BX795 |
Catalog No.GC11573
One-Click Copy Product Info
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BX795 is an inhibitor of 3-phosphoinositide-dependent protein kinase 1 (PDK1), with an IC50 value of 11nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 702675-74-9
Sample solution is provided at 25 µL, 10mM.
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BX795 is an inhibitor of 3-phosphoinositide-dependent protein kinase 1 (PDK1), with an IC50 value of 11nM. BX795 blocks the PDK1/Akt signaling pathway in tumor cells, inhibits the anchorage-dependent growth of various tumor cell lines in vitro, or induces their apoptosis. BX795 also inhibits TANK-binding kinase 1 (TBK1) and IκB kinase ε (IKKε), with the IC50 values of 6 and 41nM, respectively. BX795 potently inhibits diverse HSV-1 strains across transformed human cells, primary corneal cultures (human and animal), and murine ocular surface models. BX795 shows substantial promise as a broad-spectrum human antiviral[1][2][3].
In vitro, BX795 (0.1-10µM; 18h) dose-dependently inhibited the levels of phospho-Thr308-Akt and phospho-Thr389-S6K1 in PC-3 cells[1]. BX795 potently inhibited the growth of PC-3 cells in soft agar, displaying IC50 value of 0.25µM[1]. BX795 (1µM; 60min) blocks TBK1- and IKKε-mediated Activation of IRF3 and Production of IFN-β in HEK293-TLR3 cells[2]. BX795 (3.125-25μM; 24h) inhibited the replication of HSV-1 (HF) and HSV-2 (G) in HEC-1-A and Vero cells in a dose-dependent manner[3].
In vivo, BX795 (20mg/kg; i.p.; every other day for 8 doses) significantly reduced brain metastasis and prolonged survival in brain-metastatic mouse models[4]. BX795 (0.0473mg/kg; 10μL; twice a week for 8 weeks）alleviated cartilage degeneration, synovitis, and OA pain, and improved cartilage inflammation, senescence, and matrix metabolism in Destabilization of the Medial Meniscus (DMM)-induced mouse osteoarthritis models[5].
References:
[1] Feldman RI, Wu JM, Polokoff MA, et al. Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005;280(20):19867-19874. doi:10.1074/jbc.M501367200.
[2] Clark K, Plater L, Peggie M, Cohen P. Use of the pharmacological inhibitor BX795 to study the regulation and physiological roles of TBK1 and IkappaB kinase epsilon: a distinct upstream kinase mediates Ser-172 phosphorylation and activation. J Biol Chem. 2009;284(21):14136-14146.
[3] Su AR, Qiu M, Li YL, et al. BX-795 inhibits HSV-1 and HSV-2 replication by blocking the JNK/p38 pathways without interfering with PDK1 activity in host cells. Acta Pharmacol Sin. 2017;38(3):402-414.
[4] Khan F, Petrosyan E, Liu Y, et al. Microglial TBK1 Signaling Promotes Breast Cancer Brain Metastasis. Cancer Res. 2026;86(1):12-21.
[5] Lu R, Qu Y, Wang Z, et al. TBK1 pharmacological inhibition mitigates osteoarthritis through attenuating inflammation and cellular senescence in chondrocytes. J Orthop Translat. 2024;47:207-222.
| Cell experiment [1]: | |
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Cell lines |
PC-3 cells |
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Preparation Method |
PC-3 cells were treated with BX795 for 18h and analyzed its effects on a number of PDK1 targets using Western blotting. |
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Reaction Conditions |
0.1-10µM; 18h |
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Applications |
BX795 dose-dependently inhibited the levels of phospho-Thr308-Akt and phospho-Thr389-S6K1. |
| Animal experiment [2]: | |
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Animal models |
Brain metastatic mouse model (BCBM) |
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Preparation Method |
Developed a brain metastatic mouse model by intracarotid injection of MDA-MB-231-Br cells into the nude mice. Mice were treated with or without TBK1 inhibitor BX795 (20mg/kg; i.p.; every other day for 8 doses) beginning at day 8 post-intracranial injection. |
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Dosage form |
20mg/kg; i.p.; every other day for 8 doses |
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Applications |
BX795 significantly reduced brain metastasis and extended survival. BX795 treatment reduced metastatic outgrowth in the brain. |
References:[1] Feldman RI, Wu JM, Polokoff MA, et al. Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005;280(20):19867-19874. doi:10.1074/jbc.M501367200. [2] Khan F, Petrosyan E, Liu Y, et al. Microglial TBK1 Signaling Promotes Breast Cancer Brain Metastasis. Cancer Res. 2026;86(1):12-21. | |
| Cas No. | 702675-74-9 | SDF | |
| Chemical Name | N-[3-[[5-iodo-4-[3-(thiophene-2-carbonylamino)propylamino]pyrimidin-2-yl]amino]phenyl]pyrrolidine-1-carboxamide | ||
| Canonical SMILES | C1CCN(C1)C(=O)NC2=CC=CC(=C2)NC3=NC=C(C(=N3)NCCCNC(=O)C4=CC=CS4)I | ||
| Formula | C23H26IN7O2S | M.Wt | 591.48 |
| Solubility | ≥ 59.1mg/mL in DMSO with gentle warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6907 mL | 8.4534 mL | 16.9067 mL |
| 5 mM | 338.1 μL | 1.6907 mL | 3.3813 mL |
| 10 mM | 169.1 μL | 845.3 μL | 1.6907 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)