2. Stem Cell/Wnt MAPK/ERK Pathway TGF-beta/Smad
  3. Wnt MAP4K TGF-beta/Smad
  4. NCB-0846

NCB-0846 is an orally active, selective inhibitor for Wnt, that inhibits Traf2- and Nck-interacting kinase (TNIK) with an IC50 of 21 nM. NCB-0846 blocks TGF-β signaling pathway by inhibiting SMAD2/3 phosphorylation and nuclear translocation.

For research use only. We do not sell to patients.

CAS No. : 1792999-26-8

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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of NCB-0846:

NCB-0846 Related Antibodies

Top Publications Citing Use of Products

    NCB-0846 purchased from MedChemExpress. Usage Cited in: Oncogene. 2021 May;40(18):3287-3302.  [Abstract]

    ABT-263 had negligible effects on MCL1 mRNA levels; however, treatment with NCB-0846 alone, as well as its combination with ABT-263, resulted in a significant decrease in MCL1 mRNA levels.

    View All Wnt Isoform Specific Products:

    View All Isoforms
    Wnt1 Wnt3 Wnt5 Wnt7 Wnt11

    View All MAP4K Isoform Specific Products:

    View All Isoforms
    MAP4K2/GCK MAP4K3/GLK MAP4K4/HGK MAP4K5/KHS1 MAP4K6/MINK1 MAP4K7/TNIK MAP4K1/HPK1

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    NCB-0846 is an orally active, selective inhibitor for Wnt, that inhibits Traf2- and Nck-interacting kinase (TNIK) with an IC50 of 21 nM. NCB-0846 blocks TGF-β signaling pathway by inhibiting SMAD2/3 phosphorylation and nuclear translocation[1][2].

    IC50 & Target[1]

    Wnt

     

    TNIK

    21 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    HCT-116 IC50
    0.09 μM
    Compound: NCB-0846
    Inhibition of cell growth in human HCT-116 cells after 72 hrs by CCK-8 assay
    Inhibition of cell growth in human HCT-116 cells after 72 hrs by CCK-8 assay
    		[PMID: 38422698]
    HCT-116 IC50
    0.4 μM
    Compound: NCB-0846
    Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
    Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
    		[PMID: 34985886]
    HCT-116 IC50
    0.403 μM
    Compound: NCB-0846
    Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    		[PMID: 35447345]
    In Vitro

    NCB-0846 has anti-Wnt activity. NCB-0846 binds to TNIK in an inactive conformation, and this binding mode seems to be essential for Wnt inhibition. NCB-0846 shows inhibitory activity against TNIK with an IC50 of 21 nM. NCB-0846 also inhibits FLT3, JAK3, PDGFRα, TRKA, CDK2/CycA2, and HGK. NCB-0846 induces faster migration of TCF4 phosphorylated by TNIK within a concentration range of 0.1-0.3 μM and completely inhibits the phosphorylation of TCF4 at a concentration of 3 μM. NCB-0846 inhibits HCT116 cell growth and shows much higher (-20-fold) inhibitory activity against colony formation by the same cells in soft agar[1].

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

    NCB-0846 Related Antibodies
    In Vivo

    NCB-0846 suppresses the growth of tumors established by inoculating HCT116 cells into immunodeficient mice. The expression of Wnt-target genes (AXIN2, MYC and CCND1) in xenografts is reduced following the administration of NCB-0846. NCB-0846 induces an increase in the sub-G1 cell population. Cleavage of poly (ADP-ribose) polymerase 1 indicates the induction of apoptosis[1].

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

    375.42

    Formula

    C21H21N5O2
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O[C@@H](CC1)CC[C@@H]1OC2=CC=CC(C=N3)=C2N=C3NC4=CC=C(N=CN5)C5=C4
    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 : ≥ 30 mg/mL (79.91 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6637 mL 13.3184 mL 26.6368 mL
    5 mM 0.5327 mL 2.6637 mL 5.3274 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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.25 mg/mL (5.99 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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.
    • Protocol 2

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

      Solubility: ≥ 2.25 mg/mL (5.99 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.25 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 (22.5 mg/mL) to 900 μL Corn oil, and mix evenly.

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

    Dosage

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    +
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    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: 99.61%

    SDS (393 KB)

    COA (254 KB) LCMS (264 KB)

    Handling Instructions (2659 KB)
    References
    Animal Administration
    [1]

    Mice: NCB-0846 is suspended in DMSO/polyethylene glycol#400/30% 2-hydroxypropyl-β-cyclodextrin solution (10:45:45v/v). Five million HCT116 cells suspended in medium containing 25% Matrigel are inoculated into the subcutaneous tissues of 9-week-old female BALB/c nude mice. Mice are randomized according to tumour volume (9 mice per group). NCB-0846 was administered daily by oral gavage at 0 (vehicle alone), 40 or 80 mg/kg (body weight) BID (bis in die) for 14 days[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 2.6637 mL 13.3184 mL 26.6368 mL 66.5921 mL
    5 mM 0.5327 mL 2.6637 mL 5.3274 mL 13.3184 mL
    10 mM 0.2664 mL 1.3318 mL 2.6637 mL 6.6592 mL
    15 mM 0.1776 mL 0.8879 mL 1.7758 mL 4.4395 mL
    20 mM 0.1332 mL 0.6659 mL 1.3318 mL 3.3296 mL
    25 mM 0.1065 mL 0.5327 mL 1.0655 mL 2.6637 mL
    30 mM 0.0888 mL 0.4439 mL 0.8879 mL 2.2197 mL
    40 mM 0.0666 mL 0.3330 mL 0.6659 mL 1.6648 mL
    50 mM 0.0533 mL 0.2664 mL 0.5327 mL 1.3318 mL
    60 mM 0.0444 mL 0.2220 mL 0.4439 mL 1.1099 mL
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    NCB-0846 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:

    NCB-08461792999-26-8NCB0846NCB 0846WntMAP4KTGF-beta/SmadMAPK Kinase Kinase KinaseTransforming growth factor betaInhibitorinhibitorinhibit

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