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PHT-427

Catalog No.
A5884
Akt and PDPK1 inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$55.00
In stock
10mg
$50.00
In stock
50mg
$190.00
In stock
100mg
$320.00
In stock

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Email: [email protected]

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Background

PHT-427 is an inhibitor of Akt and PDPK1 (Ki =2.7 μM and 5.2 μM, respectively).

Akt is a serine/threonine-specific protein kinase that plays a vital role in multiple cellular processes including glucose metabolism, apoptosis, cell proliferation, transcription and cell migration etc.

In BxPC-3 cells, PHT-427 showed inhibition upon Akt function with IC50 value of 8.6±0.8 μM and for its downstream substrates. PHT-427 reduced the Akt phosphorylation on Ser473 residue and did not decrease total Akt protein level. PHT-427 also inhibited p70S6K and GSK3β in a dose-dependent manner. [1][2]

In SCID (severe combined immunodeficiency) mice of BxPC-3 pancreatic cancer xenografts, administration of PHT-427 exerted prominent antitumor activity that halted tumor growth. PHT-427 in combination with erlotinib exhibited greater than additive antitumor activity in NSC lung cancer and with paclitaxel in breast cancer. [1][2]

References:
1. Meuillet EJ, Zuohe S, Lemos R et al.  Molecular pharmacology and antitumor activity of PHT-427, a novel Akt/phosphatidylinositide-dependent protein kinase 1 pleckstrin homology domain inhibitor. Mol Cancer Ther. 2010 Mar;9(3):706-17.
2. Moses SA, Ali MA, Zuohe S et al.  In vitro and in vivo activity of novel small-molecule inhibitors targeting the pleckstrin homology domain of protein kinase B/AKT. Cancer Res. 2009 Jun 15;69(12):5073-81.

Chemical Properties

StorageStore at -20°C
M.Wt409.61
Cas No.1191951-57-1
FormulaC20H31N3O2S2
Solubility≥20.5mg/mL in DMSO, ≥51.1 mg/mL in EtOH with ultrasonic,insoluble in H2O
Chemical Name4-dodecyl-N-(1,3,4-thiadiazol-2-yl)benzenesulfonamide
SDFDownload SDF
Canonical SMILESCCCCCCCCCCCCC1=CC=C(C=C1)S(=O)(=O)NC2=NN=CS2
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Biological Activity

Description PHT-427 is an inhibitor of Akt and PDPK1 with Ki values of 2.7 μM and 5.2 μM, respectively.
Targets Akt PDK-1        
IC50 2.7 μM(Ki) 5.2 μM(Ki)        

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