BX-795 is a potent and relatively specific TBK1 and IKKε inhibitor with an IC50 of 6 and 41 nM. BX-795 also inhibit other kinases such as PDK1, Aurora B, ERK8, and MARK3 with IC50 of 111, 31, 140 and 81 nM, respectively. BX-795 prevents TBK1- and IKKε-mediated activation of IRF3 and production of IFN-β. BX-795 also suppresses the activities of MARK1, MARK2, MARK4, NUAK1, VEGFR, MLK1, MLK2, MLK3 with IC50 of 55, 53, 19, 5, 157, 50, 46 and 42 nM, respectively. BX-795 blocks the secretion of IFN-β from macrophages whether stimulated by LPS, a TLR4 agonist.
 |
Source | Acta Pharmacol Sin (2017). Figure 2. BX-795 |
| Method | Western Blot | |
| Cell Lines | HEC-1-A cells | |
| Concentrations | 25 μmol/L | |
| Incubation Time | 24 h | |
| Results | As shown in Figure 2, when cells were pretreated with BX-795, ICP0 and ICP27 mRNA transcription of HSV-1 (Figure 2D) and HSV-2 (Figure 2E) increased in a dose-dependent manner at an early stage of viral infection |
| Molecular Weight | 591.47 |
| Formula | C23H26IN7O2S |
| CAS Number | 702675-74-9 |
| Solubility (25°C) | DMSO 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Manzar Alam, et al. A review on the role of TANK-binding kinase 1 signaling in cancer
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