Tak 242

Manufactured by Merck Group

Sourced in United States, Germany, Spain, United Kingdom

TAK-242 is a chemical compound developed by Merck Group. It is a laboratory research tool used to study cellular signaling pathways. The core function of TAK-242 is to selectively inhibit the Toll-like receptor 4 (TLR4) signaling pathway, which plays a role in the body's inflammatory response.

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85 protocols using tak 242

Human Brain Endothelial Cell Isolation and TAK242 Treatment

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All experiments used primary human brain endothelial cells derived from fetal brain tissue. Fetal human brain microvascular endothelial cells (hBMVEC) were isolated as described [29 (link)]. Cells were grown on rat-tail collagen I-coated flasks (BD Biosciences) in complete medium (EBM-2 supplemented with EGM-2MV SingleQuots, Lonza, Cat No CC-3156 and CC-4147) in an incubator set to 37 °C, 5% CO₂, and 100% humidity.
For TAK242 treatment, complete cell culture medium was changed to growth factors-free/serum-free medium for overnight, followed by treatment with 100 nM TAK242 (Sigma, Cat No 614316) for 3 h.

Buzhdygan T.P., Rodrigues C.R., McGary H.M., Khan J.A., Andrews A.M., Rawls S.M, & Ramirez S.H. (2021). The psychoactive drug of abuse mephedrone differentially disrupts blood-brain barrier properties. Journal of Neuroinflammation, 18, 63.

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Isolation and Treatment of Peritoneal Macrophages

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Peritoneal macrophages (PMs) were isolated as previously described [47 (link)]. Briefly, male C57Bl/6 mice were injected intraperitoneally with 1 mL 3% brewer thioglycolate medium (Sigma-Aldrich). Four days later, PMs were obtained via peritoneal lavage with DPBS and resuspended in RPMI 1640 (Gibco) supplemented with 1% penicillin and streptomycin and 10% charcoal-stripped fetal bovine serum. PMs were plated and left to adhere for 2 h at 37 °C in a 5% CO2 atmosphere before being washed with warm DPBS. The next day, PMs were treated with 1 ng/mL lipopolysaccharide (LPS) or 0.2, 1, or 5 µg/mL biglycan for 4 h. To explore the underlying mechanisms of the effect of biglycan, the toll-like receptor 4 inhibitor (TLR4i) TAK-242 (Sigma-Aldrich) or the NF-kB inhibitor BAY 11-7082 (Sigma-Aldrich) was administered 1 h prior to treatment with 1.0 µg/mL biglycan.

Nakamura T., Bonnard B., Palacios-Ramirez R., Fernández-Celis A., Jaisser F, & López-Andrés N. (2022). Biglycan Is a Novel Mineralocorticoid Receptor Target Involved in Aldosterone/Salt-Induced Glomerular Injury. International Journal of Molecular Sciences, 23(12), 6680.

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Inhibition of EGFR Signaling Pathways

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Palmitate (PA), PP2, TAK-242 and AG1478 were purchased from Sigma-Aldrich (St. Louis, MO, USA). Novel EGFR inhibitor 542 was synthesized and characterized by our group. 542 and AG1478 were dissolved in DMSO for in vitro experiments and in sodium carboxyl methyl cellulose (CMC-Na) (1%) for in vivo experiments. Actived-Caspase-3 kit, Enhanced chemiluminescence reagent, and One Step TUNEL Apoptosis Assay Kit were obtained from Beyotime (Nantong, China).

Li W., Fang Q., Zhong P., Chen L., Wang L., Zhang Y., Wang J., Li X., Wang Y., Wang J, & Liang G. (2016). EGFR Inhibition Blocks Palmitic Acid-induced inflammation in cardiomyocytes and Prevents Hyperlipidemia-induced Cardiac Injury in Mice. Scientific Reports, 6, 24580.

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PCSK9 Regulates Macrophage Polarization

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Mouse RAW264.7 cells (Procell Life Science & Technology, China) were cultured in 10% FBS high-glucose complete DMEM in 95% air and 5% CO₂ at 37°C. The RAW264.7 cells were stimulated for 12 h with 1 ng/mL LPS (Sigma, L2880, USA) and for 24 h with 20 ng/mL IL4 (Sigma, SRP3211, USA) to induce M1 macrophage and M2 macrophage differentiation respectively. To investigate the effects of PCSK9 on macrophage polarization, recombinant mouse PCSK9 protein (500 ng/mL) (Novoprotein, CA86, China) was added to polarized RAW264.7 cells for 24 h. To further analyze whether TLR4 is involved in PCSK9-regulated macrophage polarization, cells were pretreated with TLR4 inhibitor (TAK-242, 20 nM) (Sigma, A3850, USA) for 6 h.

