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

SCH772984 

Cat. No.: HY-50846 Purity: 98.06%
Handling Instructions

SCH772984 potently inhibits ERK1 and ERK2 activity with IC50s of 4 and 1 nM, respectively.

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

SCH772984 Chemical Structure

SCH772984 Chemical Structure

CAS No. : 942183-80-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 186 In-stock
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
Estimated Time of Arrival: December 31
10 mg USD 216 In-stock
Estimated Time of Arrival: December 31
50 mg USD 648 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1008 In-stock
Estimated Time of Arrival: December 31
200 mg USD 1680 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

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Customer Review

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

    The role of Semaphorin4D in bone invasion by oral cancer.

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

    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 MCE. Usage Cited in: J Neuroinflammation. 2017 Nov 25;14(1):228.

    HSP70 release induced by morphine is reversed by ERK1/2 inhibitor in SH-SY5Y cells. SCH772984 (ERK1/2 inhibitor, 2 μM) is given 15 min before Morphine (200 μM, 12 h) administration. Supernatants are collected and analyzed by western blot (n=3).

    SCH772984 purchased from MCE. Usage Cited in: J Immunol Res. 2018 Jun 7;2018:6249085.

    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 MCE. Usage Cited in: Theranostics. 2018 Jul 30;8(15):4262-4278.

    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 MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Jan 1;495(1):781-786.

    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 MCE. Usage Cited in: Cancer Res. 2018 Feb 15;78(4):891-908.

    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 MCE. Usage Cited in: Acta Pharmaceutica Sinica 2018, 53 (4): 553-560.

    Validation of differentially expressed MAPK/ERK pathway proteins by Western blot.

    SCH772984 purchased from MCE. 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: Trametinib (GSK212) 100 nM; GDC0623 100 nM or SCH772984 1 µM.

    SCH772984 purchased from MCE. Usage Cited in: Acta Biomater. 2019 Feb;85:106-116.

    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 MCE. Usage Cited in: Sci Rep. 2019 Jan 29;9(1):907.

    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 MCE. Usage Cited in: Sci Rep. 2019 Jan 29;9(1):907.

    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 MCE. Usage Cited in: Sci Rep. 2019 Jan 29;9(1):907.

    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.

    View All ERK Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    SCH772984 potently inhibits ERK1 and ERK2 activity with IC50s of 4 and 1 nM, respectively.

    IC50 & Target

    IC50: 4/1 nM (ERK1/2)[1]

    In Vitro

    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. Flow cytometric analysis of SCH772984-sensitive melanoma cells revealed a G1 arrest as well as an increase in the sub-G1 fraction indicative of apoptosis. Less than 20% of cells wild-type for both RAS and BRAF (n=61) are sensitive to SCH772984[1].

    In Vivo

    Treatment of BRAF-mutant LOX melanoma xenografts with SCH772984 (50 mg/kg twice daily) leads to 98% tumor regression. 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].

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 51 mg/mL (86.78 mM)

    *"≥" means soluble, but saturation unknown.

    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
    10 mM 0.1702 mL 0.8508 mL 1.7016 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Kinase Assay
    [1]

    SCH772984 is tested in 8-point dilution curves in duplicate against purified ERK1 or ERK2. The enzyme is added to the reaction plate and incubated with the compound before adding a solution of substrate peptide and ATP. Fourteen microliters of diluted enzyme (0.3 ng active ERK2 per reaction) is added to each well of a 384-well plate. The plates are gently shaken to mix the reagents and incubated for 45 minutes at room temperature. The reaction is stopped with 60 μL of IMAP Binding Solution (1:2,200 dilutions of IMAP beads in 1× binding buffer). The plates are incubated at room temperature for an additional 0.5 hours to allow complete binding of phosphopeptides to the IMAP beads. Plates are read on the LJL Analyst[1].

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

    Cell Assay
    [1]

    Cell proliferation experiments are carried out in a 96-well format (six replicates), and the BRAFV600E-mutant human melanoma cell line LOXIMV1 (LOX) are plated at a density of 4,000 cells per well. At 24 hours after cell seeding, cells are treated with DMSO or a 9-point IC50 dilution (0.001-10 μM) at a final concentration of 1% DMSO for all concentrations. Viability is assayed 5 days after dosing using the ViaLight luminescence kit. For the cell line panel viability assay, cells are treated with SCH772984 for 4 days and assayed by the CellTiterGlo luminescent cell viability assay[1].

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

    Animal Administration
    [1]

    Mice[1]
    Nude mice are injected subcutaneously with specific cell lines, grown to approximately 100 mm3, randomized to treatment groups (10 mice/group), and treated intraperitoneally with either SCH772984 (12.5, 25, or 50 mg/kg) or vehicle. Tumor length (L), width (W), and height (H) are measured during and after the treatment periods by a caliper twice weekly on each mouse and then used to calculate tumor volume using the formula (L×W×H)/2. Animal body weights are measured on the same days twice weekly. Upon completion of the experiment, vehicle- and SCH772984-treated tumor biopsies are processed for Western blot analysis.

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

    References
    Molecular Weight

    587.67

    Formula

    C₃₃H₃₃N₉O₂

    CAS No.

    942183-80-4

    SMILES

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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

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    Product Name:
    SCH772984
    Cat. No.:
    HY-50846
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    Cat. No.: HY-50846