PHT-427

Catalog No.S1556 Synonyms: CS-0223

PHT-427 Chemical Structure

Molecular Weight(MW): 409.61

PHT-427 is a dual Akt and PDPK1 inhibitor (high affinity binding for the PH domains of Akt and PDPK1) with Ki of 2.7 μM and 5.2 μM, respectively.

Size Price Stock Quantity  
In DMSO USD 90 In stock
USD 70 In stock
USD 270 In stock
USD 770 In stock
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2 Customer Reviews

  • Luciferase reporter assays. 32D/BCR-ABL cells transfected with the reporter construct containing 1548 bp of the Atf5 promoter were treated with either DMSO, imatinib (5 μM for 24 hours), LY294002 (20 μM for 48 hours), PHT-427 (20 μM for 24 hours), or JAK inhibitor I (10 μM for 24 hours). Error bars represent SD.

    Blood 2011 118, 2840-2848. PHT-427 purchased from Selleck.

    The inhibition of PI3K/Akt pathway is involved in ATG-induced FOXO3a dephosphorylation in PDGF-BB-activated HSCs. Serum-starved LX-2 human HSCs were pretreated with or without DMSO (vehicle) or ATG (0.5 uM) for 4 h, in the absence or presence of PI3K inhibitor LY294002 (20 uM) or Akt inhibitor PHT-427 (20 uM), and then incubated with or without 50 ng/ml PDGF-BB for 4 h. After treatment, aliquots of whole cell lysates were collected and subjected to Western blotting analysis. The experiments were repeated three times with similar results and a representative blot was shown for each protein. Total protein levels of Akt and FOXO3a served as internal controls.

    Eur J Pharmacol 2014 747C, 71-87. PHT-427 purchased from Selleck.

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Biological Activity

Description PHT-427 is a dual Akt and PDPK1 inhibitor (high affinity binding for the PH domains of Akt and PDPK1) with Ki of 2.7 μM and 5.2 μM, respectively.
Targets
Akt [1] PDK1 [1]
2.7 μM(Ki) 5.2 μM(Ki)
In vitro

PH-427 is a pleckstrin homology domain inhibitor to Akt/PDPK1. PH-427 significantly reduces phospho-Ser241-PDPK1 phospho-Thr308-Akt in PC-3 prostate cancer cells at 10 μM, which shows that PHT-427 could inhibit both Akt and PDPK1. PHT-427 also inhibits translocation of the Akt and PDPK1 PH domains in plasma membrane. [1] PHT-427 induces apoptosis and inhibits AKT phosphorylation with IC50 of 8.6 μM (in BxPC-3 cells), which mainly on its Ser473 residue and less strongly on Thr308 residue without affecting total Akt protein expression. PHT-427 also shows antiproliferation in Panc-1 cells with IC50 of 65 μM. [2]

In vivo PHT-427 shows great antitumor activity in BxPC-3 pancreatic, MCF-7 breast and A-549 NSCL cancer xenografts. PHT-427 gives up to an 80% inhibition of tumor growth in BxPC-3 at doses of 125 to 250 mg/kg. [1]

Protocol

Kinase Assay:[1]
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Surface plasmon resonance (SPR) spectroscopy binding assays:

All interaction analyses are performed with a Biacore 2000, Biacore 2000 Control Software v3.2, and BIAevaluation v4.1 analysis software. The PH domain GST-fusion proteins (Akt1, IRS1, and PDK1) are immobilized on a CM5 Sensorchip using Biacore's Amine Coupling Kit to a level of 10,000 Response units (RUs). Small molecule analytes at concentrations ranging from 0.1 to 10 × the predicted KD are injected at a high flow rate (30μL/min). DMSO concentrations in all samples and running buffer are 1% (v/v) or less.
Animal Research:[1]
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  • Animal Models: BxPC-3, Panc-1, MiaPaCa-2, PC-3, SKOV-3, A-549 or MCF-7 cells are injected subcutaneously into the flanks of female scid mice.
  • Formulation: 40 to 50 mg/mL in sesame seed oil
  • Dosages: 125-250 mg/kg
  • Administration: Oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 82 mg/mL (200.19 mM)
Ethanol 60 mg/mL (146.48 mM)
Water slightly soluble or insoluble
In vivo Add solvents individually and in order:
5% DMSO+95% Corn oil
5 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 409.61
Formula

C20H31N3O2S2

CAS No. 1191951-57-1
Storage powder
in solvent
Synonyms CS-0223

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID