Pi 103

Manufactured by Selleck Chemicals

Sourced in United States

PI-103 is a lab equipment product that serves as a selective inhibitor of phosphoinositide 3-kinase (PI3K) enzymes. It is used for experimental research purposes.

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Lab products found in correlation

33 protocols using pi 103

B591 Synthesis and Formulation

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B591 was synthesized and identified according to Supplementary Materials and Methods (Supplementary Fig. S1-S4). For in vitro study, 10 mM stock solution of B591 in DMSO was used. For in vivo study, B591 was dissolved in the solution composed of 1.5% Tween-20, 5% PEG400 and 2% Cremophor EL in 0.9% Saline. Rapamycin, PI-103 and paclitaxel were purchased from Selleckchem (Houston, TX, USA).

Zhou H., Yu C., Kong L., Xu X., Yan J., Li Y., An T., Gong L., Gong Y., Zhu H., Zhang H., Yang X, & Li Y. (2019). B591, a novel specific pan-PI3K inhibitor, preferentially targets cancer stem cells. Oncogene, 38(18), 3371-3386.

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High-Throughput Drug Screening Assays

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Reversible EGFR/ErbB2 RTK inhibitor Lapatinib (Cat. S1028), irreversible pan-ErbB RTK inhibitor Poziotinib (Cat. S7358), and PI3K/Akt/mTOR inhibitor PI-103 (Cat. S1038) were purchased from Selleckchem (Houston, TX). Recombinant human NRG1 was acquired from BioLegend (San Diego, CA, Cat. 551904). High-throughput drug screening assays were used with compounds sourced as indicated in Suppl. Table 1.

Ippolitov D., Lin Y.H., Spence J., Glogowska A., Thanasupawat T., Beiko J., Del Bigio M.R., Xu X., Wang A., Calvo R., Kapoor A., Marugan J.J., Henderson M.J., Klonisch T, & Hombach-Klonisch S. (2024). Overcoming brain-derived therapeutic resistance in HER2+ breast cancer brain metastasis. bioRxiv.

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Multimodal Profiling of Extracellular Vesicles

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Daporinad (catalog no. S2799), venetoclax (catalog no. S8048), OSI-027 (catalog no. S2624), PI-103 (catalog no. S1038), and doxycycline (catalog no. S5159) were obtained from Selleck Chemicals (Houston, TX, USA). CCCP (catalog no. HY-100941) and metformin hydrochloride (catalog no. HY-17471A) were purchased from MedChemExpress (Greenville, SC, USA). Anti-CD63 (ab59479), anti-CD81 (ab79559), and anti-TSG101 (ab125011) antibodies for immunoblotting and flow cytometry were purchased from Abcam (Cambridge, UK).

Wu Z., Sun H., Wang C., Liu W., Liu M., Zhu Y., Xu W., Jin H, & Li J. (2020). Mitochondrial Genome-Derived circRNA mc-COX2 Functions as an Oncogene in Chronic Lymphocytic Leukemia. Molecular Therapy. Nucleic Acids, 20, 801-811.

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Long-term cytotoxicity assay in A549 and H1299

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A549 and H1299 cells (100/well) were allowed to attach overnight then treated with NU7441 or PI-103 (Selleckchem.com, Houston, TX) at the indicated concentrations for 17-22 days. Cell were then rinsed with PBS then stained with 0.5% crystal violet in 25% methanol, photographed and quantified using ImageJ as percent area covered. Differences between groups were compared by unpaired t test.

Haeger S.M., Thompson J.J., Kalra S., Cleaver T.G., Merrick D., Wang X.J, & Malkoski S.P. (2015). Smad4 loss promotes lung cancer formation but increases sensitivity to DNA topoisomerase inhibitors. Oncogene, 35(5), 577-586.

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Cytotoxicity Assay with Cisplatin

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Cisplatin, MTT reagent,
DAPI, and propedium iodide were procured from Sigma-Aldrich. PI103
and AZD6244 were purchased from Selleck Chemicals. DMEM media, LysoTracker
Red DND-99 were obtained from Life Technologies. HCT-116 cells were
obtained from National Centre for Cell Science (NCCS), Pune. Anti-phospho-Akt
(Thr308) rabbit monoclonal antibody, anti-ERK1/2 phospho monoclonal
antibody, anti-total-AKT antibody, anti-total ERK1/2 antibody, anti-GAPDH
antibody, HRP goat anti-mouse IgG antibody, and apoptosis detection
kit were purchased from BioLegend. All chemical reactions were carried
out under an argon atmosphere using dry solvents unless otherwise
stated.

Palvai S., Kuman M.M., Sengupta P, & Basu S. (2017). Hyaluronic Acid Layered Chimeric Nanoparticles: Targeting MAPK-PI3K Signaling Hub in Colon Cancer Cells. ACS Omega, 2(11), 7868-7880.

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PI3K Inhibitor Treatment Profiling

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293T and IGROV cells were plated at 5 × 10⁵ cells per 10 cm plate, and were treated with PI3K inhibitors GDC-0941 and PI-103 (Selleck Chemicals, Houston, TX) 24 hours post plating. Following 24 hours of treatment, cells were harvested as above and subjected to western blot analysis.

Nanos-Webb A., Bui T., Karakas C., Zhang D., Carey J.P., Mills G.B., Hunt K.K, & Keyomarsi K. (2015). PKC iota promotes ovarian tumor progression through deregulation of cyclin E. Oncogene, 35(19), 2428-2440.

