TPCA-1 (GW683965; GW-683965; TPCA1; TPCA 1; IKK2 Inhibitor IV)是一种高效的IKK-2抑制剂,其IC50为17.9 nM,抑制NF-κB信号通路,其对IKK-2比对IKK-1的选择性高20多倍。TPCA-1抑制STAT3磷酸化,促进细胞凋亡。
参考文献
[1] Sachse F, et al. IKK-2 inhibitor TPCA-1 represses nasal epithelial inflammation in vitro.Rhinology. 2011 Jun;49(2):168-73.
[2] Nan J, et al. TPCA-1 is a direct dual inhibitor of STAT3 and NF-κB and regresses mutant EGFR-associated human non-small cell lung cancers. Mol Cancer Ther. 2014 Mar;13(3):617-29.
[3] Podolin PL, et al. Attenuation of murine collagen-induced arthritis by a novel, potent, selective small molecule inhibitor of IkappaB Kinase 2, TPCA-1 (2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide), occurs via reduction of proinflamm.
冰袋运输。粉末直接保存于-25~-15℃,有效期2年。建议干燥保存,避免反复冻融。