Bkm120

Manufactured by MedChemExpress

Sourced in China

BKM120 is a selective pan-class I phosphoinositide 3-kinase (PI3K) inhibitor. It inhibits the catalytic activity of all four isoforms of the PI3K enzyme, which play a crucial role in various cellular processes such as cell growth, proliferation, and survival.

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Lab products found in correlation

Dihydrotestosterone, by MedChemExpress (1 mentions) Anti ha, by Abcam (1 mentions) Enzalutamide, by MedChemExpress (1 mentions) Anti α tubulin, by Cell Signaling Technology (1 mentions) Fetal bovine serum (fbs), by Thermo Fisher Scientific (1 mentions) Dulbecco modified eagle medium (dmem), by Thermo Fisher Scientific (1 mentions) Rpmi 1640, by Thermo Fisher Scientific (1 mentions) Anti gapdh, by Cell Signaling Technology (1 mentions) Penicillin, by Merck Group (1 mentions) Streptomycin, by Merck Group (1 mentions) Hek293t, by American Type Culture Collection (1 mentions) Lncap, by National Collection of Authenticated Cell Cultures (1 mentions) Pf 4708671, by MedChemExpress (1 mentions) Lncap, by American Type Culture Collection (1 mentions) Du145, by American Type Culture Collection (1 mentions) Rwpe 1, by American Type Culture Collection (1 mentions) Azd4547, by MedChemExpress (1 mentions) Incucyte nuclight red lentivirus, by Sartorius (1 mentions) Erlotinib, by MedChemExpress (1 mentions) K14 cre, by Jackson ImmunoResearch (1 mentions)

9 protocols using bkm120

Characterization of Prostate Cancer Cell Lines

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Human PCa cell lines LNCaP, C4–2, 22Rv1 and PC3 were purchased from Chinese Academy of Sciences Cell Bank (Shanghai, China) and maintained in RPMI-1640 (Invitrogen Grand Island, NY, USA). Human embryonic kidney cell HEK-293 T and human cervical cancer cell line HeLa were purchased from American Type Culture Collection (Manassas, VA, USA), and maintained in DMEM (Invitrogen, Grand Island, NY). All mediums were supplemented with 10% fetal bovine serum (FBS, Gibco, Australia), 100 U/mL penicillin (Sigma-Aldrich, St. Louis, MO, USA) and 50 μg/mL streptomycin (Sigma-Aldrich, St. Louis, MO, USA). All cell lines were cultured in incubators with humidified atmosphere of 5% CO₂ and 95% air at 37 °C. Anti-MIIP and anti-FLAG antibody were from Sigma-Aldrich (St. Louis, MO, USA). Anti-PP1α was from Sata Cruz Biotechnology (Dallas, Texas, USA). Anti-HA was from Abcam (Cambridge, MA,USA). Anti-PI3K(p110), anti-AKT, anti-p-AKT (Ser473), anti-mTOR, anti-p-mTOR (Ser2448), anti-p-mTOR (Ser2448), anti-AR, anti-GAPDH and anti-α-tubulin antibodies were from Cell Signaling Technology (Beverly, MA, USA). Dihydrotestosterone, Enzalutamide and BKM120 were commercially purchased (MedChemExpress, Princeton, NJ).

Yan G., Ru Y., Yan F., Xiong X., Hu W., Pan T., Sun J., Zhang C., Wang Q, & Li X. (2019). MIIP inhibits the growth of prostate cancer via interaction with PP1α and negative modulation of AKT signaling. Cell Communication and Signaling : CCS, 17, 44.

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Prostate Cancer Cell Line Characterization

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Human PCa cell lines, LNCaP, C4-2, PC3, DU145 and immortal prostatic epithelial cell line, RWPE1 were purchased from ATCC. C4-2MDVR was provided by Allen Gao from UC Davis^{38 (link)}. LNCaP, C4-2, C4-2MDVR, PC3 and DU145 cells were culture in DMEM medium supplemented with 10% fetal bovine serum (FBS) and 1% streptomycin and penicillin. RWPE1 cells were maintained in keratinocyte serum-free medium (SFM). For ADT treatment, RPMI-1640 (no phenol red) supplemented with 5% charcoal-stripped FBS was applied. Dimethyl-α-KG and nucleosides (AGCU) were purchased from Sigma. GLUL plasmid was purchased from Origene (RC204039). Myristoylated AKT plasmid was given by Jung Wook Park from Duke University^{29 (link)}. BKM-120, rapamycin and PF-4708671 were purchase from MedChem Express (HY-70063), Cell Signaling Technology (9904S) and Selleckchem (S2163).

