Toll-like receptor 4 (TLR4) signaling inhibitor. Binds to intracellular domain of TLR4. Inhibits LPS-induced cytokine productionin vitro(IC50values are 1.3, 1.3 and 3.2 nM for IL-6, TNFα and NO production). Reduces lesion volume in a mouse model of cerebr
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
ANTAGONIST
Mechanism of action
Antagonist of TLR4
Product Description
TAK-242 is a cell-permeable compound that selectively binds to Cys747 of TLR4 and selectively disrupts its interaction with adaptor molecules TIRAP and TRAM.
1.Ailin Yang, Haitao Fan, Yanan Zhao, Xiaonan Chen, Zhixiang Zhu, Xiaojun Zha, Yunfang Zhao, Xingyun Chai, Jun Li, Pengfei Tu, Zhongdong Hu. (2019) An immune-stimulating proteoglycan from the medicinal mushroom Huaier up-regulates NF-κB and MAPK signaling via Toll-like receptor 4. JOURNAL OF BIOLOGICAL CHEMISTRY, 294 (8):(2628-5268). [PMID:30602571][10.1074/jbc.RA118.005477]
References
1.Yamada M, Ichikawa T, Ii M, Sunamoto M, Itoh K, Tamura N, Kitazaki T. (2005) Discovery of novel and potent small-molecule inhibitors of NO and cytokine production as antisepsis agents: synthesis and biological activity of alkyl 6-(N-substituted sulfamoyl)cyclohex-1-ene-1-carboxylate.. J Med Chem, 48 (23):(7457-67). [PMID:16279805][10.1021/op500134e]
2.Ii M, Matsunaga N, Hazeki K, Nakamura K, Takashima K, Seya T, Hazeki O, Kitazaki T, Iizawa Y. (2006) A novel cyclohexene derivative, ethyl (6R)-6-[N-(2-Chloro-4-fluorophenyl)sulfamoyl]cyclohex-1-ene-1-carboxylate (TAK-242), selectively inhibits toll-like receptor 4-mediated cytokine production through suppression of intracellular signaling.. Mol Pharmacol, 69 (4):(1288-95). [PMID:16373689][10.1021/op500134e]
3.Ailin Yang, Haitao Fan, Yanan Zhao, Xiaonan Chen, Zhixiang Zhu, Xiaojun Zha, Yunfang Zhao, Xingyun Chai, Jun Li, Pengfei Tu, Zhongdong Hu. (2019) An immune-stimulating proteoglycan from the medicinal mushroom Huaier up-regulates NF-κB and MAPK signaling via Toll-like receptor 4. JOURNAL OF BIOLOGICAL CHEMISTRY, 294 (8):(2628-5268). [PMID:30602571][10.1074/jbc.RA118.005477]
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K2401544