog No. S7128), ML324 (Catalog No. S7296), JQ1 (Catalog No. S7110), OTX015 (Catalog No. S7360), ABBV744 (Catalog No. S8723), IBET151 (Catalog No. S2780), and GSK-LSD1 (Catalog No. S7574) were purchased from Selleck Chemicals (Houston, TX, USA).

Robinson R.M., Basar A.P., Reyes L., Duncan R.M., Li H, & Dolloff N.G. (2022). PDI inhibitor LTI6426 enhances panobinostat efficacy in preclinical models of multiple myeloma. Cancer Chemotherapy and Pharmacology, 89(5), 643-653.

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Modulating Endogenous RTase Activity in mESCs

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Small molecules, AZT (Sigma-Aldrich, 2169-25MG) and GSK-LSD1 (Selleck, S7574), were used to modulate the endogenous RTase activity in mESCs. To select the proper concentration for the subsequent experiments, mESCs were seeded in 96-well plates at a density of 20,000 cells/well and treated with drugs at different concentrations (0, 1, 5, 10, 50, 100, 200, 500, 1000 µM) for 24 h. Cell viability was tested by using Cell Counting Kit-8 (CCK-8, Bimake, B34302) as described previously.^{71 (link)} According to the results, mESCs were treated with AZT at 100 µM and GSK-LSD1 at 50 µM in the subsequent experiments.
One day before drug treatment, cells were seeded in 12-well plates at a density of 3 × 10⁵ cells/well. Then, cells were pre-treated with 100 µM AZT for 4–6 h or 50 µM GSK-LSD1 for 24 h, followed by virus infection and other experiments.

Wu J., Wu C., Xing F., Cao L., Zeng W., Guo L., Li P., Zhong Y., Jiang H., Luo M., Shi G., Bu L., Ji Y., Hou P., Peng H., Huang J., Li C, & Guo D. (2021). Endogenous reverse transcriptase and RNase H-mediated antiviral mechanism in embryonic stem cells. Cell Research, 31(9), 998-1010.

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Eupalinilide B Binds and Inhibits LSD1

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Eupalinilide B and LSD1 were incubated and dialyzed at 4°C for 24 hours. Then, the relative activity of LSD1 was measured to investigate the binding mode of eupalinilide B. GSK-LSD1 (Selleck Chemicals, Houston, TX, USA) was also selected as a LSD1 inhibitor to perform the dialysis experiment. Finally, the each tube was measured with a spectrophotometer (PerkinElmer).

Jiang L., Zhang L, & Zhang X. (2022). Eupalinilide B as a novel anti-cancer agent that inhibits proliferation and epithelial–mesenchymal transition in laryngeal cancer cells. The Journal of International Medical Research, 50(1), 03000605211067921.

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Cell Viability Assay with LSD1 Inhibitors

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Suspension cells were seeded at a density of 10,000 cells per well; adherent cells were plated at a density of 2,500 cells per well in a 96‐well plate. ORY‐1001 (S7795, Selleck Chemicals) and GSK‐LSD1 (S77574, Selleck Chemicals) were resuspended in DMSO and serially diluted with final concentrations ranging from 0.01 nM to 100 μM. Cells were treated in quadruplicates at indicated doses or DMSO for 6 days. Cell viability was read out with the CellTiter‐Glo^® 2.0 Cell Viability Assay (G9242, Promega) according to the manufacturer's instructions. IC50 curves were calculated with the software GraphPad PRISM 8 (non‐linear regression, log (inhibitor vs response—variable slope, four parameters)).

Leiendecker L., Jung P.S., Krecioch I., Neumann T., Schleiffer A., Mechtler K., Wiesner T, & Obenauf A.C. (2020). LSD1 inhibition induces differentiation and cell death in Merkel cell carcinoma. EMBO Molecular Medicine, 12(11), e12525.

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Modulating Retrotransposon Activity in BmN Cells

Cited 1 time

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Azidothymidine (AZT) is a widely used RT inhibitor that can inhibit endogenous RT activity (9 (link)). GSK-LSD1, an inhibitor of histone H3 lysine 9 (or histone H3 lysine 4) demethylases, has been reported to increase the methylation level of histone H3 lysine 9, thus increasing RT activity in mammalian cells. In this study, AZT (China, Absin, Cat: abs810874) and GSK-LSD1 (USA, Selleck, Cat: S7574) were used to modulate the retrotransposon activity of RT in BmN cells. MTT assays were carried out to determine the proper drug concentration for subsequent experiments. Briefly, 10³ BmN cells were seeded in 96-well plates and treated with different concentrations of AZT (0, 1, 5, 10, 25, 50, 100 mM) or GSK-LSD1 (0, 1, 5, 10, 25, 50, 100 nm) for 24 h. Cells viability was evaluated by MTT. According to MTT assay, BmN cells were treated with 5 mM AZT and/or 50 nM GSK-LSD1 in the subsequent experiments. Before further treatments, BmN cells were seeded in 6-well plates at the density of 1× 10⁶ cells/well and cultured for one day. Thereafter, cells were pretreated with 5 mM AZT for 4–6 h or 50 nM GSK-LSD1 for 24 h, followed by BmCPV infection and other downstream assays.

Zhu M., Pan J., Tong X., Qiu Q., Zhang X., Zhang Y., Sun S., Feng Y., Xue R., Cao G., Hu X, & Gong C. (2022). BmCPV-Derived Circular DNA vcDNA-S7 Mediated by Bombyx mori Reverse Transcriptase (RT) Regulates BmCPV Infection. Frontiers in Immunology, 13, 861007.

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Antibody and Chemical Reagents Protocol

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The antibodies used in this study are listed in Additional file 2.4. Doxorubicin, cycloheximide, MG132, DMOG and GSK-LSD1 were all purchased from Selleck Chemicals (Houston, TX, USA).

Zhang W., Ruan X., Li Y., Zhi J., Hu L., Hou X., Shi X., Wang X., Wang J., Ma W., Gu P., Zheng X, & Gao M. (2022). KDM1A promotes thyroid cancer progression and maintains stemness through the Wnt/β-catenin signaling pathway. Theranostics, 12(4), 1500-1517.

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