1. PI3K/Akt/mTOR
  2. PDK-1
  3. GSK2334470

GSK2334470 

Cat. No.: HY-14981 Purity: 99.78%
COA Handling Instructions

GSK2334470 is a highly specific and potent inhibitor of PDK1 with an IC50 of 10 nM.

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

GSK2334470 Chemical Structure

GSK2334470 Chemical Structure

CAS No. : 1227911-45-6

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Solution
10 mM * 1 mL in DMSO USD 109 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 109 In-stock
Estimated Time of Arrival: December 31
Solid
10 mg USD 99 In-stock
Estimated Time of Arrival: December 31
50 mg USD 330 In-stock
Estimated Time of Arrival: December 31
100 mg USD 550 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Customer Review

Based on 6 publication(s) in Google Scholar

Top Publications Citing Use of Products

    GSK2334470 purchased from MCE. Usage Cited in: Br J Cancer. 2020 Aug;123(4):542-555.  [Abstract]

    The combination of the PDK1 inhibitor GSK2334470 with AKT inhibitors of either class potentiated cell death in MDA-MB-361 cells
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GSK2334470 is a highly specific and potent inhibitor of PDK1 with an IC50 of 10 nM.

    IC50 & Target

    IC50: 10 nM(PDK1)[1]

    In Vitro

    Small molecule GSK2334470 inhibits PDK1 with an IC50 of ~10 nM, but does not suppress the activity of 93 other protein kinases including 13 AGC-kinases most related to PDK1 at 500-fold higher concentrations. Addition of GSK2334470 ablates T-loop residue phosphorylation and activation of SGK isoforms and S6K1 induced by serum or IGF-1 (insulin-like growth factor 1). GSK2334470 and AZD8055 effectively inhibite phosphorylation of PDK1 and mTOR, respectively, and induce higher G0–G1 ratio in LAN-1-MK than that in LAN-1 as well. PDK1 and mTOR inhibitors effecte on phosphorylation of GSK3β in some of resistant sublines[2].

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

    In Vivo

    The efficacy of the PDK1 inhibitor (PDKi) GSK2334470 is tested in newborn BrafV600E::Pten−/−mice subjected to systemic administration of 4-HT. Twice weekly administration of PDK1 results in marked inhibition of pigmented lesions and concomitant melanomagenesis, as well as significant inhibition of lung metastases, seen by H&E staining-based quantification (~80%), and lymph node metastases as by S100 immunostaining, similar to the phenotype seen upon genetic ablation of Pdk1[3].

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

    Molecular Weight

    462.59

    Formula

    C25H34N8O

    CAS No.
    SMILES

    O=C([[email protected]@H]1CN(C2=NC(NC)=NC(C3=CC4=C(C=C3)C(N)=NN4)=C2)[[email protected]](C)CC1)NC5CCCCC5

    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 (108.09 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1617 mL 10.8087 mL 21.6174 mL
    5 mM 0.4323 mL 2.1617 mL 4.3235 mL
    10 mM 0.2162 mL 1.0809 mL 2.1617 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 (5.40 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (5.40 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2.5 mg/mL (5.40 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.78%

    References
    Cell Assay
    [2]

    GSK2334470 is dissolved in DMSO and diluted with appropriate medium before use. To study the inhibitory effect of GSK2334470 on mTOR-S6K pathway, non-resistant cells and the resistant sublines are treated with GSK2334470 at 5 μM for 1.5 and 12 h in 10 % FBS medium with/without MK-2206 (5 μM)[2].

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

    Animal Administration
    [3]

    Mice is dissolved in DMSO and then diluted with PBS or saline. BrafV600E::Pten−/− are generated as previously described. Cohorts of six animals per group are used in each experimental group. GSK2334470 is administered through IP injection (100 mg/kg) 3 times per week starting the same day of topical administration of 4-hydroxytamoxifen and ending at the time of mouse collection, based on earlier studies[3].

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

    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    GSK2334470
    Cat. No.:
    HY-14981
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