2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Epigenetics
  3. EGFR Histone Acetyltransferase Epigenetic Reader Domain
  4. NSC 228155

NSC 228155 est un activateur de EGFR, se lie à la région extracellulaire de EGFR et améliore la phosphorylation de la tyrosine d'EGFR. NSC 228155 est également un inhibiteur puissant de l'interaction KIX-KID, inhibe le domaine inductible par kinase (KID) de CREB et le domaine interagissant avec KID (KIX) de CBP, avec un IC50 de 0,36 μM.

NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR. NSC 228155 is also a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP, with an IC50 of 0.36 μM.

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CAS No. : 113104-25-9

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Customer Review

Based on 20 publication(s) in Google Scholar

Other Forms of NSC 228155:

NSC 228155 Related Antibodies

Top Publications Citing Use of Products

    NSC 228155 purchased from MedChemExpress. Usage Cited in: Cytojournal. 2024 Nov 23:21:52.  [Abstract]

    Cell migration and invasion levels measured with Transwell assay. the si-SULF1 + NSC228155 (100 μM) group showed considerably augmented cell migration and invasion.

    NSC 228155 purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2022 May 16;18(9):3636-3652.

    Confirmation of EGFR inhibition, immunoblotting of A549 cancer cells whole cell lysates treated with Gefitinib (10µM), or Daidzein (300µM), and combination of the two drugs in the presence or absence EGFR activator NSC 228155 (2 µM).

    View All EGFR Isoform Specific Products:

    View All Isoforms
    EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

    View All Histone Acetyltransferase Isoform Specific Products:

    View All Isoforms
    CBP/p300 GCN5/PCAF TIP60 MOZ/MORF HBO1

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR[1]. NSC 228155 is also a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP, with an IC50 of 0.36 μM[2].

    IC50 & Target[1][2]

    CBP/p300

     

    EGFR

     

    KIX-KID

    0.36 μM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    HEK-293T IC50
    2.09 μM
    Compound: 1, NSC228155
    Inhibition of CREB (unknown origin)-mediated gene transcription in HEK293T cells preincubated for 30 mins followed by forskolin addition measured after 5 hrs by luciferase reporter gene assay
    Inhibition of CREB (unknown origin)-mediated gene transcription in HEK293T cells preincubated for 30 mins followed by forskolin addition measured after 5 hrs by luciferase reporter gene assay
    		[PMID: 23953193]
    HEK-293T IC50
    6.14 μM
    Compound: 1, NSC228155
    Inhibition of Herpesvirus VP16-CREB (unknown origin)-mediated gene transcription in HEK293T cells by luciferase reporter gene assay
    Inhibition of Herpesvirus VP16-CREB (unknown origin)-mediated gene transcription in HEK293T cells by luciferase reporter gene assay
    		[PMID: 23953193]
    In Vitro

    NSC 228155 (100 μM) enhances EGFR tyrosine phosphorylation via the action of SOD1[1].
    NSC 228155 (Compound 1) inhibits CREB- and VP16-CREB-mediated gene transcription in living HEK 293T cells with IC50s of 2.09 and 6.14 μM, respectively[2].
    NSC 228155 is not selective against CREB-mediated gene transcription in living HEK 293T cells[2].

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

    NSC 228155 Related Antibodies
    Molecular Weight

    290.25

    Formula

    C11H6N4O4S
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to orange

    SMILES

    [O-][N+]1=CC=CC=C1SC2=CC=C([N+]([O-])=O)C3=NON=C32
    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 : 16 mg/mL (55.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.4453 mL 17.2265 mL 34.4531 mL
    5 mM 0.6891 mL 3.4453 mL 6.8906 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.

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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    90% Corn Oil

      Solubility: ≥ 1.6 mg/mL (5.51 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.6 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 (16.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  15% Cremophor EL    85% Saline

      Solubility: 2 mg/mL (6.89 mM); Suspended solution; Need ultrasonic

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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
    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 3.4453 mL 17.2265 mL 34.4531 mL 86.1326 mL
    5 mM 0.6891 mL 3.4453 mL 6.8906 mL 17.2265 mL
    10 mM 0.3445 mL 1.7227 mL 3.4453 mL 8.6133 mL
    15 mM 0.2297 mL 1.1484 mL 2.2969 mL 5.7422 mL
    20 mM 0.1723 mL 0.8613 mL 1.7227 mL 4.3066 mL
    25 mM 0.1378 mL 0.6891 mL 1.3781 mL 3.4453 mL
    30 mM 0.1148 mL 0.5742 mL 1.1484 mL 2.8711 mL
    40 mM 0.0861 mL 0.4307 mL 0.8613 mL 2.1533 mL
    50 mM 0.0689 mL 0.3445 mL 0.6891 mL 1.7227 mL
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    NSC 228155 Related Classifications

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    • 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:

    NSC 228155113104-25-9NSC228155NSC-228155EGFRHistone AcetyltransferaseEpigenetic Reader DomainEpidermal growth factor receptorErbB-1HER1HATsHATInhibitorinhibitorinhibit

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