Wang F., Li M., Zhang A., Li H., Jiang C, & Guo J. (2022). PCSK9 Modulates Macrophage Polarization-Mediated Ventricular Remodeling after Myocardial Infarction. Journal of Immunology Research, 2022, 7685796.

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Studying Stromal Cell Interactions in Multiple Myeloma

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HC-MSC and HS-5 were pre-treated with 10 ng/mL Lipopolysaccharide (LPS) (Sigma-Aldrich, Milan, Italy) or 1 μg/mL Poly I:C (Polyinosinic:polycytidylic acid, Sigma-Aldrich) for 24 h. After washing, stromal cells were then cultured with PBMC. In a separate set of experiments, HC-MSC or HS-5 cells were incubated with human MM cell lines for 24 h (1:10) before co-culturing with PBMC. In order to assess TLR4 involvement under our experimental conditions, cultures were also treated with TAK-242 (Sigma-Aldrich), a blocker of signaling transduction triggered by TLR4 intracellular domain. For PC and HS-5 co-cultures, we used 10 μM TAK-242 2 h before adding MM cells. TAK-242 treatment did not affect HS-5 viability (Supplementary Fig. 2).

Giallongo C., Tibullo D., Camiolo G., Parrinello N.L., Romano A., Puglisi F., Barbato A., Conticello C., Lupo G., Anfuso C.D., Lazzarino G., Li Volti G., Palumbo G.A, & Di Raimondo F. (2019). TLR4 signaling drives mesenchymal stromal cells commitment to promote tumor microenvironment transformation in multiple myeloma. Cell Death & Disease, 10(10), 704.

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Inflammatory Response Modulation Assay

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Recombinant mouse IL-1β (10 ng/ml, R&D Systems), LPS (Sigma-Aldrich; catalog #L4391), TAK-242 (Sigma-Aldrich; catalog #614316), minocycline (Sigma-Aldrich; catalog #M9511-1G), TLR2 antibody (BioLegend; catalog #121801), BAY 11-7082 (Cayman Chemical; catalog #10010266), (+)-sodium L-ascorbate (vitamin C sodium salt; Sigma-Aldrich; catalog #A7631), ascorbyl palmitate (Sigma-Aldrich; 76183), ATP (Sigma-Aldrich; catalog #A26209), apyrase (Sigma-Aldrich; catalog #A6410).

Zhu L., Liu X., Nemeth D.P., DiSabato D.J., Witcher K.G., Mckim D.B., Oliver B., Le X., Gorantla G., Berdysz O., Li J., Ramani A.D., Chen Z., Wu D., Godbout J.P, & Quan N. (2019). Interleukin-1 causes CNS inflammatory cytokine expression via endothelia-microglia bi-cellular signaling. Brain, behavior, and immunity, 81, 292-304.

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Transition Metal Chloride Synthesis and Analysis

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Nickel chloride (NiCl₂), zinc chloride (ZnCl₂), cobalt chloride (CoCl₂), copper (II) chloride dihydrate (CuCl₂·2H₂O), iron (II) chloride tetrahydrate (FeCl₂·4H₂O), magnesium chloride hexahydrate (MgCl₂·6H₂O), manganese (II) chloride tetrahydrate (MnCl₂·4H₂O), lipopolysaccharides (LPS) from Escherichia coli O111, and 30% (w/v) H₂O₂ were purchased from Wako Pure Chemical Industries (Osaka, Japan). Chlorazol Black and TAK-242 were purchased from Sigma-Aldrich Co. (St. Louis, MO) and Calbiochem-Merck Millipore (Darmstadt, Germany), respectively. Newport Green^TM DCF diacetate was purchased from Invitrogen (Carlsbad, CA) and the Ni wire (purity 99.98%, diameter 0.8 mm) from Nilako (Tokyo, Japan). HNO₃ (69% (w/w)) was purchased from Kanto Chemical Co., Inc. (Tokyo, Japan).

Onodera R., Asakawa S., Segawa R., Mizuno N., Ogasawara K., Hiratsuka M, & Hirasawa N. (2018). Zinc ions have a potential to attenuate both Ni ion uptake and Ni ion-induced inflammation. Scientific Reports, 8, 2911.

