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MRT67307

MRT67307

品 牌 MCE
C A S 号 1190378-57-4
货 号 HY-13018
规 格 5mg
价 格(元) 730.00
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货号 规格 价格
HY-13018 5mg 730.00
HY-13018 10mg 1300.00
HY-13018 50mg 4990.00
HY-13018 100mg 6500.00

产品说明


MRT67307是IKKe和TBK-1的双重抑制剂。IKKe和TBK-1介导IRF3的磷酸化。



MRT67307的生物活性


MRT67307 is a dual inhibitor of the IKKe and TBK-1. IKKe and TBK-1 mediate the phosphorylation of interferon regulatory factor 3 (IRF3).
IC50 value:
Target: IKKe/TBK1

化学信息


分子量 464.6 储存条件 参考CoA中推荐的条件进行储存。
分子式 C₂₆H₃₆N₆O₂
CAS号 1190378-57-4
溶剂/溶解度 10 mM in DMSO

相关文献


[1]. Clark K et al. Novel cross-talk within the IKK family controls innate immunity. Biochem J. 2011 Feb 15;434(1):93-104.
Abstract
Members of the IKK {IκB [inhibitor of NF-κB (nuclear factor κB)] kinase} family play a central role in innate immunity by inducing NF-κB- and IRF [IFN (interferon) regulatory factor]-dependent gene transcription programmes required for the production of pro-inflammatory cytokines and IFNs. However, the molecular mechanisms that activate these protein kinases and their complement of physiological substrates remain poorly defined. Using MRT67307, a novel inhibitor of IKK?/TBK1 (TANK {TRAF [TNF (tumour-necrosis-factor)-receptor-associated factor]-associated NF-κB activator}-binding kinase 1) and BI605906, a novel inhibitor of IKKβ, we demonstrate that two different signalling pathways participate in the activation of the IKK-related protein kinases by ligands that activate the IL-1 (interleukin-1), TLR (Toll-like receptor) 3 and TLR4 receptors. One signalling pathway is mediated by the canonical IKKs, which directly phosphorylate and activate IKK? and TBK1, whereas the second pathway appears to culminate in the autocatalytic activation of the IKK-related kinases. In contrast, the TNFα-induced activation of the IKK-related kinases is mediated solely by the canonical IKKs. In turn, the IKK-related kinases phosphorylate the catalytic subunits of the canonical IKKs and their regulatory subunit NEMO (NF-κB essential modulator), which is associated with reduced IKKα/β activity and NF-κB-dependent gene transcription. We also show that the canonical IKKs and the IKK-related kinases not only have unique physiological substrates, such as IκBα, p105, RelA (IKKα and IKKβ) and IRF3 (IKK? and TBK1), but also have several substrates in common, including the catalytic and regulatory (NEMO and TANK) subunits of the IKKs themselves. Taken together, our studies reveal that the canonical IKKs and the IKK-related kinases regulate each other by an intricate network involving phosphorylation of their catalytic and regulatory (NEMO and TANK) subunits to balance their activities during innate immunity.