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Chemical Compounds for Cancer Research

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Panobinostat, vorinostat, pracinostat, trichostatin-A (TSA), RG2833, entinostat, bortezomib, marizomib, FK866, niraparib, selisistat, gefitinib, enzastaurin, dasatinib, dinaciclib, PI103, PD-0325901, HSP990, ABT737, (+)- JQ, TP0903, Bay11–7082, YM155, and cucurbitacin-I were purchased from Selleck Chemicals (Houston, TX). Vincristine, vinblastine, paclitaxel, topotecan, gemcitabine, 5-fluoruracil, and temozolomide were purchased from Sigma Aldrich (St. Louis, MO).

Jane E.P., Premkumar D.R., Thambireddy S., Golbourn B., Agnihotri S., Bertrand K.C., Mack S.C., Myers M.I., Chattopadhyay A., Taylor D.L., Schurdak M.E., Stern A.M, & Pollack I.F. (2020). Targeting NAD+ biosynthesis overcomes panobinostat and bortezomib-induced malignant glioma resistance. Molecular cancer research : MCR, 18(7), 1004-1017.

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CRC Cell Line Characterization and Drug Screens

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Human CRC cell lines used in this study were HCT-116 (CVCL_0291), HT-29 (CVCL_0320) and SW-620 (CVCL_0547). The cell lines were directly obtained from NCI. No mycoplasma testing was done in-house. Cells were routinely cultured in 1X RPMI-1640 medium (Thermo Fisher Scientific) supplemented with 10% fetal bovine serum (FBS, Sigma Aldrich), 2 mM l-Glutamine (Sigma Aldrich) and 100 U/mL Penicillin–Streptomycin (Thermo Fisher Scientific). All cells were maintained at 37 °C with 5% CO₂ and 80% relative humidity and passaged according to in-house protocols (see Supplementary Methods). Cells used in experiments never exceeded passage 21.
Drugs used in screens were olaparib (Selleckchem), oxaliplatin (Selleckchem), palbociclib (Selleckchem), PI-103 (Selleckchem), PD0325901 (Sigma Aldrich), 5-fluorouracil (5-FU, Sigma Aldrich) and 5Z-7-Oxozeaenol (Enzo Life Sciences). Assay reagents used in screens were CellTiter-Glo 2.0 Assay (Promega), CellTiter-Glo 3D Cell Viability Assay (Promega), CellTox Green Cytotoxicity Assay¹⁷ (Promega) and NucView 488 Caspase-3 Substrate¹⁸ (Biotium).

Folkesson E., Niederdorfer B., Nakstad V.T., Thommesen L., Klinkenberg G., Lægreid A, & Flobak Å. (2020). High-throughput screening reveals higher synergistic effect of MEK inhibitor combinations in colon cancer spheroids. Scientific Reports, 10, 11574.

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Cell Line Characterization and Compound Screening

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T47D, MCF7 cells were purchased from American Type Culture Collection (ATCC) in 2012 - 2015. They were authenticated using STR testing and tested negative for Mycoplasma contamination. EFM19, BT474, MDAMB453, HCC202, MDAMB361, HCC1419, MDAMB415, HCC1937, CAL51, BT20, HCC1954, and JIMT1 cells were purchased from Cancer Cell Line Encyclopedia (CCLE) at the Broad Institute in 2015-2016, and were authenticated using SpectroCHIPII-G384 by Sequenom's MassARRAY Analyzer Compact. All the cells were maintained in RPMI-1640 with 10% fetal bovine serum. BYL719, GDC0941, BKM120, AZD1208, GDC0032, PI-103, BX795, BX912, MK2204, GDC0068, sirolimus, everolimus, PP242 and WYE were purchased from Selleck Chemicals (Supplementary Material and Methods). Blasticidine was purchased from Life Technologies. LGH447 was obtained from Novartis.

Le X., Antony R., Razavi P., Treacy D.J., Luo F., Ghandi M., Castel P., Scaltriti M., Baselga J, & Garraway L.A. (2016). Systematic functional characterization of resistance to PI3K inhibition in breast cancer. Cancer discovery, 6(10), 1134-1147.

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Synthesis and Characterization of PI-103 Compound

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RIDR-PI-103 was synthesized as described [29 (link)]. PI-103 (Cat# S1038) was obtained from Selleckchem (Houston, Texas, USA). All drugs were dissolved in dimethyl sulfoxide (DMSO) (Fisher Scientific, Waltham, Massachusetts, USA) at desired concentrations and stored at −20°C. Glutathione was obtained from Fisher Scientific (Cat# BP25211). N-acetyl cysteine (NAC) was obtained from Fisher Scientific (Cat# AAA1540936). TBHP was obtained from Fisher Scientific (Cat# AC180340050). Dabrafenib (Cat# D-5699) and trametinib (Cat# T-8123) were purchased from LC Laboratories (Woburn, Massachusetts, USA).

Patel H., Mishra R., Wier A., Mokhtarpour N., Merino E.J, & Garrett J.T. (2023). RIDR-PI-103, ROS-activated prodrug PI3K inhibitor inhibits cell growth and impairs the PI3K/Akt pathway in BRAF and MEK inhibitor-resistant BRAF-mutant melanoma cells. Anti-Cancer Drugs, 34(4), 519-531.

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