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Chemical Structure| 702675-74-9 Chemical Structure| 702675-74-9

Structure of BX795
CAS No.: 702675-74-9

Chemical Structure| 702675-74-9

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BX795 is a potent and selective inhibitor of PDK1 with an IC50 of 6 nM. It also effectively inhibits TBK1 and IKKε with IC50 values of 6 nM and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, though it has lower selectivity over enzymes such as PKA, PKC, c-Kit, and GSK3β. Additionally, BX795 modulates autophagy.

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Product Details of BX795

CAS No. :702675-74-9
Formula : C23H26IN7O2S
M.W : 591.47
SMILES Code : O=C(NCCCNC1=C(C=NC(NC2=CC=CC(NC(N3CCCC3)=O)=C2)=N1)I)C4=CC=CS4
MDL No. :MFCD12546134
InChI Key :VAVXGGRQQJZYBL-UHFFFAOYSA-N
Pubchem ID :10077147

Safety of BX795

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of BX795

PI3K-AKT
pyroptosis
TLR

Isoform Comparison

Biological Activity

Target
  • PDK1

    PDK-1, IC50:6 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Human macrophages 10 µM 30 minutes Inhibiting TBK1 disrupts HMPV-induced IRF1 expression, highlighting its importance in the immune response. PMC8264192
Human Corneal Epithelial cells (HCEs) 10 μM 24 hours To evaluate the prophylactic efficacy of BX795 against HSV-1 infection, results showed that BX795 pre-treatment significantly suppressed HSV-1 infection. PMC7268978
iPSC-derived neurons 1 μM 14 days BX795 significantly restores disease-associated neurodegenerative phenotypes, including supporting neuritic growth, reducing αSyn protein aggregation, and restoring axonal pathology PMC8837749
SH-SY5Y neuroblastoma cells 1 μM BX795 restricts excessive protein synthesis and facilitates autophagy by inhibiting the mTORC1 pathway PMC8837749
human corneal epithelial cells 10 μM 24 hours BX795 dose-dependently inhibited HSV-1 infection, showing maximum antiviral activity at 10 μM with an IC50 value of 5.0 ±0.5 μM. PMC7540910
mouse embryonic fibroblasts 10 μM BX795 exhibited antiviral activity in both wild-type and TBK1 knockout MEFs, with stronger activity in wild-type cells. PMC7540910

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL6 mice C57BL6 mice Topical administration 10 μM 3 times daily for 4 weeks To evaluate the prophylactic efficacy and tolerability of BX795 against HSV-1 infection in murine corneas, results showed that BX795 significantly reduced HSV-1 infection with no detectable toxicity or inflammation. PMC7268978
BALB/c mice corneal HSV-1 infection model topical administration 10 μM single dose, observed for 9 days Topical application of BX795 significantly suppressed corneal HSV-1 infection in mice, reduced viral titers, and prevented virus transmission to the trigeminal ganglia. PMC7540910

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.69mL

0.34mL

0.17mL

8.45mL

1.69mL

0.85mL

16.91mL

3.38mL

1.69mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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