Tak 242

Manufactured by Apexbio

Sourced in United States

TAK-242 is a small molecule compound that functions as a selective inhibitor of Toll-like receptor 4 (TLR4). TLR4 is a cell surface receptor that plays a key role in the innate immune response to various pathogenic stimuli. The primary role of TAK-242 is to modulate TLR4 signaling pathways.

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Lab products found in correlation

20 protocols using tak 242

Paeoniflorin Inhibits TLR4/NF-κB Pathway

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Paeoniflorin was purchased from Shanghai Yuanye Biotechnology Company (Shanghai, China), and TAK-242 was from APExBio (A3850). TLR4, MyD88, NF-κB p65, and β-actin were purchased from Abcam (USA) and those against caspase-3, Bax, and BCL2 were from Abbkine (China). The H9c2 cell line were purchased from the cell resource center of Shanghai Institute of Life Sciences, Chinese Academy of Sciences.

Shi H., Zhou P., Ni Y.Q., Wang S.S., Song R., Shen A.L., Fang Z.H, & Wang L. (2021). In vivo and in vitro studies of Danzhi Jiangtang capsules against diabetic cardiomyopathy via TLR4/MyD88/NF-κB signaling pathway. Saudi Pharmaceutical Journal : SPJ, 29(12), 1432-1440.

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Baicalin Modulates TLR4/PI3K/AMPK Pathway

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Baicalin (purity ≥ 98%) was obtained from Xi’an Kai Lai Biological Engineering Co., Ltd. (Xi’an, China). Fluoxetine hydrochloride (Flu) was purchased from Changzhou Siyao Pharmaceuticals Co., Ltd. (Changzhou, China). Lipopolysaccharide (LPS), 4,6-diamidino-2-phenylindole (DAPI), and compound C were bought from Sigma-Aldrich Co (St. Louis, USA). TAK-242 (a TLR4 antagonist) and LY294002 (a PI3K inhibitor) were products purchased from Apex Bio (Houston, USA). Poly-d-lysine was obtained from Sigma (MO, USA). Interleukin-1β (IL-1β), Interleukin-6 (IL-6), and tumor necrosis factor α (TNF-α) enzyme-linked immunosorbent assay (ELISA) kits were supplied by Elabscience Biotechnology Co., Ltd. (Wuhan, China). The antibodies were obtained from the cited commercial sources: anti-p-PI3K (#4228), anti-PI3K (#4292), anti-p-Akt (Ser473, #9271), anti-Akt (#9272), anti-β-actin (#4967), anti-PCNA (#13110), anti-p-AMPK (#2531), and anti-AMPK (#2603) were from Cell Signaling Technology (Beverly, MA, USA); anti-PTEN (sc-7974) and anti-p-PTEN (sc-377573) were from Santa Cruz Biotechnology (Santa Cruz, CA); anti-TLR4 (AF7017), anti-p-GSK3β (AF2016), and anti-GSK3β (AF7814) were from Affinity Biosciences (Changzhou, China); and anti-FoxO1 (ab52857), anti-p-FoxO1 (Ser 256, ab131339), and goat anti-rabbit IgG H&L (Alexa Fluor® 488, ab150077) were from Abcam (Cambridge, MA, USA).

Guo L.T., Wang S.Q., Su J., Xu L.X., Ji Z.Y., Zhang R.Y., Zhao Q.W., Ma Z.Q., Deng X.Y, & Ma S.P. (2019). Baicalin ameliorates neuroinflammation-induced depressive-like behavior through inhibition of toll-like receptor 4 expression via the PI3K/AKT/FoxO1 pathway. Journal of Neuroinflammation, 16, 95.

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Inhibition of MAPK Signaling Pathways

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COX-2 inhibitor NS398 (50 μM), p38 MAPK inhibitor SB202190 (FHPI) (10 μM), and ERK1/2 MAPK inhibitor SCH772984 (10 μM), was purchased from Selleck Chemicals (Houston, United States). TLR4 inhibitor TAK-242 (10 μM) was purchased from APEXBIO Technology (Houston, United States). Cells were separately pretreated with these drugs at the indicated concentrations for 1 h at 37°C. At the time of the second addition of gentamicin, the inhibitors were also added, and the point was defined as time 0. Cells treated with TAK-242 were collected at 1 h after infection to detect the protein level of phosphorylated and unphosphorylated ERK1/2 MAPK and p38 MAPK, and at 6 h after infection to determine the COX-2 expression level. ERK1/2 inhibitor SCH772984 and p38 MAPK inhibitor SB202190 (FHPI) treated cells were collected at 6 h after infection to detect COX-2 expression level. NS398 treated cells were collected at 6 h and 9 h after infection to detect reactive oxygen species (ROS), cell death, and cytokine expression levels. NS398 treated cells were collected at 6 h after infection to investigate the LC3 expression level. These experiments were performed in triplicate with three biological repetitions.

