T6167923
目录号: PL07597 纯度: ≥99%
CAS No. :2437475-16-4
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中文名称
T6167923
英文名称
T6167923
英文别名
T6167923
Cas No.
2437475-16-4
分子式
C17N3O3S2BrH20
分子量
458.39
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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。
生物活性
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 IC 50 s 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.
性状
Solid
IC50 & Target[1][2]
IC50: 2.7?μM (IFN-γ), 2.9 μM (IL-1β), 2.66 μM (IL-6), 2.66 μM (TNF-α)
体外研究(In Vitro)
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 on MyD88-signaling.
T6167923 (1-500 μM; 13 h) inhibits full-length MyD88 homodimeric formation. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
T6167923 (0.17 and 1 mg; i.p. once) survives the mice from intoxication with SEB and LPS injection. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 16-20 week-old BALB/c mice with LPS
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 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.
[2]. Olson MA, et al. Discovery of small molecule inhibitors of MyD88-dependent signaling pathways using a computational screen. Sci Rep. 2015 Sep 18;5:14246.
溶解度数据
In Vitro: DMSO : 250 mg/mL (545.39 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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