Bkm120

Manufactured by Merck Group

Sourced in United States

BKM120 is a lab equipment product manufactured by Merck Group. It is a PI3K inhibitor compound primarily used for research purposes in biochemical and cell-based assays. The core function of BKM120 is to inhibit the activity of the phosphoinositide 3-kinase (PI3K) enzyme, which plays a role in cellular signaling pathways.

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Lab products found in correlation

6 protocols using bkm120

Targeting PI3K/Akt Pathway in Glioma Cells

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TMZ was supplied by Tasly Pharmaceutical Co., Ltd. (Tianjin, China). The PI3K inhibitor, BKM120, was purchased from Sigma-Aldrich (Merck KGaA, Darmstadt, Germany). Stock solutions of TMZ and BKM120 (TMZ, 120 mM; BKM120, 3 mM) were made by dissolving in dimethyl sulfoxide (DMSO; Sigma-Aldrich; Merck KGaA). For TMZ treatment solutions, the DMSO concentrations were limited to <1% (v/v), and the vehicle controls were added at the same concentration as DMSO. The terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) assay cell death kit was purchased from Roche Diagnostics (Indianapolis, IN, USA). The Cell Counting Kit-8 (CCK-8) and Hoechst 33342 were supplied by Beyotime Institute of Biotechnology (Haimen, China). All primary antibodies were purchased from Cell Signaling Technology, Inc. (Danvers, MA, USA), including rabbit anti-rat antibodies against PI3K (cat. no. 4257, 1:1,000 dilution), phosphorylated (p)-Akt (Ser⁴⁷³) (cat. no. 4060, 1:1,000 dilution), NF-κB p65 (cat. no. 3033, 1:1,000 dilution), pS6 (cat. no. 2215S, 1:1,000 dilution), cleaved caspase-3 (cat. no. 9664, 1:1,000 dilution), Bax (cat. no. 14796, 1:1,000 dilution) and GAPDH (cat. no. 5174, 1:1,000 dilution,), and goat anti-rabbit horseradish peroxidase (HRP)-conjugated immunoglobulin G (IgG) secondary antibody (cat. no. 31460, 1:1,000 dilution; Pierce; Thermo Fisher Scientific, Inc.).

Li M., Liang R.F., Wang X., Mao Q, & Liu Y.H. (2017). BKM120 sensitizes C6 glioma cells to temozolomide via suppression of the PI3K/Akt/NF-κB/MGMT signaling pathway. Oncology Letters, 14(6), 6597-6603.

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Investigating BKM120's Effects on Gastric Cancer

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BKM120, a pan-class I PI3K inhibitor, was purchased from Sigma-Aldrich (Saint-Quentin Fallavier, France). For the in vitro experiments, BKM120 was prepared as 10 mmol/L stock solution in DMSO and conserved at −20 °C for ≤2 months. Adherent cultured cells were treated for 48 h to 72 h one day after seeding with a medium change. Three-dimensional cultured cells were treated during the seeding of the cells to analyze tumorsphere formation. Tumorspheres were treated 4 days after seeding to analyze CD44 expression. For the in vivo experiments, BKM120 was dissolved in 10% NMP (1-methyl-2-pyrrolidone) and 90% PEG300 (all from Sigma-Aldrich). Vehicle treatment consisted of a solution containing 10% NMP and 90% PEG300. Solution was administrated by oral gavage at 20 mg/kg once per day on a schedule of five days on, two days off schedule for three weeks. The GC10 PDX cell and MKN45 gastric cancer cell lines treated with BKM120 were PIK3CA wild-type.

Giraud J., Bouriez D., Seeneevassen L., Rousseau B., Sifré E., Giese A., Mégraud F., Lehours P., Dubus P., Gronnier C, & Varon C. (2019). Orthotopic Patient-Derived Xenografts of Gastric Cancer to Decipher Drugs Effects on Cancer Stem Cells and Metastatic Dissemination. Cancers, 11(4), 560.

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Signaling Pathway Antibodies and Inhibitors

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PREX1 [D8O8D] rabbit monoclonal, PTEN [138G6] rabbit monoclonal, Phospho-PAK1 (Ser144)/PAK2 (Ser141) rabbit polyclonal, PAK2 [3B5] mouse monoclonal were purchased from Cell Signaling (Danvers, MA, USA). GAPDH [6C5] mouse monoclonal and CDC42 [M152] mouse monoclonal were purchased from Abcam (Cambridge, MA, USA). Phospho-PKCι (T555)/PKCλ (T563) rabbit polyclonal was purchased from Invitrogen (Carlsbad, CA, USA) and PKCι mouse monoclonal from (BD Transduction Laboratories (Mississauga, ON, Canada). Sox2 mouse monoclonal was from R&D Systems (Minneapolis MN, USA). Rac1[23A8] mouse monoclonal, anti-Flag M2 mouse monoclonal and Stem121 mouse monoclonal were purchased from Millipore (Temecula, CA, USA), Sigma-Aldrich (Oakville, ON, Canada) and StemCells Inc. (Newark, CA, USA), respectively. Human brain cerebral cortex protein medley was purchased from Clontech (Mountain View, CA, USA). The following inhibitors were used in the study: gallein (Santa Cruz Biotechnology, CA, USA), BKM120 (Sigma-Aldrich, Oakville, ON, Canada); trichostatin A (Cayman Chemical Company, Ann Arbor, MI, USA); haloperidol, L-741,626 and L-745,870 (Tocris Bioscience, Minneapolis, MN, USA).

