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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.
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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 |
[2] Manzar Alam, et al. A review on the role of TANK-binding kinase 1 signaling in cancer
| Related PDK1 Products |
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| MP7
MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor. |
| PDKtide
PDKtide is a biological active peptide. |
| PDK1-IN-RS2
PDK1-IN-RS2 is a mimic of peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor with a Kd of 9 μM. PDK1-IN-RS2 suppresses the activation of the downstream kinases S6K1 by PDK1. |
| PS47
PS47 is an inactive E-isomer of PS48. PS48 is an activator of PDK1. PS47 can be used as a negative control for PS48. |
| PS210
PS210 is a potent activator of PDK1 that binds to the PIF-pocket and allosterically modulates the active site of PDK1. |
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