Cat. No.: HY-10514

BX795

41 Cited Publications

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Based on 41 publication(s) in Google Scholar

BX795 is a potent and selective inhibitor of PDK1, with an IC₅₀ of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKε, with an IC₅₀ of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy.

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Pureté: 99.84%
CAS No.: 702675-74-9
Formule: C₂₃H₂₆IN₇O₂S
Masse moléculaire:591.47

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

BX795 Chemical Structure

CAS No.: 702675-74-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (41)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]^[2]

PDK1

6 nM (IC₅₀)

TBK1

6 nM (IC₅₀)

IKKε

41 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform IKK :

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	CC₅₀	46 μM Compound: 73; BX795	Cytotoxicity against human HeLa cells Cytotoxicity against human HeLa cells	[PMID: 33539089]

In Vitro

BX795 effectively blocks PDK1 activity in PC-3 cells, as shown by their ability to block phosphorylation of S6K1, Akt, PKCδ, and GSK3β. BX795 potently inhibits tumor cell growth on plastic with IC₅₀ of 1.6, 1.4, and 1.9 μM for MDA-468, HCT-116, and MiaPaca cells, respectively.
In soft agar, BX795 displays higher growth inhibition with IC₅₀ of 0.72, and 0.25 μM for MDA-468, and PC-3 cells, respectively^[1].
In addition, BX795, as an inhibitor of the TBK1/IKKε, blocks TBK1- and IKKε-mediated activation of IRF3 and production of IFN-β^[2]. In platelet physiological responses, BX795 produces inhibitory effect on 2-MeSADP-induced or collagen-induced aggregation, ATP secretion, and thromboxane generation^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 702675-74-9
Appearance Solid
Masse moléculaire 591.47
Formule C₂₃H₂₆IN₇O₂S
Color White to light brown
SMILES

O=C(NCCCNC1=C(C=NC(NC2=CC=CC(NC(N3CCCC3)=O)=C2)=N1)I)C4=CC=CS4
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (41)

All WB

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Journal Impact Factor

Nature

Clathrin-associated AP-1 controls termination of STING signalling. [Abstract]

2022 Oct;610(7933):761-767. PMID: 36261523

BX795 purchased from MedChemExpress. Usage Cited in: Nature. 2022 Oct;610(7933):761-767. [Abstract]

HeLa cells pretreated with DMSO or 2 µM BX795 for 24 h are stimulated with 2.5 µM diABZI or not and analysed by Western blot.
Immunity

A chemical agonist and the Golgi-resident lipid PI4P activate STING by inducing transmembrane helix rearrangement. [Abstract]

2025 Dec 5:S1074-7613(25)00506-0. PMID: 41352342
Autophagy

TRIM21-mediated ubiquitination of SQSTM1/p62 abolishes its Ser403 phosphorylation and enhances palmitic acid cytotoxicity. [Abstract]

2025 Jan;21(1):178-190. PMID: 39172027
Autophagy

HSF1 stress response pathway regulates autophagy receptor SQSTM1/p62-associated proteostasis. [Abstract]

2017 Jan 2;13(1):133-148. PMID: 27846364

BX795 purchased from MedChemExpress. Usage Cited in: Autophagy. 2017 Jan 2;13(1):133-148. [Abstract]

HeLa cells are treated with a BX795 TBK1 inhibitor (1 μM) and MG132 (10 μM) for 12 h. Cell lysates are analyzed by immunoblot analysis. Band intensities are measured, and phosphorylated-SQSTM1 values are normalized to total SQSTM1. The combined MG132/BX795 treatment results in a 90% reduction in S403 phosphorylation but has no effect on S349 phosphorylation.
Nat Commun

IKKε and TBK1 prevent RIPK1 dependent and independent inflammation. [Abstract]

2024 Jan 2;15(1):130. PMID: 38167258
Mol Cell

Asparagine sensing by TBK1 controls its phase separation to drive antiviral innate immune responses. [Abstract]

