2. NF-κB
  3. NF-κB
  4. NIK SMI1

NIK SMI1 is a potent, selective NF-κB inducing kinase (NIK) inhibitor, which inhibits NIK-catalyzed hydrolysis of ATP to ADP with IC50 of 0.23±0.17 nM. NIK SMI1 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.

CAS No. : 1660114-31-7

Size Price Stock Quantity
Free Sample (0.1 - 0.2 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 16 publication(s) in Google Scholar

Other Forms of NIK SMI1:

NIK SMI1 Related Antibodies

Top Publications Citing Use of Products

    NIK SMI1 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2025 Oct 7;44(10):116404.  [Abstract]

    NIK SMI1 (SMI1; 1 μM; 1 h) fully blocked effects observed in cells expressing the IKK1-AA mutant.

    NIK SMI1 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2025 Oct 7;44(10):116404.  [Abstract]

    NIK SMI1 (SMI1; 0.2,1 μM) decreased the protein expression of p-p105 S932, P-IKBα, and P-P65 s536 in IKK1-AA HeLa cells.Immunoblot analysis in cells treated with TWEAK and with the IKK2 inhibitor IKK16 or the NIK inhibitor SMI1 both at 200 nM and 1 μM. MG132 was applied for the last hour.

    NIK SMI1 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2025 Oct 7;44(10):116404.  [Abstract]

    Immunoblot assessment of the phosphorylation of the indicated NF-κB proteins (top) and the nuclear translocation of NF-κB proteins (bottom) in response of immortalized MDFs (IMDFs) derived from WT and NIK Xmut mice to TWEAK and MG132 and its arrest by the NIK inhibitor NIK SMI1 (SMI1; 1 μM).

    NIK SMI1 purchased from MedChemExpress. Usage Cited in: Nat Immunol. 2020 May;21(5):535-545.  [Abstract]

    NIK SMI1 (NIKi; 0, 1, 10 μM) suppressed nuclear accumulation of RelB in THP1 cells. Immunoblotting of nuclear extracts from THP1 cells treated with LPS (100 ng/mL) and/or NIK inhibitor (NIKi).

    NIK SMI1 purchased from MedChemExpress. Usage Cited in: Nat Immunol. 2020 May;21(5):535-545.  [Abstract]

    NIK SMI1 (NIKi; 0, 1, 10 μM) inhibited progenitor colony formation in methylcellulose containing cytokines compared to untreated cells. CD34+ del(5q) MDS BM and normal CD34+ BM cells treated with NIKi were evaluated for colony formation in methylcellulose.

    View All NF-κB Isoform Specific Products:

    View All Isoforms
    NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    NIK SMI1 is a potent, selective NF-κB inducing kinase (NIK) inhibitor, which inhibits NIK-catalyzed hydrolysis of ATP to ADP with IC50 of 0.23±0.17 nM. NIK SMI1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

    IC50 & Target

    NIK[1]
    Cellular Effect
    Cell Line Type Value Description References
    B-cell line IC50
    373 nM
    Compound: 4f
    Inhibition of BAFF-stimulated mouse splenic B cell survival preincubated for 1 hr followed by BAFF stimulation measured after 4 days by Cell-Titer Glo assay
    Inhibition of BAFF-stimulated mouse splenic B cell survival preincubated for 1 hr followed by BAFF stimulation measured after 4 days by Cell-Titer Glo assay
    		[PMID: 29940120]
    In Vitro

    NIK SMI1 (Compound 4f) inhibits NIK-catalyzed hydrolysis of ATP to ADP (fluorescence polarization, FP) with an IC50 of 0.23±0.17 nM. NIK SMI1 inhibits the expression of NIK SMI1 response elementregulated firefly luciferase reporter gene in HEK293 cells with an IC50 of 34±6 nM. Consistent with expectations for a NIK inhibitor, NIK SMI1 is shown to inhibit nuclear translocation of p52 (RelB) (IC50=70 nM). NIK SMI1 inhibits BAFF-induced B cell (mouse) survival in vitro with an IC50 of 373±64 nM[1].

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

    NIK SMI1 Related Antibodies
    In Vivo

    C57BL/6 mice are treated twice daily for 7 days with orally administered NIK SMI1 or with three injections of recombinant BAFF receptor fusion protein (Br3- mIgG2a) over the course of the 7-day experiment as a positive control. The nonlinearity of exposure relative to dose between 100 and 200 mg/kg is a result of saturation of clearance mechanisms. The pharmacology of NIK SMI1 is examined in SD rat, CD-1 mouse, beagle, and cynomologous monkey with 20, 32, 18, and 7.8 mL/kg per min, respectively. Volume of distribution (Vd, L/kg) is 1.35, 1.58, 0.778, and 1.39, respectively[1].