Xu L., Zhao B., Butler W., Xu H., Song N., Chen X., Hauck J.S., Gao X., Zhang H., Groth J., Yang Q., Zhao Y., Moon D., George D., Zhou Y., He Y, & Huang J. (2022). Targeting glutamine metabolism network for the treatment of therapy-resistant prostate cancer. Oncogene, 41(8), 1140-1154.

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Targeted Cancer Cell Inhibition

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All cell culture reagents (including media and sera) were obtained from Gibco unless otherwise noted. BKM120, Erlotinib, and AZD4547 were purchased from MedChemExpress and resuspended in DMSO to a stock concentration of 10 mM. BKM120 was used at a final concentration of 1 μM. Erlotinib and AZD547 were used at a final concentration of 0.5 μM. IncuCyte NucLight red lentivirus was purchased from Essen Biosciences. SMARTpool ON-TARGETplus siRNA pools (of four different siRNA duplexes) were purchased from Dharmacon (Negative control, non-targeting: D-001810–10-05; Sox2 targeted: L-011778–00-0005). Antibodies are listed in Table 1.

Nguyen K.A., Keith M.J., Keysar S.B., Hall S.C., Bimali A., Jimeno A., Wang X.J, & Young C.D. (2022). Epidermal growth factor receptor signaling in precancerous keratinocytes promotes neighboring head and neck cancer squamous cell carcinoma cancer stem cell-like properties and phosphoinositide 3-kinase inhibitor insensitivity. Molecular carcinogenesis, 61(7), 664-676.

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Genetic Manipulation and 4NQO-Induced Carcinogenesis

Cited 2 times

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K14Cre, K14CreER, and Ribotag mouse strains were purchased from The Jackson Laboratory (Bar Harbor, ME, USA). Mettl1^flox and Mettl1^cKI mice were kindly provided by Dr. Shuibin Lin from The First Affiliated Hospital of Sun Yat‐sen University. Mice were treated with 50 μg/mL 4‐nitroquinoline N‐oxide (4NQO) (Sigma‐Aldrich, St. Louis, MO, USA) in drinking water as previously described [26 (link)]. Four‐week‐old K14CreER;Mettl1^wt/wt (Mettl1^cKO‐Ctrl) and K14CreER;Mettl1^fl/fl (Mettl1^cKO) mice were injected with tamoxifen (Sigma‐Aldrich) at a dose of 4.44 mg/g body weight for 5 consecutive days and then treated with 4NQO in their drinking water for 16 weeks followed by another 12 weeks with normal drinking water. For the Mettl1 overexpression study, we crossed male and female K14Cre;Mettl1^cKI/wt mice to obtain K14Cre;Mettl1^wt/wt (Mettl1^cKI‐Ctl) and K14Cre;Mettl1^cKI/cKI (Mettl1^cKI) mice. For the mouse rescue assay, SC79 (0.04 mg/g), an AKT activator [27 (link)], was intraperitoneally injected for 4 weeks after 4NQO treatment and fed for 20 weeks in Mettl1^cKO‐Ctrl and Mettl1^cKO mice. Mettl1^cKI‐Ctrl and Mettl1^cKI mice were treated with BKM120 (MedChemExpress, Shanghai, China), a PI3K inhibitor [28 (link)], by oral gavage (35 mg/kg) for 4 weeks after 4NQO treatment and feeding for 20 weeks.

Chen J., Li K., Chen J., Wang X., Ling R., Cheng M., Chen Z., Chen F., He Q., Li S., Zhang C., Jiang Y., Chen Q., Wang A, & Chen D. (2022). Aberrant translation regulated by METTL1/WDR4‐mediated tRNA N7‐methylguanosine modification drives head and neck squamous cell carcinoma progression. Cancer Communications, 42(3), 223-244.

