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

XMD17-109 

Cat. No.: HY-15665 Purity: 99.44%
Handling Instructions

XMD17-109 is a novel, specific ERK-5 inhibitor, with an IC50 of 162 nM.

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

XMD17-109 Chemical Structure

XMD17-109 Chemical Structure

CAS No. : 1435488-37-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 236 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 168 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 264 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 744 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

    XMD17-109 purchased from MCE. Usage Cited in: Oncotarget. 2016 Jun 7;7(23):34322-40.

    HCT116 parental cells are treated for up to 48 h with increasing doses of 5-FU in combination with 4 μM XMD8-92 or 2 μM XMD17-109, two highly-selective ERK5 pharmacological inhibitors.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    XMD17-109 is a novel, specific ERK-5 inhibitor, with an IC50 of 162 nM.

    IC50 & Target[1]

    ERK5

    162 nM (IC50)

    LRRK2[G2019S]

    339 nM (IC50)

    In Vitro

    XMD17-109 (Compound 26) inhibits ERK5 biochemically with an IC50 of 0.162 ± 0.006 μM, and blocks pidermal growth factor induced ERK5 autophosphorylation with an EC50 of 0.09 ± 0.03 μM in cells. XMD17-109 also inhibits LRRK2[G2019S] with an IC50 of 339 nM[1]. XMD17-109 demonstrats low nanomolar cellular activity judged by the significant dose-dependent reduction of mobility shifted phosphorylated ERK5 bands from sorbitol stimulated cells. XMD17-109 completely inhibits the ERK5-mediated AP1 transcriptional activity at 30 μM and has an EC50 of 4.2 μM[2].

    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 1.5654 mL 7.8272 mL 15.6544 mL
    5 mM 0.3131 mL 1.5654 mL 3.1309 mL
    10 mM 0.1565 mL 0.7827 mL 1.5654 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [2]

    HeLa cells are maintained in DMEM supplemented with 10% FBS, 2 mM l-glutamine, 50 U/mL penicillin G, and 50 μg/mL streptomycin. Before use HeLa cells are serum starved for 16 h in DMEM supplemented with 2 mM l-glutamine, 50 U/mL penicillin G, and 50 μg/mL streptomycin. HeLa cells are then incubated with ERK5-IN-1 at the indicated concentrations for 1 h prior to stimulation with 0.5mol/Lsorbitol for 30 min. Cells are lysed in Triton lysis buffer (50 mM Tris-HCl, pH 7.5, 1 mM EGTA, 1 mM EDTA, 1 mM sodium orthovanadate, 50 mM sodium fluoride, 1 mM sodium pyrophosphate, 0.27mol/Lsucrose, 1 μM microcystin-LR, 1% (v/v) Triton X-100, 0.1% (v/v) 2-mercaptoethanol) and 20 μg of protein loaded per well. Samples are run on 8% polyacrylamide gels using standard methods. Proteins are transferred onto nitrocellulose membranes and specific proteins detected by immunoblotting. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    638.8

    Formula

    C₃₆H₄₆N₈O₃

    CAS No.

    1435488-37-1

    SMILES

    O=C1C2=C(C=CC=C2)N(C3CCCC3)C4=NC(NC5=C(OCC)C=C(C(N6CCC(N7CCN(C)CC7)CC6)=O)C=C5)=NC=C4N1C

    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

    Solvent & Solubility

    10 mM in DMSO

    XMD17-109 is dissolved in 30% (2-hydroxypropyl)-β-cyclodextrin[2].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

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    Product Name:
    XMD17-109
    Cat. No.:
    HY-15665
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