Gont A., Daneshmand M., Woulfe J., Lavictoire S.J, & Lorimer I.A. (2016). PREX1 integrates G protein-coupled receptor and phosphoinositide 3-kinase signaling to promote glioblastoma invasion. Oncotarget, 8(5), 8559-8573.

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Evaluating Combination Inhibitor Efficacy

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H1975, H460, and A549 cells were treated with 0–3 μM MEK162 (MEK inhibitor, Sigma, St. Louis, MO, USA) or 0–15 μM BKM120 (PI3K inhibitor, Sigma), alone or in combination for 48 h. H1975, H460, and A549 cells were treated with 1 μM BIBW2992 (EGFR inhibitor, Sigma), a second-generation EGFR-TKI, or 2 μM ARQ197 (MET inhibitor, Sigma) combination for 48 h. A stock solution of the chemical inhibitors was prepared in 100% DMSO and further diluted with normal saline. The inhibitors were used at a final concentration of 0.05% DMSO.

Qu G.P., Shi M., Wang D., Wu J.H., Wang P., Gong M.L, & Zhang Z.J. (2021). Dual targeting of MEK and PI3K effectively controls the proliferation of human EGFR-TKI resistant non-small cell lung carcinoma cell lines with different genetic backgrounds. BMC Pulmonary Medicine, 21, 208.

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Evaluating Efficacy of Targeted Therapies

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NVP-BEZ235 (BEZ235), NVP-BKM120 (Buparlisib, BKM120), GSK1120212 (Trametinib, JTP-74057), PD0325901, and AZD6244 were purchased from Chemie Tek (Indianapolis, IN). Temozolomide, doxorubicin and paclitaxel were purchased from Sigma. For in vivo studies, BEZ235 and BKM120 were resuspended in NMP (N-methyl-2-pyrrolidone):PEG300 1:9 v:v, and GSK1120212 and PD0325901 were resuspended in 0.5% hydroxypropyl-methylcellulose (Sigma):0.2% Tween 80 (Sigma) (Gilmartin et al., 2011 (link); Kinross et al., 2011 (link)). BKM120, GSK1120212 and PD0325901 were given once daily by oral gavage at 10 ml/kg. Mice were treated with BEZ235 on a 5 days on, 2 days off schedule (Liu et al., 2009 (link)). Vehicle- and drug-treated mice were closely monitored on a daily basis for clinical signs as described above.

El Meskini R., Iacovelli A.J., Kulaga A., Gumprecht M., Martin P.L., Baran M., Householder D.B., Van Dyke T, & Weaver Ohler Z. (2014). A preclinical orthotopic model for glioblastoma recapitulates key features of human tumors and demonstrates sensitivity to a combination of MEK and PI3K pathway inhibitors. Disease Models & Mechanisms, 8(1), 45-56.

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Investigating Pak1/2 Signaling Regulation

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Antibodies were purchased from the following suppliers: Cell Signaling Technologies (Danvers, MA, USA) (phospho Pak1 S199/204Pak2 S192/197-2605, phospho-Pak1 T423/Pak2 T402-2601, Pak1-2602, Rac1/2/3-2465, phospho Akt Thr308-4056, Akt1-2938) Abcam (Cambridge, MA, USA) (βactin-ab7817) and Santa Cruz Biotech. (Santa Cruz, CA, USA) (ALT1-S374501, ALT2-398383). Inhibitors and metabolites were purchased from Selleck Chemicals (Houston, TX, USA) (BKM120), Sigma-Aldrich (St. Louis, MO, USA) (EIPA, L-cycloserine, L-alanine, pyruvate), and Santa Cruz Biotech. (EHT 1864). PAK1 T423E cDNA was obtained from pCMV6M-PAK1 T423E, a gift from Jonathan Chernoff purchased from Addgene (Addgene plasmid #12208, Watertown, MA, USA). The PAK1 T423E cDNA was sub-cloned into the retroviral vector pBABE-puro for stable expression via retroviral infection.

Hodakoski C., Hopkins B.D., Zhang G., Su T., Cheng Z., Morris R., Rhee K.Y., Goncalves M.D, & Cantley L.C. (2019). Rac-Mediated Macropinocytosis of Extracellular Protein Promotes Glucose Independence in Non-Small Cell Lung Cancer. Cancers, 11(1), 37.

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