2026 Feb 19;86(4):722-739.e8. PMID: 41653919
Mol Cell

STING mediates lysosomal quality control and recovery through its proton channel function and TFEB activation in lysosomal storage disorders. [Abstract]

2025 Mar 27:S1097-2765(25)00201-1. PMID: 40185098
Adv Sci (Weinh)

EGR Proteins Mediate Interferon-Independent Anti-HSV-1 Responses Through Viral and Host Targets. [Abstract]

2026 Mar;13(13):e15546. PMID: 41486724
Cell Mol Biol Lett

Inhibition of SQSTM1 S403 phosphorylation facilitates the aggresome formation of ubiquitinated proteins during proteasome dysfunction. [Abstract]

2023 Oct 24;28(1):85. PMID: 37872526
Pharmacol Res

Fluvoxamine alleviates bleomycin-induced lung fibrosis via regulating the cGAS-STING pathway. [Abstract]

2023 Jan:187:106577. PMID: 36435270
J Orthop Translat

TBK1 pharmacological inhibition mitigates osteoarthritis through attenuating inflammation and cellular senescence in chondrocytes. [Abstract]

2024 Jun 28:47:207-222. PMID: 39040492
Cell Chem Biol

Identifying enhancers of innate immune signaling as broad-spectrum antivirals active against emerging viruses. [Abstract]

2022 Jul 21;29(7):1113-1125.e6. PMID: 35728599
EMBO J

Basal IFN-λ2/3 expression mediates tight junction formation in human epithelial cells. [Abstract]

2025 Sep 1. PMID: 40890487
J Anim Sci Biotechnol

Genome-wide identification of functional enhancers and their potential roles in pig breeding. [Abstract]

2022 Jul 4;13(1):75. PMID: 35781353
Cell Rep

In vivo G-CSF treatment activates the GR-SOCS1 axis to suppress IFN-γ secretion by natural killer cells. [Abstract]

2022 Sep 13;40(11):111342. PMID: 36103837
mLife

Potential antiviral effects of the marine probiotic Paraliobacillus zengyii on the respiratory syncytial virus. [Abstract]

2025 Jun 18;4(3):249-258. PMID: 40600055
Mol Cell Proteomics

Functional Proteomics and Deep Network Interrogation Reveal a Complex Mechanism of Action of Midostaurin in Lung Cancer Cells. [Abstract]

2018 Dec;17(12):2434-2447. PMID: 30217950

BX795 purchased from MedChemExpress. Usage Cited in: Mol Cell Proteomics. 2018 Dec;17(12):2434-2447. [Abstract]

Relative A427 cell counts upon 96 hrs siRNA-mediated knockdown of PDPK1 and/or AURKA and/or 72 hrs treatment with 250 nM BX795.
J Cell Biol

DNA damage promotes microtubule dynamics through a DNA-PK-AKT axis for enhanced repair. [Abstract]

2021 Feb 1;220(2):e201911025. PMID: 33404607
Cancer Immunol Immunother

Therapeutic potential of anti-ErbB3 chimeric antigen receptor natural killer cells against breast cancer. [Abstract]

2025 Jan 3;74(2):73. PMID: 39751931
Transl Oncol

BX-795 inhibits neuroblastoma growth and enhances sensitivity towards chemotherapy. [Abstract]

2022 Jan;15(1):101272. PMID: 34823094
Oncol Rep

PIK3CA mutation affects the proliferation of colorectal cancer cells through the PI3K-MEK/PDK1-GPT2 pathway. [Abstract]

2022 Jan;47(1):11. PMID: 34751411
iScience

Suppression of TREX1 deficiency-induced cellular senescence and interferonopathies by inhibition of DNA damage response. [Abstract]

2023 Jun 10;26(7):107090. PMID: 37416470
Poultry Sci

BX795, a kinase inhibitor, inhibit duck plague virus infection via targeting US3 kinase. [Abstract]

2023 May;102(5):102597. PMID: 36931072
Microbiol Spectr

Replication of Porcine Astrovirus Type 1-Infected PK-15 Cells In Vitro Affected by RIG-I and MDA5 Signaling Pathways. [Abstract]

2023 Jun 15;11(3):e0070123. PMID: 37140381
J Biotechnol

Interferon inhibitors increase rAAV production in HEK293 cells. [Abstract]

2025 Mar:399:9-18. PMID: 39824361
J Cell Sci

Alpha-synuclein fibrils recruit TBK1 and OPTN to lysosomal damage sites and induce autophagy in microglial cells. [Abstract]

2018 Nov 30;131(23). pii: jcs226241. PMID: 30404831
Vet Res

Duck STING mediates antiviral autophagy directing the interferon signaling pathway to inhibit duck plague virus infection. [Abstract]

2024 Jun 28;55(1):83. PMID: 38943190
J Proteome Res

Quantitative Proteomics Reveals a Novel Role of the E3 Ubiquitin-Protein Ligase FANCL in the Activation of the Innate Immune Response through Regulation of TBK1 Phosphorylation during Peste des Petits Ruminants Virus Infection. [Abstract]

2021 Aug 6;20(8):4113-4130. PMID: 34289691
Viruses

Screening and Identification of Lujo Virus Inhibitors Using a Recombinant Reporter Virus Platform. [Abstract]

2021 Jun 28;13(7):1255. PMID: 34203149
Appl Biochem Biotechnol

Angiopoietin 1 Relieves Osteolysis by Promoting Macrophage Mitophagy Through the TBK1-SQSTM1 Pathway to Inhibit AIM2 Inflammasome-Mediated Pyroptosis. [Abstract]

2024 Nov;196(11):7908-7927. PMID: 38662322
Tissue Cell

Bi-magnolignan suppresses triple-negative breast cancer by triggering TBK1-dependent mitophagy. [Abstract]

2026 Apr 22:102:103550. PMID: 42035609
Fitoterapia

The antagonism between apigenin and protoapigenone to the PDK-1 target in Macrothelypteris torresiana. [Abstract]

2019 Apr:134:14-22. PMID: 30731149

BX795 purchased from MedChemExpress. Usage Cited in: Fitoterapia. 2019 Apr:134:14-22. [Abstract]

BT474 cells are exposed to protoapigenone, apigenin and BX-795 using different administration combination and analyzed by Western blot, β-actin was used as internal control.

BX795 purchased from MedChemExpress. Usage Cited in: Fitoterapia. 2019 Apr:134:14-22. [Abstract]

MDA-MB-231 cells are exposed to protoapigenone, apigenin and BX-795 using different administration combination and analyzed by Western blot, β-actin was used as internal control.
PLoS One

Drug repositioning for pan-cancers of the digestive system: Identification of amonafide and BX795 as potential therapeutics via integrative Omics analysis. [Abstract]

2025 Jun 16;20(6):e0325700. PMID: 40522954
Res Sq

2026 May 25.
bioRxiv

2026 Apr 23.
bioRxiv

2026 Mar 12.
bioRxiv

2025 Dec 25.
Res Sq

2025 Oct 6.
University of Greifswald

2025.
Oxid Med Cell Longev

Apelin/APJ-Manipulated CaMKK/AMPK/GSK3 β Signaling Works as an Endogenous Counterinjury Mechanism in Promoting the Vitality of Random-Pattern Skin Flaps. [Abstract]

2021 Jan 25:2021:8836058. PMID: 33574981
Patent

US20200268864A1.