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

    365.38

    Formula

    C20H19N3O4
    CAS No.
    Appearance

    Solid

    Color

    Off-white to pink

    SMILES

    O=C(N)C1=NC(C2=CC=CC(C#C[C@]3(O)CCN(C)C3=O)=C2)=CC(OC)=C1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (342.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7369 mL 13.6844 mL 27.3688 mL
    5 mM 0.5474 mL 2.7369 mL 5.4738 mL
    View the 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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.

    • Protocol 1

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.5 mg/mL (6.84 mM); Clear solution

    • Protocol 2

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.84 mM); Clear 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.

    • Protocol 1

      Add each solvent one by one:  Corn Oil

      Solubility: 10 mg/mL (27.37 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 5 mg/mL (13.68 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation

    Purity: 99.92%

    SDS (251 KB)

    COA (252 KB) RP-HPLC (224 KB) MS (69 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    Human B cells are re-suspended in RPMI with 10% FBS for the proliferation assays and 2.5% FBS for the survival assays. Mouse B cells are plated in Co-star 96-well plates at either 50,000 cells/well for the survival assays or at 150,000 cells/well for the proliferation assays. Compounds (e.g., NIK SMI1) diluted in DMSO (final DMSO assay concentration=0.1%) are added to the cells. The cells are incubated with NIK SMI1 for one hour at 37°C. Stimulus is then added to the plates and survival or proliferation is measured after four days. For the proliferation assays, cells are treated with either Anti-IgM (20 µg/mL) or rhCD40L (10 µg/mL) or anti-mouse CD40 (100 ng/mL). For the BAFF survival assay, cells are treated with human or mouse rBAFF at 10 ng/mL followed by Cell Titer Glo to measure survival on day four[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice[1]
    Age-matched C57BL/6 mice are used. Only female mice are used in these experiments. The single oral doses of NIK SMI1 are 10, 20, 60, 100, and 200 mg/kg. For PO dosing, animals are manually restrained, then dosed via oral gavage using an appropriately sized gavage needle. Animals are monitored for any signs of aspiration or distress-respiratory abnormalities, lethargy, pale extremities, etc. For sample collection, 3 mice per group are bled a total of 8 times via tail prick using a 27 G needle (lateral tail vein). 10 μL of blood is collected at each timepoint and deposited into a pre-filled costar cluster tube containing 40 μL of 1.7 mg/mL EDTA/water, the tube is capped, votexed for 5 seconds, then stored on dry ice. Samples are transferred to a -80°C freezer for storage[1].

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

    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
    DMSO 1 mM 2.7369 mL 13.6844 mL 27.3688 mL 68.4219 mL
    5 mM 0.5474 mL 2.7369 mL 5.4738 mL 13.6844 mL
    10 mM 0.2737 mL 1.3684 mL 2.7369 mL 6.8422 mL
    15 mM 0.1825 mL 0.9123 mL 1.8246 mL 4.5615 mL
    20 mM 0.1368 mL 0.6842 mL 1.3684 mL 3.4211 mL
    25 mM 0.1095 mL 0.5474 mL 1.0948 mL 2.7369 mL
    30 mM 0.0912 mL 0.4561 mL 0.9123 mL 2.2807 mL
    40 mM 0.0684 mL 0.3421 mL 0.6842 mL 1.7105 mL
    50 mM 0.0547 mL 0.2737 mL 0.5474 mL 1.3684 mL
    60 mM 0.0456 mL 0.2281 mL 0.4561 mL 1.1404 mL
    80 mM 0.0342 mL 0.1711 mL 0.3421 mL 0.8553 mL
    100 mM 0.0274 mL 0.1368 mL 0.2737 mL 0.6842 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    NIK SMI1 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    NIK SMI11660114-31-7NIK SMI 1NIK SMI-1NF-κBNuclear factor-κBNuclear factor-kappaBInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Requested Quantity *

    Applicant Name *

    		 

    Salutation

    Email Address *

    		 

    Phone Number *

    Department

    		 

    Organization Name *

    City

    State

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    NIK SMI1
    Cat. No.:
    HY-112433
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    SAFETY DATA SHEET (SDS)

    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)

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.