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|
|Cell Lines||HEC-1-A cells|
|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|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 90 mg/mL|
|Related PDK1 Products|
BX517 is a potent and selective inhibitor of PDK1 with IC50 of 6 nM.
NVP-BAG956 is a potent, ATP-competitive and selective dual PDK1 and class I PI 3-K inhibitor (IC50 values are 245, 56, 446, 35 and 117 nM for PDK1 and PI 3-K p110 -α, -β, -δ, and -γ respectively).
HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM.
BX912 is a selective potent PDK1 inhibitor with IC50 of 12 nM.
GSK2334470 is a highly specific and potent inhibitor of PDK1 with IC50 of 10 nM.
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