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Evaluating Inhibitors on Cell Viability

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5000 cells were plated in 96 well plates and changed to medium (growth media or serum-free media/50ng/ml EGF) containing inhibitors at different concentrations. The following inhibitors were used: BKM-120 and BYL719 (MedChemExpress, LLC), GDC0068 (Selleck), Trametinib (Selleck), Erlotinib (Selleck). After 72 hours, the relative numbers of remaining cells were measured with CellTiter-Glo (Promega, G7572).

Liu H., Paddock M.N., Wang H., Murphy C.J., Geck R.C., Navarro A.J., Wulf G.M., Elemento O., Haucke V., Cantley L.C, & Toker A. (2020). The INPP4B Tumor Suppressor Modulates EGFR Trafficking and Promotes Triple Negative Breast Cancer. Cancer discovery, 10(8), 1226-1239.

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Targeted Delivery of BKM120 in Mice

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As previously described^{33 (link)}, the pan-PI3K inhibitor BKM120 (MedChemExpress) was dissolved in DMSO to 100 mg ml⁻¹. A 10% (v/v) solution was then sequentially diluted in 40% PEG300, 5% Tween-80 and 45% PBS. DMSO (10%) was used as vehicle control. The course of treatment was daily gavage for 14 days. Tumour-bearing mice were first anaesthetized lightly and 100 µl of the solution was delivered to the mouse stomach through a feeding needle (Thermo Fisher Scientific). The study was blinded by one experimentalist performing gavage and the other one measuring the tumour sizes every 2–3 days without knowing the treatment or control. The results were analysed at day 15 after the initial treatment.

Yuan S., Stewart K.S., Yang Y., Abdusselamoglu M.D., Parigi S.M., Feinberg T.Y., Tumaneng K., Yang H., Levorse J.M., Polak L., Ng D, & Fuchs E. (2022). Ras drives malignancy through stem cell crosstalk with the microenvironment. Nature, 612(7940), 555-563.

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Evaluating Anticancer Compound Cytotoxicity

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Macrophages were plated at 10,000 cells in a 96-well plate and left to rest overnight before treatment with 0.0005 – 50 μM of PI-103, BKM-120 (MedChemExpress, MCE), GSK-2636771 (MCE), or Dasatinib (MCE) at 37 °C. At 72 hours, cell viability was assessed by CellTiter-Glo assay in quadruplicate.

López C.L., Brempelis K.J., Matthaei J.F., Montgomery K.S., Srinivasan S., Roy D., Huang F., Kreuser S.A., Gardell J.L., Blumenthal I., Chiefari J., Jensen M.C., Crane C.A, & Stayton P.S. (2021). Arming Immune Cell Therapeutics with Polymeric Prodrugs. Advanced healthcare materials, 11(9), e2101944.

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Comprehensive Inhibitor Protocol

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AZD6244, MEK162, BKM120 and PD0325901 were purchased from Selleck Chemical. Everolimus, AZD8055, GSK690693, MK2206 and BKM120 (as a control) were purchased from MedChemExpress. All inhibitors were solubilized in dimethyl sulfoxide (DMSO) at stock concentrations of 1mM.

Kiessling M.K., Curioni-Fontecedro A., Samaras P., Lang S., Scharl M., Aguzzi A., Oldrige D.A., Maris J.M, & Rogler G. (2016). Targeting the mTOR Complex by Everolimus in NRAS Mutant Neuroblastoma. PLoS ONE, 11(1), e0147682.

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Cellular Proliferation Assay with Inhibitors

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Primary cell line CF-00034-5 was prepared in a 384-well plate for cellular proliferation assay in an identical manner as above. After overnight incubation, the cultures were treated with inhibitors BKM120 (HY-70063, MedChemExpress LLC), BYL719 (S2814, Selleck Chemical), and AUY922 (HY-10215, MedChemExpress). All of the pharmaceuticals were administered at final concentrations of 0.3, 0.949, 3, 9.49, and 30 µM. Cellular proliferation was measured by Cell Titer Glo as described above. IC₅₀ values were determined using GraphPad software and combination indexes were calculated using CalcuSyn software (Biosoft).

Crawford K.A., Berlow N.E., Tsay J., Lazich M., Mancini M., Noakes C., Huang T, & Keller C. (2020). Case report for an adolescent with germline RET mutation and alveolar rhabdomyosarcoma. Cold Spring Harbor Molecular Case Studies, 6(3), a004853.

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