B022
Based on 19 publication(s) in Google Scholar
B022 is a potent and selective NF-κB-inducing kinase (NIK) inhibitor (Ki of 4.2 nM; IC50=15.1 nM). B022 protects liver from toxin-induced inflammation, oxidative stress, and injury. B022 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
For research use only. We do not sell to patients.
- Purity : 99.27%
- CAS No.: 1202764-53-1
- Formula: C19H16ClN5OS
- Molecular Weight:397.88
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) B022
More- Signal Transduct Target Ther. 2025 Oct 3;10(1):326. [Abstract]
- Immunity. 2025 Mar 11;58(3):585-600.e6. [Abstract]
- Nat Commun. 2022 Dec 16;13(1):7782. [Abstract]
- Nat Commun. 2022 Nov 12;13(1):6881. [Abstract]
- Adv Sci (Weinh). 2026 Apr;13(21):e18975. [Abstract]
- Cell Death Differ. 2024 Oct;31(10):1267-1284. [Abstract]
- J Neuroinflammation. 2025 Aug 26;22(1):206. [Abstract]
- J Neuroinflammation. 2025 Jan 24;22(1):17. [Abstract]
- Am J Transplant. 2024 Dec;24(12):2187-2198. [Abstract]
- Liver Int. 2024 Nov;44(11):2950-2963. [Abstract]
- Int J Pharm. 2022 Nov 25:628:122361. [Abstract]
- Int J Mol Sci. 2026 Apr 2;27(7):3232. [Abstract]
- Inflammation. 2025 Jul 5. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2024 Feb 11;1870(4):167066. [Abstract]
- Res Sq. 2026 Apr 10.
- University of Bonn. 2025.
- bioRxiv. 2025 Oct 1.
- bioRxiv. 2025 Jan 1.
- University of North Carolina at Chapel Hill. 2024.
Customer Validation & Images
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Flow Cytometry
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Cell Proliferation/Viability Assay
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WB
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Flow Cytometry
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IF
Biological Activity
Description
IC50 & Target
Ki: 4.2 nM (NF-κB-inducing kinase (NIK))[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Macrophage | IC50 |
58.6 μM
Compound: B022
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Anti-inflammatory activity in mouse macrophages extracted from abdominal activity assessed as inhibition of LPS-induced nitric oxide production at 1 uM measured after 22 hrs by Griess reagent assay relative to control
Anti-inflammatory activity in mouse macrophages extracted from abdominal activity assessed as inhibition of LPS-induced nitric oxide production at 1 uM measured after 22 hrs by Griess reagent assay relative to control
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[PMID: 38563549] |
In Vitro
B022 (0-5 μM; 12 hours; Hepa1 cells) treatment suppresses NIK-induced p52 formation in a dose-dependent manner[1].
B022 (0-5 μM; 12 hours; Hepa1 cells) treatment for 8 h completely blocks NIK-induced expression of TNF-a, IL-6, iNOS, CCL2, and CXCL5[1].
B022 prevents NIK- or H2O2-induced β cell death and also ameliorates streptozotocin (STZ)-induced β cell death and hyperglycemia[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Hepa1 cells
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Concentration:0 μM, 0.5 μM, 5 μM
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Incubation Time:12 hours
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Result:Suppressed NIK-induced p52 formation in a dose-dependent manner.
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Cell Line:Hepa1 cells
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Concentration:0 μM, 0.5 μM, 5 μM
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Incubation Time:12 hours
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Result:Dose-dependently blocked NIK-induced expression of chemokines, cytokines, and iNOS in these cells. Completely blocked NIK-induced expression of TNF-a, IL-6, iNOS, CCL2, and CXCL5.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:STOP-NIK male mice (8 weeks) infected with Ad-cre[1]
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Dosage:30 mg/kg
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Administration:Intravenous injection; twice a day; for 10 days
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Result:Completely prevents the lethal effect of abnormally high levels of hepatic NIK in mice. Inhibited the majority of the deteriorating effects of aberrant activation of hepatic NIK.
Chemical Information
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CAS No. 1202764-53-1
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Appearance Solid
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Molecular Weight 397.88
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Formula C19H16ClN5OS
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Color Light yellow to yellow
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SMILES
CC(C1=NC=CS1)(C#CC2=CC3=C(CCN3C4=NC(N)=NC=C4Cl)C=C2)O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (19)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Retinol Binding Protein 4 reactivates latent HIV-1 by triggering canonical NF-κB, JAK/STAT5 and JNK signalling. [Abstract]2025 Oct 3;10(1):326. PMID: 41038866 -
Immunity
Splenic TNF-α signaling potentiates the innate-to-adaptive transition of antiviral NK cells. [Abstract]2025 Mar 11;58(3):585-600.e6. PMID: 40023159 -
Nat Commun
Hepatic neddylation deficiency triggers fatal liver injury via inducing NF-κB-inducing kinase in mice. [Abstract]2022 Dec 16;13(1):7782. PMID: 36526632
B022 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Dec 16;13(1):7782. [Abstract]
B022 (5 µM; 48 h) significantly attenuates MLN-induced aberrant NIK signaling in HepG2 cells. Veh (black), B022 (blue).
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Nat Commun
IL-33 induces thymic involution-associated naive T cell aging and impairs host control of severe infection. [Abstract]2022 Nov 12;13(1):6881. PMID: 36371464 -
Adv Sci (Weinh)
Targeting PRKCN, an Essential Driver Orchestrating mTOR-IRF4 Axis Independently of Kinase Activity, in Multiple Myeloma. [Abstract]2026 Apr;13(21):e18975. PMID: 41655233 -
Cell Death Differ
2024 Oct;31(10):1267-1284. PMID: 39215104 -
J Neuroinflammation
TLR9/NF-κB-mediated dendritic cell activation by neutrophil extracellular traps drives pathogenesis in experimental cerebral malaria. [Abstract]2025 Aug 26;22(1):206. PMID: 40859255
B022 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2025 Aug 26;22(1):206. [Abstract]
Representative MFI histograms of CD86, CD80, and CD40 expression in BMDC, BMDC + NETs, BMDC + NETs + BAY 11-7082, and BMDC + NETs + B022 (5 µM) groups.
