My cart
In the shopping cart is not goods, to choose and buy!
  • Product Name
  • Size
  • Quantity
  • Amount
    Selected items : 0 pieces Total : CHECK OUT()
    DTP3
    DTP3

    Price:
    Market Price:

    This product is for research use only, not for human use. We do not sell to patients.
    Number: - + Pieces(InventoryPieces)
    InvivoChem Cat #: V0474
    CAS #: 1809784-29-9Purity ≥98%

    Description: DTP3 (DTP-3) is a novel, potent and selective inhibitor of GADD45β/MKK7 ((growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) with potential anticancer activity. It inhibits cancer-selective NF-κB survival pathway. DTP3 exhibits potent antitumor activity against MM in mouse plasmacytoma model. It acts by binding to MKK7, DTP3 dissociated the GADD45b/MKK7 complex through an allosteric mechanism and causing conformational rearrangement of the kinase. In both MM and non-MM cell lines with high expression of GADD45B, DTP3 inhibited cell growth and displayed potent and selective activity and was completely inactive in tumor cell lines with low GADD45B expression. 

    References: Cancer Cell. 2014 Oct 13;26(4):495-508.

    Customer Validation
    Official Supplier of
    • VE
    • OF
    • YALE
    • hhmi
    • 香港大学
    Related Products
    Publications Citing InvivoChem Products
    • Physicochemical and Storage Information
    • Protocol
    • Quality Control Documentation
    • Related Biological Data
    • Customer Review
    Molecular Weight (MW)525.6
    FormulaC26H35N7O5
    CAS No.1809784-29-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (190.3 mM)
    Water: 100 mg/mL (190.3 mM)
    Ethanol: N/A
    SMILESCC(N[[email protected]](CC1=CC=C(O)C=C1)C(N[[email protected]](CCCNC(N)=N)C(N[[email protected]](CC2=CC=CC=C2)C(N)=O)=O)=O)=O
    SynonymsDTP 3; DTP3; DTP-3


    • Molarity Calculator
    • Dilution Calculator
    • The molarity calculator equation

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

      • Mass
      • Concentration
      • Volume
      • Molecular Weight *
      • =
      • ×
      • ×
    • The dilution calculator equation

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

      This equation is commonly abbreviated as: C1V1 = C2V2

      • Concentration (start)
      • ×
      • Volume (start)
      • =
      • Concentration (final)
      • ×
      • Volume (final)
      • ×
      • =
      • ×
      • C1
      •  
      • V1
      •  
      • C2
      •  
      • V2

    <

    In Vitro

    In vitro activity: DTP3 physically interacts with MKK7, both in isolation and within the complex with GADD45β, and dissociates the GADD45β/MKK7 complex via an allosteric mechanism. DTP3 selectively kills cells and induces apoptosis in MM cells with functional MKK7 and elevated GADD45β expression without toxicity to normal cells. In addition, DTP3 displays synergistic activity with bortezomib in two different MM cell lines, exhibiting a combination index of 0.21 in U266 cells and of 0.56 in KMS-12 cells.


    Kinase Assay: The stoichiometry and KD value of the DTP3/MKK7 interaction are determined by tryptophan fluorescence quenching analysis, after fitting the fluorescence data with a nonlinear regression algorithm. 


    Cell Assay: [3H]Thymidine incorporation assays are performed using standard protocols. Briefly, cell lines (CD138+ cells) are seeded into wells of 96-well plates at a concentration of 1.0x104 cells/well and then left untreated or treated daily with the indicated concentrations of peptides and maintained in complete RPMI-1640 medium at 37°C in 5% CO2, splitting them with medium as necessary. At 24, 72 or 144 hr, cells are incubated for an additional 16 hr with 0.037 MBq/well of [3H]thymidine, and then harvested onto glass fibre filter mats using a 96-well plate automated Tomtec cell harvester and analyzed by liquid scintillation spectroscopy with a LKB Wallac Trilux Microbeta 3-counter. Values are expressed as the percentage of the counts per minute (cpm) measured in the treated cultures relative to the cpm measured in the respective untreated cultures. The IC50 values are calculated using either 5 or 7 concentrations of compound and are defined as the mean concentration of compound inducing 50% inhibition of [3H]thymidine uptake relative to the uptake measured in untreated cells. Trypan blue exclusion assays are performed. Briefly, cells from lentivirus-infected cell lines are seeded into wells of 48-well plates in complete medium at a concentration of 2.0x105 cells/well, and then cultured at 37°C in 5% CO2, splitting them as necessary during the assays. Cell viability is monitored over a period of up to 8 days by cell counting using trypan blue, and the numbers of live infected cells in the cultures are extrapolated, where appropriate, from the cell counts by accounting for the percentages of eGFP+ cells, using flow cytometry. Values are expressed as the percentage of live infected cells present in the cultures at the times indicated relative to the number of live infected cells present in the same cultures at day 0.

    In Vivo DTP3 (14.5 mg/kg/day) exhibits potent antitumor activity against MM in mouse plasmacytoma model.
    Animal model SCID mice implanted with U266 or KMS-11 MM cells
    Formulation & DosageDissolved in PBS; 14.5 mg/kg/day; Administered through Alzet osmotic pump
    References

    Cancer Cell. 2014 Oct 13;26(4):495-508.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    DTP3

    The High Target Specificity of DTP3 in Cells. Cancer Cell. 2014 Oct 13; 26(4): 495–508.

    DTP3

    DTP3

    The High Target Specificity of DTP3 in Cells. Cancer Cell. 2014 Oct 13; 26(4): 495–508.

    DTP3

    DTP3 Exhibits Potent Therapeutic Activity against MM, In Vivo, in the Absence of Any Apparent Side Effects. Cancer Cell. 2014 Oct 13; 26(4): 495–508.


    DTP3 Exhibits Potent Therapeutic Activity against MM, In Vivo, in the Absence of Any Apparent Side Effects. Cancer Cell. 2014 Oct 13; 26(4): 495–508.


    评论

      Home Prev Next Last page / pices

      发评论

      ×
      Your information is safe with us. * Required Fields.
      Products are for research use only;  We do not sell to patients
      Tel: 1-708-310-1919
      Fax: 1-708-557-7486
      Subscribe to our E-newsletter
      • Name*
      • *
      • E-mail*
      • *
      • instructions:
      • *
      Copyright 2020 InvivoChem LLC | All Rights Reserved
      prompt
      Do you confirm the receipt?