1. NF-κB
  2. IKK
  3. SC-514

SC-514 (Synonyms: GK 01140)

Cat. No.: HY-13802 Purity: 99.99%
Handling Instructions

SC-514 is a selective IKK-2 inhibitor (IC50=11.2 μM), which does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.

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

SC-514 Chemical Structure

SC-514 Chemical Structure

CAS No. : 354812-17-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 61 In-stock
Estimated Time of Arrival: December 31
10 mg USD 55 In-stock
Estimated Time of Arrival: December 31
50 mg USD 130 In-stock
Estimated Time of Arrival: December 31
100 mg USD 200 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    SC-514 purchased from MCE. Usage Cited in: Dig Dis Sci. 2019 May;64(5):1204-1216.

    The expression of BAX, Bcl2, P53, PARP, cleaved caspase 3, and cleaved caspase 9 in SGC-7901 cells is measured by western blotting in the treatment of SC-514.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    SC-514 is a selective IKK-2 inhibitor (IC50=11.2 μM), which does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.

    IC50 & Target[1]

    IKK-2

    11.2 μM (IC50)

    CDK2/A

    61 μM (IC50)

    AUR2

    71 μM (IC50)

    PRAK

    75 μM (IC50)

    MSK

    123 μM (IC50)

    In Vitro

    SC-514 inhibits the native IKK complex or recombinant human IKK-1/IKK-2 heterodimer with IC50s of 6.1±2.2 μM and 2.7±0.7 μM, respectively. IKK-2 inhibition by SC-514 is selective, reversible, and competitive with ATP. SC-514 inhibits transcription of NF-κB-dependent genes in IL-1β-induced rheumatoid arthritis-derived synovial fibroblasts in a dose-dependent manner. SC-514 inhibits all forms of recombinant human IKK-2 including rhIKK-2 homodimer, rhIKK-1/rhIKK-2 heterodimer, as well as the constitutively active form of rhIKK-2 with comparable IC50 values in the 3-12 μM range[1]. To evaluate whether the reactive oxygen species (ROS)-inducing IKKβ inhibitor increases the sensitivity of melanoma cells to nitrosourea. The responses of melanoma cells are first assessed to SC-514/Fotemustine co-treatment. Melanoma cell lines are treated with 50 µM of SC-514 and Fotemustine alone and in combination for 48 h and growth inhibition is assessed. Co-treatment with SC-514 significantly enhances Fotemustine-induced cytotoxicity in all melanoma cell lines tested[2].

    In Vivo

    SC-514 is efficacious in an acute model of inflammation, namely LPS-induced serum TNFα production in the rat. SC-514 shows a dose-dependent inhibition of TNFα production, validating IKK-2 as a potential anti-inflammatory drug target in vivo[1]. To obtain in vivo evidence for the implication of SC-514 in the response of cancer cells to Fotemustine, the xenograft mouse model of melanoma is used. Nude mice engrafted with A375 or G361 tumors are treated with vehicle control and 25 mg/kg SC-514 and/or 25 mg/kg Fotemustine daily for 13-15 consecutive days and the tumor behavior is monitored. Fotemustine treatment with SC-514 shows a clear combined effect and reduces the size of tumors in mice[2].

    Molecular Weight

    224.30

    Formula

    C₉H₈N₂OS₂

    CAS No.

    354812-17-2

    SMILES

    O=C(C1=C(N)C=C(C2=CSC=C2)S1)N

    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: 

    DMSO : 100 mg/mL (445.83 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 4.4583 mL 22.2916 mL 44.5831 mL
    5 mM 0.8917 mL 4.4583 mL 8.9166 mL
    10 mM 0.4458 mL 2.2292 mL 4.4583 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Kinase Assay
    [1]

    IKK complexes are immunoprecipitated from IL-1β-treated RASF cell lysates (0.5-2 mg) using a NEMO antibody (3-10 μg) followed by the addition of protein A-agarose beads. Antibody complexes are pelleted by centrifugation and washed 3 times with 1 mL of cold whole-cell lysis buffer followed by 2 washes in kinase buffer (25 mM HEPES, pH 7.6, 2 mM MgCl2, 2 mM MnCl2, 10 mM NaF, 5 mM DTT, and 1 mM phenylmethylsulfonyl fluoride). 100-200 μg of immunoprecipitated IKK is analyzed for kinase activity in a reaction containing 10 μM biotinylated IκBα peptide as substrate and 1 μM [γ-33P]ATP (2500 Ci/mmol). After incubation at room temperature for 30 min, 25 μL of the reaction mixture is withdrawn and added to a SAM 96 biotin capture plate. After successive wash steps the plate was allowed to air-dry, and 25 μL of scintillation fluid is added to each well. Incorporation of [γ-33P]ATP is measured using a Top-Count NXT[1].

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

    Cell Assay
    [2]

    For crystal violet staining assay, melanoma cell lines (1×104) are seeded in 60 mm dishes, and then untreated or pretreated with SC-514 (50 µM) and/or Fotemustine. Then, cells are formalin-fixed and stained with crystal violet. Cell numbers are measured as the optical density at 595 nm (OD595) of solubilized crystal violet from formalin-fixed cells. Cytotoxicity are also determined by the MTT reduction assay[2].

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

    Animal Administration
    [1][2]

    Rats[1]
    SC-514 or vehicle (2% Me2SO in saline) is administered either by oral gavage (50 mg/kg) or intraperitoneally (10 and 50 mg/kg) to adult male Wistar rats that have been deprived of food overnight. Two hours after compound treatment, 1 mg/kg LPS (Escherichia coli) in saline is administered intraperitoneally 90 min after LPS administration; the animals are bled and serum TNFα levels analyzed by a rat-specific TNFα ELISA.
    Mice[2]
    Male nu/nu BALB/c mice (6 weeks old) are maintained in individual ventilated cages. A375 or G361 (5×106) cells are resuspended in 0.1 mL PBS and inoculated subcutaneously into the backs of nude mice and allowed to grow for 7 days. After that, mice are randomly assigned to 4 groups (n=6 for each group) and treated by intraperitoneal injection with 200 µL 30% PEG/5% Tween-80 solution as the vehicle control and 25 mg/kg SC-514 and/or 25 mg/kg Fotemustine daily for 13-15 consecutive days. Body weight and tumor volume are measured every 3 days. Tumor volumes are determined by a caliper and calculated. At the end of the experiment, mice are sacrificed and tumor xenografts are collected. Tumor tissues are stored at -80°C for Western blot analysis.

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

    References

    Purity: 99.99%

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    Keywords:

    SC-514GK 01140SC514SC 514GK01140GK-01140IKKIκB kinaseI kappa B kinaseInhibitorinhibitorinhibit

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