1. MAPK/ERK Pathway
  2. MAP4K
    MAP3K

NG25 

Cat. No.: HY-15434 Purity: 99.45%
Handling Instructions

NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively.

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

NG25 Chemical Structure

NG25 Chemical Structure

CAS No. : 1315355-93-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 312 In-stock
Estimated Time of Arrival: December 31
1 mg USD 96 In-stock
Estimated Time of Arrival: December 31
5 mg USD 264 In-stock
Estimated Time of Arrival: December 31
10 mg USD 468 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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    NG25 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2014 Oct 10;453(1):106-11.

    786-O/A489 RCC cells are treated with LYTAK1 (100 nM), 5Z-7-oxozeanol (5Z, 0.25 lM) or NG-25 (NG-25, 2.5 lM) for 24 h, Western blots are applied to tested list proteins.

    NG25 purchased from MCE. Usage Cited in: Mol Med Rep. 2018 Jan;17(1):1710-1716.

    Expression level of p TAK1 and downstream targets following NG25 treatment. Western blot detection of p TAK1 and TAK1 expression levels in the sham group, and samples from HI, DMSO treated and NG25 treated rat brain cortexes.

    NG25 purchased from MCE. Usage Cited in: Sci Rep. 2016 Sep 7;6:32737.

    TAK1 inhibition inhibits Dox-induced p38 activation and IκBα degradation. Breast cancer cell lines T-47D, MCF7, HCC1954, MDA-MB-231, and BT-549 are treated with Dox (20 μM) alone or combined with NG25 (2 μM) for 0, 2 h, 4 h or 6 h. The protein extracts are subjected to SDS-PAGE and immunoblotted with the antibodies against p-p38, p38, and IκBα. β-actin are detected as loading controls for whole cell extracts.

    NG25 purchased from MCE. Usage Cited in: Oncogene. 2017 Oct 5;36(40):5620-5630.

    C3-TAg cells are starved and stimulated for 0, 15 and 30 min with ephrin-A1-Fc (EphA2 ligand; 1 μg/mL) in the presence or absence of ALW-II-41-27 or NG-25 control. EphA2 is immunoprecipitated and products probed for tyrosine phosphorylation and EphA2. ALW-II-41-27 significantly reduces basal and ephrin-A1-Fc induced tyrosine phosphorylation.

    NG25 purchased from MCE. Usage Cited in: Nat Cell Biol. 2017 Oct;19(10):1248-1259.

    Immortalized RIPK1 +/+ fetal liver mouse macrophages were infected with YopP-negative Ye-ΔyopP in presence of inhibitors for TAK1 (NP, NG25), IKKβ, IKK, p38, MK2, JNK, or MEK1/ERK. The phosphorylation of RIPK1 is analyzed by immunoblotting in cell lysates prepared after 75 min of infection.

    NG25 purchased from MCE. Usage Cited in: Oncotarget. 2017 Nov 1;8(61):104330-104346.

    MC38-CT or -CC1-L cells are treated with 1 μM of DMSO, or the non-specific NG-25 or specific ALW-II-41-27 EPHA2 receptor inhibitor for indicated periods of time, followed by stimulation with EFNA1-Fc (2 μg/mL) in the last 15 min of treatments. Protein lysates are prepared and subjected to immunoblotting using antibodies to determine the effect of kinase inhibitors on EPHA2 activation.

    NG25 purchased from MCE. Usage Cited in: Sci Signal. 2018 Jul 10;11(538). pii: eaan5850.

    A549 cells are treated for 30 min with either 5z-7-oxozeanol or NG-25 to inhibit TAK1 and immunoblotted with the indicated antibodies.

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    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively.

    IC50 & Target[3]

    MAP4K2

    21.7 nM (IC50)

    TAK1

    149 nM (IC50)

    LYN

    12.9 nM (IC50)

    GSK

    56.4 nM (IC50)

    ABL,ARG

    75.2 nM (IC50)

    FER

    82.3 nM (IC50)

    SRC

    113 nM (IC50)

    Eph B2

    672 nM (IC50)

    ZAK

    698 nM (IC50)

    Eph A2

    773 nM (IC50)

    Eph B4

    999 nM (IC50)

    ZC1/HGK

    3250 nM (IC50)

    RAF1

    7590 nM (IC50)

    In Vitro

    NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively. NG25 also potently suppresses several kinases such as LYN, CSK, FER, p38α, ABL,ARG and SRC, with IC50s of 12.9, 56.4, 82.3, 102, 75.2, and 113 nM, respectively[1]. NG25 is very potent suppressor of CpG B- or CpG A-stimulated secretion of IFNα and CL097-stimulated secretion of IFNβ, with complete inhibition by 400 nM[2]. NG25 treatment reduces cell viability of all tested breast cancer cell lines in a dose dependent manner. NG25 (2 μM) enhances the cytotoxic effect of Dox on breast cancer cells[3].

    Solvent & Solubility
    In Vitro: 

    10 mM in DMSO

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8602 mL 9.3009 mL 18.6019 mL
    5 mM 0.3720 mL 1.8602 mL 3.7204 mL
    10 mM 0.1860 mL 0.9301 mL 1.8602 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Kinase Assay
    [2]

    IRF7 is expressed in Escherichia coli as a glutathione S-transferase (GST) fusion protein with a PreScission proteinase cleavage site between the GST and the IRF7. The GST-IRF7 is captured on glutathione-Sepharose and IRF7 released from GST and glutathione-Sepharose by digestion with PreScission proteinase. His6-tagged IKKβ and TBK1 are expressed in their active phosphorylated forms in insect Sf21 cells and purified by affinity chromatography on nickel nitrilotriacetate-agarose. Active GST-IKKα is purchased from Millipore and assayed.

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

    Cell Assay
    [2]

    3.5×105 Gen2.2 cells or Flt3-DCs are incubated for 1 h in 96-well plates without or with the indicated concentrations of inhibitor, then stimulated with 1 μM CpG (type A or B) or 1 μg/mL of CL097 or R848. After 5 or 12 h the cell culture supernatants are collected, clarified by centrifugation, and frozen at −80°C until cytokine levels are analyzed. For cell viability assays, unstimulated cells are incubated for 12 h in the absence or presence of inhibitors. Cells are then fixed and the percentage of live cells analyzed by flow cytometry.

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

    References
    Molecular Weight

    537.58

    Formula

    C₂₉H₃₀F₃N₅O₂

    CAS No.

    1315355-93-1

    SMILES

    O=C(NC1=CC(C(F)(F)F)=C(CN(CC2)CCN2CC)C=C1)C3=CC(OC4=C5C(NC=C5)=NC=C4)=C(C)C=C3

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

    Room temperature in continental US; may vary elsewhere

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    Cat. No.:
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    Cat. No.: HY-15434