| Bioactivity | TBK1-IN-1 is a potent and selective TANK binding kinase 1 (TBK1) inhibitor with an IC50 value of 22.4 nM. TBK1-IN-1 inhibits TBK1 downstream target genes cxcl10 and ifnβ expression. TBK1-IN-1 has anticancer activity[1]. | ||||||||||||
| Invitro | TBK1-IN-1 (compound 7l; 0.1 and 1 μM; 2 h) inhibitsTBK1 downstream target genes cxcl10 and ifnβ expression in THP1 and RAW264.7 cells induced by poly (I:C) and lipopolysaccharide, respectively[1].TBK1-IN-1 (1-100 μM; 72 h) has moderate antiproliferative activities against A549 and LLC with IC50 values of 17.6 and 9.4 μM, respectively[1]. Cell Viability Assay[1] Cell Line: | ||||||||||||
| Name | TBK1-IN-1 | ||||||||||||
| Formula | C27H35N7O2 | ||||||||||||
| Molar Mass | 489.61 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Vassilev LT, et, al. In vivo activation of the p53 pathway by small-molecule antagonists of MDM2. Science. 2004 Feb 6;303(5659):844-8. |