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BX-795

Cat. No. M2310
BX-795 Structure
Size Price Availability Quantity
10mg USD 110 In stock
25mg USD 230 In stock
50mg USD 360 In stock
100mg USD 550 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 591.47
Formula C23H26IN7O2S
CAS Number 702675-74-9
Purity >99%
Solubility DMSO 90 mg/mL
Storage at -20°C
Customer Product Validations & Biological Datas
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
Rating
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: BX-795 supplier, PDK1, inhibitors

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