1. MAPK/ERK Pathway Stem Cell/Wnt
  2. ERK
  3. SCH772984

SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC50s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-naïve and MAPK inhibitor-resistant cells containing BRAF or RAS mutations.

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

SCH772984 Chemical Structure

SCH772984 Chemical Structure

CAS No. : 942183-80-4

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10 mM * 1 mL in DMSO
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Customer Review

Based on 129 publication(s) in Google Scholar

Top Publications Citing Use of Products

116 Publications Citing Use of MCE SCH772984

IF
WB

    SCH772984 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Feb 13;14(1):802.  [Abstract]

    SCH772984 upregulates Mbp and Ng2, as well as significantly reduces Cd74 and Erk1/2, in primary neuronal cultures from control and Alzheimer’s disease knock-in mice (Fig. i and j).

    SCH772984 purchased from MedChemExpress. Usage Cited in: Acta Biomater. 2019 Feb;85:106-116.  [Abstract]

    Western analysis of related protein expression in the treatment of DBM/CBD-IKVAV-cRGD, DBM/CBD-IKVAV-cRGD + FAK inhibitor PF-573228 or DBM/CBD-IKVAV-cRGD + ERK inhibitor SCH772984.

    SCH772984 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2019 Jan 29;9(1):907.  [Abstract]

    HCT116 cells are first treated with different concentrations of PD0325901 or SCH772984 for 36 h and are then treated without or with MG132 for 12 hours before harvested for analysis of the levels of proteins by western blotting using antibodies as indicated.

    SCH772984 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2019 Jan 29;9(1):907.  [Abstract]

    KYSE70 cells are first treated with different concentrations of PD0325901 or SCH772984 for 36 hours and are then treated without or with MG132 for 12 hours before cells are harvested for western blotting using antibodies as indicated.

    SCH772984 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2019 Jan 29;9(1):907.  [Abstract]

    HCT116 cells are treated with different concentrations of PD0325901 or SCH772984 before cells are harvested for western blotting analysis for ERK1/2 and phosphorylated ERK1/2

    SCH772984 purchased from MedChemExpress. Usage Cited in: Theranostics. 2018 Jul 30;8(15):4262-4278.  [Abstract]

    BV2 cells are pretreated with 0.1% DMSO (Ctrl), JuA (25 µM) or JuA (25 µM)+SCH772984 (10 µM) for 30 min, followed by administration of Aβ42 (5 μM) for 6 h.

    SCH772984 purchased from MedChemExpress. Usage Cited in: Cancer Res. 2018 Feb 15;78(4):891-908.  [Abstract]

    A549 cells are treated with 10 μM SCH772984 (ERK1/2 inhibitor) or DMSO for 16 hr and analyzed for PSC formation by immunostaining

    SCH772984 purchased from MedChemExpress. Usage Cited in: J Immunol Res. 2018 Jun 7;2018:6249085.  [Abstract]

    The level of p-ERK1/2 expression is suppressed by SCH772984. RAW264.7 cells are preincubated with 1 μM SCH772984 for 2h followed by treatment with 20 μg/mL ox-LDL for 24 h.

    SCH772984 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Jan 1;495(1):781-786.  [Abstract]

    Representative images of migrated cells. HUVECs are pretreated with PD98059 (10 μM), SCH772984 (500 nM) or mock control for 2 h, and seeded in upper chambers of transwell inserts. VEGF (100 ng/ml), Scg3 (1 μg/ml) or PBS in medium with reduced FBS is added to bottom chambers in the presence or absence of the inhibitor. After culturing for 4 or 20 h, cells migrated to the lower surface of transwell membrane are stained with DAPI.

    SCH772984 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2017 Nov 25;14(1):228.  [Abstract]

    HSP70 release is reversed by ERK1/2 inhibitor in SH-SY5Y cells. SCH772984 (ERK1/2 inhibitor, 2 μM) is given 15 min. Supernatants are collected and analyzed by western blot (n=3).

    SCH772984 purchased from MedChemExpress. Usage Cited in: Neurotox Res. 2017 Nov;32(4):535-543.  [Abstract]

    Lithium promotes autophagy flux by activating MEK/ERK pathway in cells. Original Western blot showing LC3-II and p62 abundance following treatment with lithium in the presence of PD184352 and SCH772984 in neurons. Arithmetic means±SEM (n=5) showing LC3-II abundance following treatment with lithium in the presence of PD184352 and SCH772984 in neurons.

    SCH772984 purchased from MedChemExpress. Usage Cited in: Faculty of Medicine, Dentistry and Health Sciences. University of Melbourne. 2017 Sep.