B022 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2025 Aug 26;22(1):206. [Abstract]
Immunoblot analysis was performed on IκBα, P65 and p-P65 in the BMDC, BMDC + NETs, BMDC + NETs + BAY 11-7082 and BMDC + NETs + B022 (5 µM) groups.
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J Neuroinflammation
2025 Jan 24;22(1):17. PMID: 39856699
B022 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2025 Jan 24;22(1):17. [Abstract]
Cell viability under different concentrations of B022 was detected using the CCK-8 assay.
B022 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2025 Jan 24;22(1):17. [Abstract]
Mean fluorescence intensity (MFI) of CD80 and CD86 in the culture medium group and the B022 group (1000 nM).
B022 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2025 Jan 24;22(1):17. [Abstract]
B022 (30 mg/kg; ip). Immunofluorescence staining of neuromuscular junction structures, specifically acetylcholine receptor clusters (green) and complement deposits C5b-9 (red).
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Am J Transplant
Electrostimulation suppresses allograft rejection via promoting lymphatic regulatory T cell migration mediated by lymphotoxin - lymphotoxin receptor β signaling. [Abstract]2024 Dec;24(12):2187-2198. PMID: 38992495 -
Liver Int
Lymphotoxin beta-activated LTBR/NIK/RELB axis drives proliferation in cholangiocarcinoma. [Abstract]2024 Nov;44(11):2950-2963. PMID: 39164890 -
Int J Pharm
Norcantharidin liposome emulsion hybrid delivery system enhances PD-1/PD-L1 immunotherapy by agonizing the non-canonical NF-κB pathway. [Abstract]2022 Nov 25:628:122361. PMID: 36332828 -
Int J Mol Sci
2026 Apr 2;27(7):3232. PMID: 41977413 -
Inflammation
ACE2 Alleviates Microglia Neuroinflammation by RANK-RANKL-OPG Axis in Parkinson's Disease. [Abstract]2025 Jul 5. PMID: 40615762 -
Biochim Biophys Acta Mol Basis Dis
LRRC8A as a central mediator promotes colon cancer metastasis by regulating PIP5K1B/PIP2 pathway. [Abstract]2024 Feb 11;1870(4):167066. PMID: 38350542 -
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Solvent & Solubility
In Vitro:
DMSO : 250 mg/mL (628.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.23 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
The EdU incorporation assay measures DNA synthesis by adding the thymidine analog 5-ethynyl-2′-deoxyuridine to cells or tissues, where it is incorporated into newly synthesized DNA during S phase. Incorporated EdU is detected by copper-catalyzed azide-alkyne cycloaddition, in which a fluorescent azide covalently reacts with the ethynyl group on EdU, allowing S-phase cells to be detected by fluorescence microscopy, flow cytometry, or high-content imaging. EdU detection does not require DNA denaturation or anti-BrdU antibody access, which preserves sample structure and improves compatibility with immunostaining and multiparameter cytometry compared with BrdU-based detection. EdU can be cytotoxic in a cell-type- and exposure-dependent manner, so pulse duration, concentration, and continuous-labeling designs should be validated for each cell type.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Purity & Documentation
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Data Sheet (280 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Ren X, et al. A small-molecule inhibitor of NF-κB-inducing kinase (NIK) protects liver from toxin-induced inflammation, oxidative stress, and injury. FASEB J. 2017 Feb;31(2):711-718. [Content Brief]
[2]. Li Z, et al. Discovery of a Potent and Selective NF-κB-Inducing Kinase (NIK) Inhibitor That Has Anti-inflammatory Effects in Vitro and in Vivo. J Med Chem. 2020;63(8):4388-4407. [Content Brief]
[3]. Li X, et al. Activation of NF-κB-Inducing Kinase in Islet β Cells Causes β Cell Failure and Diabetes. Mol Ther. 2020;28(11):2430-2441. [Content Brief]
Complete Stock Solution Preparation Table
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.5133 mL | 12.5666 mL | 25.1332 mL | 62.8330 mL |
| 5 mM | 0.5027 mL | 2.5133 mL | 5.0266 mL | 12.5666 mL | |
| 10 mM | 0.2513 mL | 1.2567 mL | 2.5133 mL | 6.2833 mL | |
| 15 mM | 0.1676 mL | 0.8378 mL | 1.6755 mL | 4.1889 mL | |
| 20 mM | 0.1257 mL | 0.6283 mL | 1.2567 mL | 3.1417 mL | |
| 25 mM | 0.1005 mL | 0.5027 mL | 1.0053 mL | 2.5133 mL | |
| 30 mM | 0.0838 mL | 0.4189 mL | 0.8378 mL | 2.0944 mL | |
| 40 mM | 0.0628 mL | 0.3142 mL | 0.6283 mL | 1.5708 mL | |
| 50 mM | 0.0503 mL | 0.2513 mL | 0.5027 mL | 1.2567 mL | |
| 60 mM | 0.0419 mL | 0.2094 mL | 0.4189 mL | 1.0472 mL | |
| 80 mM | 0.0314 mL | 0.1571 mL | 0.3142 mL | 0.7854 mL | |
| 100 mM | 0.0251 mL | 0.1257 mL | 0.2513 mL | 0.6283 mL |
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