Ko143

Manufactured by MedChemExpress

Sourced in United States

Ko143 is a laboratory equipment product offered by MedChemExpress. It is a potent and selective inhibitor of the breast cancer resistance protein (BCRP/ABCG2) transporter.

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Lab products found in correlation

7 protocols using ko143

Ovarian Cancer Cell Line Analysis

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The human HGSOC cell lines OVCAR3 and OVCAR8 were gifts from Professor Zhi Yao (Tianjin Medical University, Tianjin, China) and a mouse ovarian epithelial papillary serous adenocarcinoma cell line ID8 cell was a gift from Professor Luyuan Li (Nankai University, Tianjin, China). All the cells were cultured in RPMI 1640 or DMEM (Thermo Fisher Scientific, Inc.) supplemented with 10% (v/v) FBS (Gibco; Thermo Fisher Scientific, Inc.). The reagents for in vitro studies included cisplatin (DDP; Qilu Pharmaceutical Co., Ltd.) (OVCAR3; 40 μM; ID8; 10 μM); paclitaxel (PTX; Yangtze River Pharmaceutical Group) (OVCAR3; 3 nM; ID8; 20 nM); troglitazone (a PPARγ agonist; Trog, Selleck Chemicals), 25 μM; GW9662 (a PPARγ agonist; Selleck Chemicals), 25 μM; and an ABCG2 inhibitor, KO143 (MedChemExpress), 10 μM. For in vitro studies, cells were pretreated with Trog, GW9662 and KO143 for 2 h after which the media was changed to the normal media for further treatments.

Chen S., Liu Z., Wu H., Wang B., Ouyang Y., Liu J., Zheng X., Zhang H., Li X., Feng X., Li Y., Shen Y., Zhang H., Xiao B., Yu C, & Deng W. (2024). Adipocyte-rich microenvironment promotes chemoresistance via upregulation of peroxisome proliferator-activated receptor gamma/ABCG2 in epithelial ovarian cancer. International Journal of Molecular Medicine, 53(4), 37.

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Stem Cell Culture with Signaling Modulators

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Hoechst 33342, Ko143 and YHO-13177 were purchased from Med Chem Express (Monmouth Junction, NJ, USA). Recombinant human R-spondin 1 and recombinant mouse noggin were obtained from Pepro Tech Inc. (Rocky Hill, NJ, USA). Mouse recombinant EGF, advanced DMEM/F12, B-27 supplement and N-2 supplement were supplied by Invitrogen (Carlsbad, CA, USA). Matrigel (GFR, phenol-free) was bought from Corning Inc. (Bedford, MA, USA). Anti-BCRP antibody and goat anti-rabbit antibody were purchased from Abcam (Cambridge, UK). Trizol, PrimeScript™ RT reagent Kit and SYBR^® Premix Ex Taq™ II MIX were supplied by Takara (Dalian, China).

Zhang L., Zhao J., Liang C., Liu M., Xu F, & Wang X. (2017). A novel biosensor based on intestinal 3D organoids for detecting the function of BCRP. Drug Delivery, 24(1), 1453-1459.

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Baicalein Glucuronides Profiling Protocol

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Polyethylene glycol 400 was obtained from Xiqiao Chemical Co., Ltd. Baicalein‐7‐O‐β‐d‐glucuronide(BG), baicalein and genistein (IS) standards (purity ≥98%) were obtained from China National Institute for the Control of Pharmaceutical and Biological Products. Baicalein‐6‐O‐β‐d‐glucuronide(B6G) standard (purity ≥95%) was obtained from Dalian Medical University. Hank's buffered salt solution (HBSS), phosphate‐buffered saline (PBS), Tris‐HCl buffer solution (PH = 7.4) and Tris‐Tricine‐SDS‐PAGE gel kit were obtained from Solarbio (Beijing Solarbio Science & Technology Co., Ltd.). 100 U/ml of penicillin, 100 μg/ml of streptomycin, fetal bovine serum (FBS), and 0.25% trypsin with ethylenediaminetetraacetic acid (trypsin–EDTA) were obtained from Wiseen. Verapamil, MK571 and KO143 were obtained from MedChemExpress. The human intestine microsomes were obtained from Xenotech. The uridine diphosphate glucuronic acid (UDPGA) (purity ≥95%) was obtained from Quanyang Biotechnology Co., Ltd. The alamethicin (purity ≥98.0%) was obtained from Shanghai Aladdin Biochemical Technology Co., Ltd.

Cao S., Zhang M., Yuan M., Yang D., Zhao M., Zhang S., Wang P., Zhang R, & Gao X. (2022). The pharmaceutical excipient PEG400 affect the absorption of baicalein in Caco‐2 monolayer model by interacting with UDP‐glucuronosyltransferases and efflux transport proteins. Pharmacology Research & Perspectives, 10(1), e00928.