Solvant et solubilité

In Vitro:

DMSO : 33.33 mg/mL (56.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6907 mL

8.4535 mL

16.9070 mL

5 mM

0.3381 mL

1.6907 mL

3.3814 mL

10 mM

0.1691 mL

0.8454 mL

1.6907 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.23 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.23 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Kinase Assay^[1]

PDK1 is assayed in a direct kinase assay and a coupled assay format measuring PDK1- and PtdIns-3,4-P2-mediated activation of AKT2. For the coupled assay, the final assay mixture (60 μL) contained: 15 mM MOPS, pH 7.2, 1 mg/mL bovine serum albumin, 18 mM β-glycerol phosphate, 0.7 mM dithiothreitol, 3 mM EGTA, 10 mM MgOAc, 7.5 μM ATP, 0.2 μCi of [γ-³³P]ATP, 7.5 μM biotinylated peptide substrate (biotin-ARRRDGGGAQPFRPRAATF), 0.5 μL of PtdIns-3,4-P2-containing phospholipid vesicles, 60 pg of purified recombinant human PDK1, and 172 ng of purified recombinant human AKT2. After incubation for 2 h at room temperature, the biotin-labeled peptide is captured from 10 μL of the assay mixture on streptavidin-coated SPA beads, and product formation is measured by scintillation proximity in a Wallac MicroBeta counter. The product formed is proportional to the time of incubation and to the amount of PDK1 and inactive AKT2 added. PDK1 is added at suboptimal levels so that the assay could sensitively detect inhibitors of AKT2 activation as well as direct inhibitors of PDK1 or AKT2. To measure PDK1 activity directly, the final assay mixture (60 μL) contained 50 mM Tris-HCl, pH 7.5, 0.1 mM EGTA, 0.1 mM EDTA, 0.1% β-mercaptoethanol, 1 mg/mL bovine serum albumin, 10 mM MgOAc, 10 μM ATP, 0.2 μCi of [γ-³³P]ATP, 7.5 μM substrate peptide (H2N-ARRRGVTTKTFCGT), and 60 ng of purified recombinant human PDK1. After 4 h at room temperature, we add 25 mM EDTA and spotted a portion of the reaction mixture on Whatman P81 phosphocellulose paper. The filter paper is washed three times with 0.75% phosphoric acid and once with acetone. After drying, the filter-bound labeled peptide is quantified using a Fuji phosphorimager.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[1]

Cells seeded at a low density (1,500-3,000 cells/well, 0.1 mL/well, 96-well plates) are incubated overnight. Compound treatments are made by adding 10 μL/well of the compound in 1% dimethyl sulfoxide and growth medium (final concentration of dimethyl sulfoxide, 0.1%), followed by brief shaking. Treated cells are incubated for 72 hours, and viability is measured by the addition of 10 μL of the metabolic dye WST-1. The WST-1 signal is read in a plate reader at 450 nm, and a no cell, or zero time cell, background is subtracted to calculate the net signal. Results are reported as the average±S.E. of two or more replicates.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Feldman RI, et al. Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005 May 20;280(20):19867-74. [Content Brief]

[2]. Clark K, et al. 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 May 22;284(21):141 [Content Brief]

[3]. Dangelmaier C, et al. PDK1 selectively phosphorylates Thr(308) on Akt and contributes to human platelet functional responses. Thromb Haemost. 2014 Mar 3;111(3):508-17. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.6907 mL	8.4535 mL	16.9070 mL	42.2676 mL
	5 mM	0.3381 mL	1.6907 mL	3.3814 mL	8.4535 mL
	10 mM	0.1691 mL	0.8454 mL	1.6907 mL	4.2268 mL
	15 mM	0.1127 mL	0.5636 mL	1.1271 mL	2.8178 mL
	20 mM	0.0845 mL	0.4227 mL	0.8454 mL	2.1134 mL
	25 mM	0.0676 mL	0.3381 mL	0.6763 mL	1.6907 mL
	30 mM	0.0564 mL	0.2818 mL	0.5636 mL	1.4089 mL
	40 mM	0.0423 mL	0.2113 mL	0.4227 mL	1.0567 mL
	50 mM	0.0338 mL	0.1691 mL	0.3381 mL	0.8454 mL

Keywords

BX795

41 Cited Publications

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BX795

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

NF-κB Signaling Compound Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Mitochondria-Targeted Compound Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) BX795

Voir tous les produits spécifiques à Isoform IKK

Activité biologique

Chemical Information

Publications (41)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

BX795 Related Classifications

HY-10514 Related Classifications