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

SCH772984 

Cat. No.: HY-50846 Purity: 99.53%
Handling Instructions

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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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 186 In-stock
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5 mg USD 144 In-stock
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10 mg USD 216 In-stock
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50 mg USD 648 In-stock
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100 mg USD 1008 In-stock
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200 mg USD 1680 In-stock
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Customer Review

Based on 61 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE SCH772984

    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 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 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: 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 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.

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    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].

    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].

    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.

    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

    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 : 14.29 mg/mL (24.32 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    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.
    In Vivo:
    • 1.

      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

    • 2.

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

      Solubility: 1.43 mg/mL (2.43 mM); Suspended solution; Need ultrasonic

    • 3.

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

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

    • 4.

      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

    *All of the co-solvents are provided by MCE.
    References
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    Keywords:

    SCH772984SCH 772984SCH-772984ERKExtracellular signal regulated kinasesInhibitorinhibitorinhibit

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    Product Name:
    SCH772984
    Cat. No.:
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