1. MAPK/ERK Pathway
    Stem Cell/Wnt
    Epigenetics
  2. ERK
    Epigenetic Reader Domain
  3. XMD8-92

XMD8-92 

Cat. No.: HY-14443 Purity: 99.93%
Handling Instructions

XMD8-92 is a potent ERK5 (BMK1)/BRD4 inhibitor with Kds of 80 and 190 nM, respectively. XMD8-92 inhibits DCAMKL2, PLK4 and TNK1 with Kds of 190, 600 and 890 nM, respectively. Anti-cancer activity.

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

XMD8-92 Chemical Structure

XMD8-92 Chemical Structure

CAS No. : 1234480-50-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
10 mg USD 100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 350 In-stock
Estimated Time of Arrival: December 31
100 mg USD 590 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 9 publication(s) in Google Scholar

Top Publications Citing Use of Products

    XMD8-92 purchased from MCE. Usage Cited in: Sci Signal. 2014 Oct 28;7(349):ra102.

    Activation of ERK5 in neuroblastoma cell lines expressing activated ALK. (A to C) Immunoblotting for the indicated proteins in neuroblastoma cells CLB-BAR (A), CLB-GE (B), and IMR32 (C) cultured on six-well plates in complete growth medium and treated with inhibitors as indicated for 6 hours alone (A and B) or before (C) stimulation with mAb46 for 30 min.

    XMD8-92 purchased from MCE. Usage Cited in: PLoS One. 2015 Apr 17;10(4):e0125054.

    The induction of c-Fos is blocked by inhibition of the ERK5 pathway. 4B12 cells (2.5 × 104) are pretreated with or without BIX02189 or XMD8-92 for 6 hrs and then cultured in the presence of M-CSF (10 ng/mL) for 24 hrs. The expression of c-Fos is measured by Western blot analysis.

    XMD8-92 purchased from MCE. Usage Cited in: Stem Cell Reports. 2018 Oct 9;11(4):929-943.

    Immunoblotting of total cell lysates of CML cell lines; tubulin is a loading control; representative images from four independent experiments.

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    Description

    XMD8-92 is a potent ERK5 (BMK1)/BRD4 inhibitor with Kds of 80 and 190 nM, respectively. XMD8-92 inhibits DCAMKL2, PLK4 and TNK1 with Kds of 190, 600 and 890 nM, respectively. Anti-cancer activity[1][2].

    IC50 & Target[1]

    BMK1

    80 nM (Kd)

    BRD4

    190 nM (Kd)

    In Vitro

    XMD8-92 (0-5 Μm; 48 hours) inhibits the proliferation of HMEC and cancer cells[1].
    XMD8-92 effectively inhibits BMK1 activation as well as induces PML’s (promyelocytic leukemia protein) downstream effector, p21. XMD8-92 significantly inhibits basic fibroblast growth factor (bFGF) induced angiogenesis in Matrigel plugs. XMD8-92 significantly induces p21 expression in HeLa and A549 cells[1].

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

    Cell Viability Assay[1]

    Cell Line: HMEC, A549 and HeLa cells
    Concentration: 0.16, 0.32, 0.63, 1.25, 2.5 or 5 μM
    Incubation Time: 48 hours
    Result: Inhibited the proliferation of HMEC and cancer cells.
    In Vivo

    XMD8-92 (i.p.; twice a day for 28 days) significantly inhibits the growth of the xenografted human tumors[1].

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

    Animal Model: HeLa Xenograft Model (6-week-old Nod/Scid mice)[1]
    Dosage: 50 mg/kg
    Administration: I.p.; twice a day for 28 days
    Result: Significantly inhibited the growth of the xenografted human tumors.
    Molecular Weight

    474.55

    Formula

    C₂₆H₃₀N₆O₃

    CAS No.

    1234480-50-2

    SMILES

    CN(C1=O)C2=CN=C(N=C2N(C3=C1C=CC=C3)C)NC4=C(C=C(C=C4)N5CCC(CC5)O)OCC

    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 : 50 mg/mL (105.36 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1073 mL 10.5363 mL 21.0726 mL
    5 mM 0.4215 mL 2.1073 mL 4.2145 mL
    10 mM 0.2107 mL 1.0536 mL 2.1073 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: ≥ 2.5 mg/mL (5.27 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (5.27 mM); Clear solution

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

    XMD8-92ERKEpigenetic Reader DomainExtracellular signal regulated kinasespromyelocyticleukemiaproteinHMECcancerbFGFInhibitorinhibitorinhibit

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    Product Name:
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    Cat. No.:
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