
T6167923 B
CAS No. 2437475-16-4
T6167923 B ( —— )
产品货号. M33136 CAS No. 2437475-16-4
T6167923 是一种选择性的 MyD88 依赖型信号通路的抑制剂。T6167923 直接与 MyD88 的 Toll/IL1 受体 (TIR) 结构域结合,破坏 MyD88 的同二聚体形成。T6167923 抑制 NF-κB 驱动的葡萄球菌肠毒素AP (SEAP) 活性,并且改善抗炎活性,对 IFN-γ,IL-1β,IL-6 和 TNF-α 的 IC50s 分别为 2.7 ?μM,2.9 μM,2.66 μM 和 2.66 μM。
纯度: >98% (HPLC)






规格 | 价格/人民币 | 库存 | 数量 |
2MG | ¥2364 | 有现货 |
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5MG | ¥3739 | 有现货 |
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10MG | ¥5612 | 有现货 |
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25MG | ¥9619 | 有现货 |
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50MG | ¥13059 | 有现货 |
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100MG | ¥17213 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称T6167923 B
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注意事项本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
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产品简述T6167923 是一种选择性的 MyD88 依赖型信号通路的抑制剂。T6167923 直接与 MyD88 的 Toll/IL1 受体 (TIR) 结构域结合,破坏 MyD88 的同二聚体形成。T6167923 抑制 NF-κB 驱动的葡萄球菌肠毒素AP (SEAP) 活性,并且改善抗炎活性,对 IFN-γ,IL-1β,IL-6 和 TNF-α 的 IC50s 分别为 2.7 ?μM,2.9 μM,2.66 μM 和 2.66 μM。
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产品描述T6167923 is a selective inhibitor of MyD88-dependent signaling pathways. T6167923 directly binds to Toll/IL1 receptor (TIR) domain of MyD88 and disrupts MyD88 homodimeric formation. T6167923 inhibits NF-κB driven Staphylococcus enterotoxin AP (SEAP) activity, and improves anti-inflammatory activity with IC50s of 2.7 ?μM, 2.9 μM, 2.66 μM and 2.66 μM for IFN-γ, IL-1β, IL-6 and TNF-α, respectively.
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体外实验T6167923 (0-500 μM; 20 h) inhibits the pro-inflammatory cytokine response of staphylococcal enterotoxin B (SEB) in peripheral blood mono nuclear cells.T6167923 (10-500 μM; 2 h) inhibits secreted alkaline phosphatase response (SEAP) expression in HEK 293T cells.T6167923 (100 μM; 16 h) binds to TIR protein and reduced the inhibitory effect onMyD88-signaling.T6167923 (1-500 μM; 13 h) inhibits full-length MyD88 homodimeric formation.Cell Viability Assay Cell Line:Peripheral blood mono nuclear cells Concentration:0-500 μM Incubation Time:20 hours Result:Dose-dependently attenuated the response of SEB to TNF-α, INF-γ, IL-6, and IL-1β with IC50s of 2.66, 2.7, 2.66 and 2.9 μM in peripheral blood mono nuclear cells.Cell Viability Assay Cell Line:HEK 293T cell line Concentration:10-500 μM Incubation Time:2 hours Result:Dose-dependently inhibited lipo-polysaccharide (LPS) induced MyD88-mediated NF-kB driven SEAP expression in HEK 293T cells with IC50s in the range of 40–50 μM.Cell Viability Assay Cell Line:HEK 293T cell line Concentration:100 μM Incubation Time:16 hours Result:Specifically targeted MyD88 and dose-denpendently with TIR protein to reduced the inhibitory effect of MyD88-signaling.Western Blot Analysis Cell Line:HEK 293-I3A cells with MyD88 knockout Concentration:1-500 μM Incubation Time:13 hours Result:Dose-dependently inhibited TIR domain-mediated dimerization of full-length MyD88 and the recombinant TIR domain protein.
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体内实验T6167923 (0.17 and 1 mg; i.p. once) survives the mice from intoxication with SEB and LPS injection.Animal Model:16-20 week-old BALB/c mice with LPS potentiation model Dosage:0.17 and 1 mg Administration: Intraperitoneal injection; 0.17 and 1 mg once Result:Dose-dependently showed a therapeutic efficacy against SEB intoxication.
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同义词——
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通路Immunology/Inflammation
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靶点MyD88
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受体MyD88
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研究领域——
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适应症——
化学信息
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CAS Number2437475-16-4
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分子量458.39
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分子式C17H20BrN3O3S2
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纯度>98% (HPLC)
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溶解度In Vitro:?DMSO 中的溶解度 : 250 mg/mL (545.39 mM; 超声助溶 ) H2O 中的溶解度 : < 0.1 mg/mL (insoluble)
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SMILESC[C@H](NC(=O)N1CCN(CC1)S(=O)(=O)c1cccc(Br)c1)c1cccs1
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Saqib U, et al. Identifying the inhibition of TIR proteins involved in TLR signalling as an anti-inflammatory strategy. SAR QSAR Environ Res. 2018 Apr;29(4):295-318.?
产品手册




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T6167923
T6167923 (T-6167923) 是一种 MyD88 依赖性信号通路的小分子抑制剂,可破坏 MyD88 同二聚体的形成;抑制 SEB 诱导的 PBMC 细胞因子产生抑制,IC50 为 2-10 uM,还抑制 SEA 诱导的促炎细胞因子产生,在原代细胞中高达 100 uM 无毒性;特异性抑制 TIR 结构域介导的全长 MyD88 以及重组 TIR 结构域蛋白的二聚化;针对 SEB 中毒的剂量依赖性体内治疗效果。