2. Apoptosis
    Metabolic Enzyme/Protease
  3. MDM-2/p53
    E1/E2/E3 Enzyme
  4. Nutlin-3

Nutlin-3 

Cat. No.: HY-50696 Purity: 99.18%
COA Handling Instructions

Nutlin-3 is a commercial available p53-MDM2 inhibitor, with Ki of 90 nM.

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

Nutlin-3 Chemical Structure

Nutlin-3 Chemical Structure

CAS No. : 548472-68-0

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Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 135 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 135 In-stock
Solid
5 mg USD 106 In-stock
10 mg USD 158 In-stock
50 mg USD 594 In-stock
100 mg USD 1030 In-stock
200 mg   Get quote  
500 mg   Get quote  

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

Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of Nutlin-3:

Top Publications Citing Use of Products

    Nutlin-3 purchased from MCE. Usage Cited in: EBioMedicine. 2019 Oct;48:248-263.  [Abstract]

    p53 and p21 protein accumulation in HCT116 cells overexpressing p52-ZER6 and treated with nutlin-3 (final concentration: 5 μM), as examined using western blotting.

    Nutlin-3 purchased from MCE. Usage Cited in: EBioMedicine. 2019 Oct;48:248-263.  [Abstract]

    Binding capacity of MDM2 to p53 in HCT116 cells overexpressing p52-ZER6 and treated with nutlin-3 (final concentration: 5 μM). Cells are treated with MG132 to inhibit proteasomal degradation. Cell lysates are immunoprecipitated against anti-p53 antibody. The presence ofMDM2 is detected by immunoblotting.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Nutlin-3 is a commercial available p53-MDM2 inhibitor, with Ki of 90 nM.

    IC50 & Target

    Ki: 90 nM (p53-MDM2)[1]
    In Vitro

    Nutlin-3 is an inhibitor of the MDM2-p53 interaction. In particular, co-treatment of p53-positive HCT116 cells with 1 μM of Inauhzin and 2 μM of Nutlin-3 more significantly activated p53 as measured by its protein level as well as the level of its target p21, PUMA or cleaved PARP as indication of apoptosis[2]. Nutlin-3 is a small-molecule inhibitor that acts to inhibit MDM2 binding to p53 and subsequent p53-dependent DNA damage signaling. As a single agent, Nutlin-3 (2-10 μM) stabilizes p53 and p21WAF levels and is toxic to WTp53-22RV1 cells (IC50, 4.3 μM) but has minimal toxicity toward p53-deficient cells (IC50, >10 μM). Nutlin-3 induces p53 and p21WAF expression in a dose-dependent manner in 22RV1 cells. Short-term cell cycle assays show that, at a dose of 10 μM, Nutlin-3 increasea slightly the G1-phase fraction and decreasea S-phase fraction of all three cell lines[3].

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

    Nutlin-3 can suppress the growth of xenograft tumors derived from human osteosarcoma or leukemia cells, the anti-tumor activity of Nutlin-3 even at the dose of 200 mg/kg per oral administration is marginal in an HCT116-derived xenograft tumor model[2]. Nutlin-3 may be a useful adjunct to improve the therapeutic ratio using precision radiotherapy targeted to hypoxic cells and warrants further study in vivo[3].

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

    581.49

    Appearance

    Solid

    Formula

    C30H30Cl2N4O4
    CAS No.
    SMILES

    O=C1NCCN(C(N2[[email protected]@H](C3=CC=C(Cl)C=C3)[[email protected]@H](C4=CC=C(Cl)C=C4)N=C2C5=CC=C(OC)C=C5OC(C)C)=O)C1
    Shipping

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

    Ethanol : 100 mg/mL (171.97 mM; Need ultrasonic)

    DMSO : ≥ 50 mg/mL (85.99 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7197 mL 8.5986 mL 17.1972 mL
    5 mM 0.3439 mL 1.7197 mL 3.4394 mL
    10 mM 0.1720 mL 0.8599 mL 1.7197 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% EtOH    40% PEG300    5% Tween-80    45% saline

      Solubility: 5 mg/mL (8.60 mM); Clear solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% EtOH    90% corn oil

      Solubility: 5 mg/mL (8.60 mM); Clear solution; Need ultrasonic

    • 3.

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

      Solubility: ≥ 2.5 mg/mL (4.30 mM); Clear solution

    • 4.

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

      Solubility: 2.5 mg/mL (4.30 mM); Suspended solution; Need ultrasonic

    • 5.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.30 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.18%

    COA (266 KB) HNMR (299 KB) LCMS (266 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    Human non-small-cell lung carcinoma wild type p53-containing H460 and A549, human non-small-cell lung carcinoma p53-null H1299, and human colon cancer HCT116 (p53+/+ and p53-/-) cells are used. Cells (1.5×105) are plated into 6-well plates, and incubated at 37°C overnight. After treatment of Inauhzin and Nutlin 3 at the indicated concentrations for 48 h, cells are harvested, fixed in 70% ice-cold ethanol overnight at -20°C, resuspended in propidium iodide-solution (50 µg/mL PI, 0.1 mg/mL RNase A, 0.05% Tritin X-100 in PBS) for 40 min at 37°C, then analyzed for DNA content using a flow cytometer and proprietary software[2].

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

    Mice[2]
    Five-week-old female SCID mice are used. Mice are subcutaneously inoculated with 3×106 HCT116p53+/+ cells in the right flank and tumor growth is monitored with calipers. After the mean tumor volume reaches 50-100 mm3, animals are administered Inauhzin intraperitoneally (IP), Nutlin 3 orally, or vehicles (4% DMSO for Inauhzin, EtOH: Tween: 5% Glucose=5:5:90 for Nutlin 3). Tumor volume is measured every other day, and inhibition of tumor growth (T/C) is calculated on the last day of treatment.

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

    Nutlin-3548472-68-0Nutlin3Nutlin 3MDM-2/p53E1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseInhibitorinhibitorinhibit

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