2. NF-κB
  3. Keap1-Nrf2
  4. NK-252

NK-252 

Cat. No.: HY-19734 Purity: 99.93%
COA Handling Instructions

NK-252 is a potential Nrf2 activator, which exhibits a great Nrf2-activating potential.

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

NK-252 Chemical Structure

NK-252 Chemical Structure

CAS No. : 1414963-82-8

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 73 In-stock
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10 mM * 1 mL in DMSO USD 73 In-stock
Solid
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10 mg USD 92 In-stock
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Customer Review

Based on 9 publication(s) in Google Scholar

NK-252 Related Antibodies

Top Publications Citing Use of Products

    NK-252 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2020 Jul 30;11(7):607.  [Abstract]

    The levels of nuclear Nrf2 and the mRNA expression levels of Nrf2, SOD1, SOD3, CAT, and Gpx are significantly increased after LA+NK-252 (2 μM) treatment.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    NK-252 is a potential Nrf2 activator, which exhibits a great Nrf2-activating potential.

    IC50 & Target

    Nrf2[1]
    In Vitro

    The luciferase activity in Huh-7.5 cells treated with Oltipraz (OPZ) or NK-252 shows activation of the NAD(P)H quinone oxidoreductase 1 (NQO1)-ARE in a dose-dependent manner. NK-252 displays this effect with higher potency than OPZ based on the fact that the EC2 value (concentration for a 2-fold induction above background), calculated with linear extrapolation from the values above and below the induction threshold, is 20.8 μM for OPZ and 1.36 μM for NK-252.? NK-252 has potential as an Nrf2 activator in hepatic cells. Prototypical Nrf2 activators that include OPZ have been reported to protect microglial cells from H2O2-induced cytotoxicity. The protective effects of OPZ and NK-252 are examined against H2O2-induced cytotoxicity using Huh-7 cells to evaluate their antioxidant properties. The cells treated with OPZ or NK-252 show increased resistance to H2O2-induced cytotoxicity compared with control cells[1].

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

    NK-252 Related Antibodies
    In Vivo

    Rats on a choline-deficient L-amino acid–defined (CDAA) diet given OPZ or NK-252 display decreased fibrosis scores compared with CDAA control rats, with median scores of 3, corresponding to bridging fibrosis. CDAA control rats display approximately 20-fold augmentation of the liver fibrosis area compared with rats fed a normal control diet (naive) (14.7 and 0.72%, respectively).This augmentation is also drastically reduced by administration of OPZ or NK-252 (5.80% for OPZ, 6.20% for NK-252_low, and 4.97% for NK-252_high). The effects of NK-252 on both fibrosis score and fibrosis area are dose-dependent[1]. NK-252 alone has no antitumour effect in P388/S- and P388/VCR-mice. The combination therapy of Etoposide with NK-252 administered p.o. significantly increases the life-span of mice inoculated i.p. with P388/S compared with the corresponding therapeutic effects with Etoposide alone. The combination therapy with Etoposide and NK-252 significantly increases the life-span of mice inoculated i.p. with P388/VCR compared with the corresponding survival time with Etoposide alone[2].

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

    285.26

    Appearance

    Solid

    Formula

    C13H11N5O3
    CAS No.
    SMILES

    O=C(NCC1=NC=CC=C1)NC2=NN=C(C3=CC=CO3)O2
    Shipping

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

    DMSO : ≥ 29 mg/mL (101.66 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.5056 mL 17.5279 mL 35.0557 mL
    5 mM 0.7011 mL 3.5056 mL 7.0111 mL
    10 mM 0.3506 mL 1.7528 mL 3.5056 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

      Solubility: ≥ 2.08 mg/mL (7.29 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (7.29 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2.08 mg/mL (7.29 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation
    References
    Cell Assay
    [1]

    The Huh-7.5 cells, a subline derived from Huh-7 cells, are transfected with ARE/pGL4.32 by lipofectamine LTX. The stable clonal transfectant is isolated by selection in hygromycin B (0.1 mg/mL). Cells derived from stable clones are transfected with control or Nrf2 small interfering RNA by lipofectamine RNAiMAX (30 hours), then treated with OPZ, NK-252 (0.1-30 μM, 16 hours) , or DMSO alone (control). The luciferase activity values are measured using the Steady-Glo Luciferase Assay System[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1][2]

    Rats[1]
    Six-week-old male Fischer 344 rats are randomly divided into four compound administration groups and four control groups. Compound administration groups of rats fed a CDAA diet receive oral administration as follows: 1) OPZ from 1 week after feeding at a dose of 60 mg/kg once daily for 9 weeks (CDAA+OPZ group; N=8), 2) NK-252 from 1 week after feeding at a dose of 20 mg/kg once daily for 9 weeks (CDAA+NK-252_low group; N=8), 3) NK-252 from 1 week after feeding at a dose of 60 mg/kg once daily for 9 weeks (CDAA+NK-252_high group; N=8), or 4) NK-252 from 6 weeks after feeding at a dose of 60 mg/kg once daily for 4 weeks (CDAA+NK-252_delayed administration: DA group; N=7). Two control groups of rats are fed a CDAA diet for 6 or 10 weeks (pre-CDAA control or CDAA control group; N=9 each), and the other two control groups of rats are fed standard rodent chow (CRF-1) for 6 or 10 weeks (prenaive or naive; N=3 each). Laparotomy and blood sampling are performed under isoflurane anesthesia. After blood sampling, rats are euthanized by exsanguination under isoflurane anesthesia, and the livers are immediately extirpated. [2]Mice[2]
    Six- to 8-week-old male BALB/c x DBA/2 F1 (hereafter called CD2F1) mice weighing 22 to 26 g are used. Male CD2F1 mice are inoculated i.p. with 106 cells of P388/S and P388/VCR cell line on day 0. Each group consist of six mice. NK-250 and NK-252 (100, 300, and 1000 mg/kg) are given p.o. daily from day 1 to 5. Mean survival days and the range of survival days are analysed.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
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    NK-252 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.

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    Keywords:

    NK-2521414963-82-8NK252NK 252Keap1-Nrf2Inhibitorinhibitorinhibit

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