Ren H., Chen X., Jiang F, & Li G. (2020). Cyclooxygenase-2 Inhibition Reduces Autophagy of Macrophages Enhancing Extraintestinal Pathogenic Escherichia coli Infection. Frontiers in Microbiology, 11, 708.

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RAGE and TLR4 Inhibition in Traumatic Brain Injury

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59 C57BL/6 wild-type (WT) mice at the age of 2 months received undercut or sham surgeries. They received daily vehicle (normal saline), RAGE monoclonal (RAGE mAb, 10 mg/kg, i.p. Abbvie Laboratories, Deerfield, IL) or TAK242, a TLR4 inhibitor (3 mg/kg, i.p., Apexbio Technology LLC, TX) injection for 1 week starting on the next day after surgery. At 2 weeks after the injury, a PTZ test was performed on these animals.

Ping X., Chai Z., Wang W., Ma C., White F.A, & Jin X. (2021). Blocking receptor for advanced glycation end-products (RAGE) or toll like receptor 4 (TLR4) prevents posttraumatic epileptogenesis in mice. Epilepsia, 62(12), 3105-3116.

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TLR Inhibitors Modulate A-MSCs and T Cells

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The TLR3 inhibitor CU CPT 4a (ApexBio, B5752, USA) and TLR4 inhibitor TAK-242 (ApexBio, A3850, USA) were separately added to the α-MEM cell medium containing 10% FBS to a final concentration of 10 μM. The supernatant was removed and repeatedly washed with 0.9% NaCl after a 24 h incubation with A-MSCs. Following this, 0–1000 ng/mL PLP were added to stimulate A-MSCs for 48 h. Simultaneously, cells without inhibitor stimulation were used as control groups. Lymphocytes were cocultured with PLP-stimulated A-MSCs for 48 h, and the supernatant and cells were collected to measure the ratio of CD3⁺CD8⁺ T lymphocytes. The level of kynurenic acid in the supernatant from blank groups was determined using a human kynurenic acid kit (JSBOSSEN, BS-E7827H2, China).

Li C., Huang J., Zhu H., Shi Q., Li D, & Ju X. (2019). Pyridoxal-5′-Phosphate Promotes Immunomodulatory Function of Adipose-Derived Mesenchymal Stem Cells through Indoleamine 2,3-Dioxygenase-1 and TLR4/NF-κB Pathway. Stem Cells International, 2019, 3121246.

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Quantifying Autophagy in RAW264.7 Cells

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RAW264.7 cells were harvested in the logarithmic growth phase and placed in 96-well plates (10⁵ cells/well). RAW264.7 cells were pre-treated or not with TLR4 inhibitor TAK242 (1 μM; APExBIO, A3850), incubated with recombinant proteins (5 μg/mL) for 24 h, and stained with monodansylcadaverine (MDC) (100 μM; Sigma-Aldrich, #30432) at 37 °C in the dark for 10 min. The cells were washed gently with warm Ca/Mg-containing Hank’s Balanced Salt Solution (Gibco, #14025-092) and counterstained with Hoechst 33342 (1 μM) at 37 °C in the dark for 5 min. After repeated washing with the same buffer, cells kept in warm buffer were immediately observed and quantified using the Operetta High-content Screening system (Perkin-Elmer, Hopkinton, MA, USA).

Li X., Zhang Y., Zhao Y., Qiao K., Feng M., Zhou H., Tachibana H, & Cheng X. (2020). Autophagy Activated by Peroxiredoxin of Entamoeba histolytica. Cells, 9(11), 2462.

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Blocking AT1R and TLR4 in Hypertensive Rats

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All procedures were approved by the Institutional Animal Care and Use Committee (protocol 2017–2883) and were performed in accordance with the Guide for the Care and Use of Laboratory Animals, as recommended by the US National Institutes of Health. Male Wistar Kyoto rats (WKY) and SHRs (Charles River Laboratories, USA) were housed in temperature- and humidity-controlled rooms (22±1°C; 50±5%) under a 12–12h light-dark cycle with standard rat chow and water ad libitum. Animals were 7–8 weeks old (175–225g) at the start of experiments. SHRs were randomly divided into control or experimental groups. For AT1R blockade, SHRs were treated daily with Losartan (AT1R antagonist; TCI America, USA; 20mg/kg BW^{16 (link)}; oral gavage; SHR-Los) or vehicle for 4 weeks, and age-matched with WKYs (n=6/group). For TLR4 blockade, SHRs were treated daily with TAK-242 (TLR4 antagonist; Apex Bio, USA; MedChem Express, USA; 2mg/kg BW^{30 (link)}; i.p.; SHR-TAK; n=17) for 2 weeks, and age-matched with control SHRs (n=13) and WKYs (n=11). The dose of TAK-242 was chosen based on previous work supporting suppression of cardiac and renal inflammatory cytokines levels (TNF-a, IL-1β and MCP-1) and prevention of blood pressure increases in a model of Aldosterone-induced hypertension^{31 (link)}.