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Efficient Multidrug Resistance Inhibition

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The σ₂ receptor ligand A011 was prepared as previously reported (Feng et al., 2019 (link)). KO143 was purchased from MedChemExpress (Monmouth Junction, NJ, United States). Cisplatin (DDP), adriamycin (ADR), paclitaxel, verapamil, mitoxantrone and rhodamine 123 (Rh123) were acquired from Solarbio (Beijing, China). Cell Counting Kit-8 (CCK-8) was bought from Dojindo Laboratories (Japan). Pgp-Glo™ Assay Systems were purchased from Promega (Madison, USA). Anti-P Glycoprotein antibody, ABCG2, GAPDH, Goat Anti-Rabbit IgG H&L Secondary Antibody (Alexa Fluor 488), Goat Anti-Rabbit IgG H&L Secondary Antibody and Goat Anti-Mouse IgG H&L Secondary Antibody were purchased from Abcam (Cambridge, United Kingdom). SlowFade^TM Gold antifade reagent was purchased from Thermo Fisher (MA, United States).

Zeng Z., Liao S., Zhou H., Liu H., Lin J., Huang Y., Zhou C, & Xu D. (2022). Novel Sigma-2 receptor ligand A011 overcomes MDR in adriamycin-resistant human breast cancer cells by modulating ABCB1 and ABCG2 transporter function. Frontiers in Pharmacology, 13, 952980.

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Investigating Multidrug Resistance Mechanisms

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Gedatolisib (purity: 99.09%) was purchased from Selleck Chemicals (Houston, TX, USA). Paclitaxel (purity: 99.02%), doxorubicin (purity: 99.37%), vincristine (purity: 99.19%), mitoxantrone hydrochloride (purity: 99.9%), topotecan hydrochloride (purity: 100.0%), and cisplatin (purity: 99.62%) were purchased from Energy Chemicals (Shanghai, China). Verapamil hydrochloride (purity: 99.95%) and Ko143 (purity: 99.79%) were purchased from MedChemExpress (NJ, USA). Tritium-labeled paclitaxel and mitoxantrone were obtained from SuYa Medicine (Beijing, China). Fetal bovine serum (FBS), Dulbecco’s modified Eagle’s Medium (DMEM), penicillin/streptomycin, and trypsin were purchased from Corning Incorporated (Corning, NY, USA). G418, DMSO, 3-[4,5-dimethylthiazol-yl]-2,5-diphenyltetrazolium bromide (MTT), propidium iodide (PI), and paraformaldehyde, were purchased from Beyotime Biotechnology (Shanghai, China). Antibody of GAPDH, ABCB1, and ABCG2, Alexa Fluor 488 conjugated goat anti-mouse IgG secondary antibody, HRP-conjugated goat anti-mouse IgG secondary antibody were purchased from Cell Signaling Technology (Danvers, MA, USA). All other chemicals were obtained from Sigma Chemical Co (St. Louis, MO, USA).

Liu C., Xing W., Yu H., Zhang W, & Si T. (2021). ABCB1 and ABCG2 restricts the efficacy of gedatolisib (PF-05212384), a PI3K inhibitor in colorectal cancer cells. Cancer Cell International, 21, 108.

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Investigating Multidrug Resistance Mechanisms

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Metyrapone, ketoconazole, and mitoxantrone were purchased from Shanghai Yuanye Bio-Technology Co., Ltd (Shanghai, China). Ko143 was purchased from MedChemExpress (Monmouth Junction, NJ). Anti-ABCG2 (N338) and anti-β-tubulin polyclonal antibodies were purchased from Bioworld Technology (Louis Park, MN). DNA transfection reagents were purchased from Vazyme Biotech Co., Ltd (Nanjing, China). An RNA transfection reagent was purchased from Zeta Life (Menlo Park, CA). All other chemicals were of analytical grade and obtained from standard suppliers unless mentioned otherwise.

Xu Z., Li M., Lu W., Wang L, & Zhang Y. (2022). Chicken xenobiotic receptor upregulates the BCRP/ABCG2 transporter. Poultry Science, 102(1), 102278.

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Detailed Pharmacological Reagents Protocol

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TAK-243 (formerly known as MLN7243) was provided by Millennium Pharmaceuticals, Inc., a wholly owned subsidiary of Takeda Pharmaceutical Company Limited, and purchased from Active Biochem (catalog A-1384), and pevonedistat (MLN4924/TAK-924) was provided by Dalton Medicinal Chemistry. Bortezomib (catalog S1013) was purchased from Selleckchem, TAK-981 from ChemiTek (catalog CT-TAK981), mitoxantrone (catalog M6545) and HPBCD (catalog H107) from MilliporeSigma, and tunicamycin (catalog 3516), thapsigargin (catalog 1138), zosuquidar (catalog 5456), and Ko143 (catalog 3241) from Tocris. Ko143 for animal experiments was purchased from MedChemExpress (catalog HY-10010).

Barghout S.H., Aman A., Nouri K., Blatman Z., Arevalo K., Thomas G.E., MacLean N., Hurren R., Ketela T., Saini M., Abohawya M., Kiyota T., Al-Awar R, & Schimmer A.D. (2021). A genome-wide CRISPR/Cas9 screen in acute myeloid leukemia cells identifies regulators of TAK-243 sensitivity. JCI Insight, 6(5), e141518.

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