    Western blot analysis is performed on protein lysates from exponentially growing melanoma cell lines following 24 hours treatment with 0.1% DMSO as a vehicle control or: GSK1120212 (GSK212) 100 nM; GDC0623 100 nM or SCH772984 1 µM.

    SCH772984 purchased from MedChemExpress. Usage Cited in: Department of Dental Pharmacology. Okayama University. 2015.

    The role of Semaphorin4D in bone invasion by oral cancer.

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    • Purity & Documentation

    • References

    • Customer Review

    Description

    SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC50s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-naïve and MAPK inhibitor-resistant cells containing BRAF or RAS mutations[1].

    IC50 & Target[1]

    ERK2

    1 nM (IC50)

    ERK1

    4 nM (IC50)

    In Vitro

    SCH772984 (300 nM; 24-48hours) results in a G1 arrest in SCH772984-sensitive melanoma cells[1].
    SCH772984 (3-300 nM; 24 hours) inhibits ERK and RSK phosphorylation[1].
    SCH772984 shows EC50 values less than 500 nM in approximately 88% and 49% of BRAF-mutant (n=25) or RAS-mutant (n=35) tumor lines, respectively[1].

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

    Cell Cycle Analysis[1]

    Cell Line: LOX cells (SCH772984-sensitive melanoma cells)
    Concentration: 300 nM
    Incubation Time: 24, 48 hours
    Result: Revealed a G1 arrest as well as an increase in the sub-G1 fraction indicative of apoptosis.

    Western Blot Analysis[1]

    Cell Line: LOX BRAFV600E melanoma cells
    Concentration: 3, 10, 30, 100, 300 nM
    Incubation Time: 24 hours
    Result: A dose-dependent inhibition of phosphorylation of the ERK substrate RSK (T359/S363 phospho-RSK), and also inhibited phosphorylation of residues in the activation loop of ERK itself (T202/Y204 and T185/Y187 of ERK1 and ERK2, respectively).
    In Vivo

    SCH772984 (12.5-50 mg/kg; i.p.; twice daily for 14 days) leads to 98% tumor regression[1].
    Dose-dependent antitumor activity is also observed in the KRAS-mutant pancreatic MiaPaCa model, with 36% regression at 50 mg/kg twice daily. Importantly, tumor regression is accompanied by robust inhibition of ERK phosphorylation in tumor tissue. SCH772984 is well tolerated on this schedule as measured by morbidity, lethality, or body weight loss[1].

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

    Animal Model: Female nude mice bearing human LOX BRAFV600E tumors[1]
    Dosage: 12.5, 25, 50 mg/kg
    Administration: Intraperitoneal injection; twice daily for 14 days
    Result: Tumor regressions were observed at all doses, such as 17% at 12.5 mg/kg, 84% at 25 mg/kg, and 98% at 50 mg/kg).
    Molecular Weight

    587.67

    Formula

    C33H33N9O2

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C([C@H](CC1)CN1CC(N(CC2)CCN2C(C=C3)=CC=C3C4=NC=CC=N4)=O)NC5=CC6=C(C=C5)NN=C6C7=CC=NC=C7

    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 : 48 mg/mL (81.68 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 1.7016 mL 8.5082 mL 17.0164 mL
    5 mM 0.3403 mL 1.7016 mL 3.4033 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 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.4 mg/mL (4.08 mM); Clear solution

    • Protocol 2

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

      Solubility: ≥ 1.43 mg/mL (2.43 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

    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:  20% SBE-β-CD adjusted to pH 4-4.5 with 1 N acetic

      Solubility: 20 mg/mL (34.03 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    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

    Purity: 99.27%

    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 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. 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 1.7016 mL 8.5082 mL 17.0164 mL 42.5409 mL
    5 mM 0.3403 mL 1.7016 mL 3.4033 mL 8.5082 mL
    10 mM 0.1702 mL 0.8508 mL 1.7016 mL 4.2541 mL
    15 mM 0.1134 mL 0.5672 mL 1.1344 mL 2.8361 mL
    20 mM 0.0851 mL 0.4254 mL 0.8508 mL 2.1270 mL
    25 mM 0.0681 mL 0.3403 mL 0.6807 mL 1.7016 mL
    30 mM 0.0567 mL 0.2836 mL 0.5672 mL 1.4180 mL
    40 mM 0.0425 mL 0.2127 mL 0.4254 mL 1.0635 mL
    50 mM 0.0340 mL 0.1702 mL 0.3403 mL 0.8508 mL
    60 mM 0.0284 mL 0.1418 mL 0.2836 mL 0.7090 mL
    80 mM 0.0213 mL 0.1064 mL 0.2127 mL 0.5318 mL
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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.

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