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BV2 Cell-based Ischemic Injury Model

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Under normal conditions (20% O₂, 5% CO₂), BV2 cells were cultured with conventional high glucose DMEM in a 37°C incubator. Then, they were divided into normal group, MCAO group, MCAO + hesperidin (100 μM) group, MCAO + TAK-242 group, and MCAO + BAY group. After growing to 50% density, MCAO was induced by transferring BV2 cells into DMEM without glucose and serum (Life Sciences, Inc., USA) and N₂ was inflated for 5 min prior to administration. The dishes were then placed in an incubator at 37°C (containing 1% O₂, 5% CO₂ and 92% N₂) in the presence or absence of hesperidin for 24 h before the medium was changed. After processing, the medium containing hesperidin was removed, replaced with the normal full medium. TAK242 (2 μM; Sigma-Aldrich, 243984) or BAY 11-7082 (15 μM; Sigma-Aldrich, B5556) was adopted for specific inhibition of TLR4 and NF-κB. All chemicals/drugs were sterile and incubated at 5% CO₂ and 37°C for 24 h.

Zhang J., Jiang H., Wu F., Chi X., Pang Y., Jin H., Sun Y, & Zhang S. (2021). Neuroprotective Effects of Hesperetin in Regulating Microglia Polarization after Ischemic Stroke by Inhibiting TLR4/NF-κB Pathway. Journal of Healthcare Engineering, 2021, 9938874.

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TLR4 Inhibition in Human ONH LC Cells

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Primary human ONH LC cells were grown to confluency and pretreated with the selective TLR4 inhibitor, TAK-242 (In vivoGen, San Diego, CA, USA) at 15mM for 2 hours. TAK-242 is a cyclohexene derivative that specifically inhibits TLR4 signaling by binding to the intracellular domain of TLR4 and blocking downstream signaling. We previously performed a dose response curve using TAK-242 in primary human trabecular meshwork cells in culture and determined 15μM had the greatest inhibitory effect without affecting cell viability (29 (link)). Cells were then treated with TGFβ2 (5ng/mL) and/or TAK-242 (15μM) for 72 hours in serum-free medium. For TLR4 activation studies, hONH LC cultures were grown to confluency and treated with cellular fibronectin (cFN) (10μg/mL) containing the FN-EDA isoform (F2518; Sigma-Aldrich Corp., St. Louis, MO, USA) and/or TGFβ2 (5ng/mL), and/or TAK-242 (15μM) for 72 hours in serum-free medium. Western blot and immunocytochemistry experiments were performed as described below.

Geiduschek E.K., Milne P.D., Mzyk P., Mavlyutov T.A, & McDowell C.M. (2022). TLR4 signaling modulates extracellular matrix production in the lamina cribrosa. Frontiers in ophthalmology, 2, 968381.

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Intravascular Hemolysis Model in Mice

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Animal experiments were performed in accordance with the Directive 2010/63/EU of the European Parliament and were approved by the Institutional Animal Care and Use Committee (IIS‐Fundación Jimenez Diaz). All mice were male, aged 12 weeks, and weighed 25–30 g. In a first set of experiments, intravascular hemolysis was induced in C57BL/6J mice (Tlr4
^+/+; EnVigo, Barcelona, Spain) and TLR4‐deficient mice (Tlr4
^−/−; obtained from Dr. Consuelo Guerri, CIPF, Spain) by a single intraperitoneal administration of freshly prepared phenylhydrazine (Phe) solution (150 mg/kg of body weight, Cat#114715 Sigma‐Aldrich, St. Louis, MO, USA). In another study, the TLR4 inhibitor TAK‐242 (5 mg/kg of body weight, Cat#614316 Sigma‐Aldrich) was administrated intraperitoneally 1 or 4 h before and 24 and 48 h after intraperitoneal injection of phenylhydrazine. TAK‐242 reaches a high concentration in plasma 3 h after intraperitoneal injection [20 (link)]. Mice were euthanized 72 h after phenylhydrazine injection. Blood samples were collected for hematological analysis (Scil Vet ABC hematology analyzer, Scil, Madrid, Spain) and biochemical analysis (ADVIA 2400 Clinical Chemistry System, Siemens Healthcare, Erlangen, Germany). Dissected kidneys, liver, and spleen were fixed in 4% paraformaldehyde and embedded in paraffin wax for histological studies or snap‐frozen for RNA and protein isolation.

Vázquez‐Carballo C., Herencia C., Guerrero‐Hue M., García‐Caballero C., Rayego‐Mateos S., Morgado‐Pascual J.L., Opazo‐Rios L., González‐Guerrero C., Vallejo‐Mudarra M., Cortegano I., Gaspar M.L., de Andrés B., Egido J, & Moreno J.A. (2022). Role of Toll‐like receptor 4 in intravascular hemolysis‐mediated injury. The Journal of Pathology, 258(3), 236-249.

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