Mowry F.E., Peaden S.C., Stern J.E, & Biancardi V.C. (2021). TLR4 and AT1R mediate blood-brain barrier disruption, neuroinflammation, and autonomic dysfunction in spontaneously hypertensive rats. Pharmacological research, 174, 105877.

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Investigating Berberine's Effect on Diabetic Nephropathy in Podocytes

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Conditionally immortalized mouse podocytes were purchased from Yubo Bio-Technique Co. Ltd (Shanghai, China) and cultured in RPMI 1640 medium (Hyclone, Logan, UT, USA) supplemented with 10% fetal bovine serum (FBS; Hyclone), 100 U/ml penicillin/streptomycin, 5.6 mM glucose (Dingguo Changsheng Biotechnology Co., Ltd., Beijing, China) and 10 U/ml recombinant mouse interferon-γ (IFNγ; Pepro Technology, Rocky Hill, NJ, USA) at 33 °C in a 5% CO₂ humidified incubator. To investigate the effect of BBR on DN, podocytes were pre-treated with 30 mM high glucose (HG) for 24 h prior to treatment with BBR at a dose of 10, 30 or 90 μM for 24 h. In some experiment, podocytes were pre-treated with 30 mM HG in the presence of TLR4 antagonist resatorvid (TAK-242, 1 μΜ; ApexBio, Houston, TX, USA), NF-κB inhibitor pyrrolidine dithiocarbamate (PDTC; 50 μM; Sigma), or combined with NF-κB activator phorbol myristate acetate (PMA, 100 ng/ml; Sigma), followed by treated with 30 μM BBR for 24 h.

Zhu L., Han J., Yuan R., Xue L, & Pang W. (2018). Berberine ameliorates diabetic nephropathy by inhibiting TLR4/NF-κB pathway. Biological Research, 51, 9.

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S100A8/A9 Modulates Osteogenesis

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BMSC and C3H/10T1/2 were treated with 200, 500, and 1000 ng/mL of endotoxin-free S100A8/A9 RP (8916-S8-050, R&D, USA) for 7 days in osteogenic medium. C2C12 stromal cells were treated with 100, 200, and 300 ng/mL of S100A8/A9 RP for 5 days in osteogenic medium. BPADs and BADs induced from C2C12 cells (C2C12 BADs) were treated with rapamycin (HY-10219, MCE, shanghai, China) ranging from 4 to 12 nM for 12h before cells and CM were collected. For NF-κB inhibition, C2C12 BADs were treated with 10 μM SN50 (HY-P0151, MCE) and 10 nM QNZ (EVP4593, Selleck, shanghai, China) for 2 h and 24 h, respectively. For TLR4 inhibition, C3H/10T1/2 were treated with S100A8/A9 RP and 200 nM TAK-242(A3850, Apexbio, USA) for 7 days in osteogenic medium.

Wang T., Zhao C., Zhang J., Li S., Zhang Y., Gong Y., Zhou Y., Yan L., Zhang S., Zhang Z., Hu H., Liu A., Bai X, & Zou Z. (2024). Whitening of brown adipose tissue inhibits osteogenic differentiation via secretion of S100A8/A9. iScience, 27(2), 108857.

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In Vivo TAK 242 Administration for Neuroinflammation

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TAK 242 is a selective inhibitor of TLR4, which binds to the TIR domain of the receptor and disrupts the interaction of TLR4 with its adaptor molecules, thereby inhibiting downstream signaling [16 (link)]. The molecule has been used to study the role of TLR4 and its signaling molecules in several inflammatory conditions [6 , 18 (link)]. The protocol used in this study was adapted from previous in vivo experiments with TAK 242 [18 (link)]. Briefly, TAK 242 (ApexBio, TX, USA) was dissolved in 10 % dimethyl sulfoxide (DMSO) and further diluted in saline to 1 mg/ml for intraperitoneal injection. To study the preventive effect, mice were treated with either TAK 242 (10 mg/kg b. w.) or vehicle 2 days prior to surgery, then three times a week until day 21 post-PSNL. For the reversal effect, TAK 242 treatment (10 mg/kg b. w.) started at day 17 post-PSNL and was continued for three times a week until day 38 post-PSNL, for a duration of 21 days.

Oladiran O., Shi X.Q., Yang M., Fournier S, & Zhang J. (2021). Inhibition of TLR4 signaling protects mice from sensory and motor dysfunction in an animal model of autoimmune peripheral neuropathy. Journal of Neuroinflammation, 18, 77.

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