PHT-427A pleckstrin homology domain inhibitor to Akt and PKB Kinase (PDPK1)

PHT-427 (CAS 1191951-57-1)

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Synonym: 4-dodecyl-N-(1,3,4-thiadiazol-2-yl)benzenesulfonamide
Application: A pleckstrin homology domain inhibitor to Akt and PKB Kinase (PDPK1)
CAS Number: 1191951-57-1
Purity: ≥98%
Molecular Weight: 409.61
Molecular Formula: C20H31N3O2S2
* Refer to Certificate of Analysis for lot specific data (including water content).
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PHT-427 is a a pleckstrin homology domain inhibitor with dual Akt and PKB Kinase (PDPK1) inhibitory activity(Ki values: Akt = 2.7 μM and PKB Kinase (PDPK1) = 5.2 μM). PHT-427 significantly reduces phosphorylation of phospho-Ser241-PKB Kinase (PDPK1) and phospho-Thr308-Akt in PC-3 prostate cancer cells which shows that PHT-427 could inhibit both Akt and PKB Kinase (PDPK1). PHT-427 also inhibits translocation of the Akt and PKB Kinase (PDPK1) PH domains in plasma membrane. PHT-427 induces apoptosis and inhibits Akt phosphorylation (IC50 = 6.3 μM), mainly on Akt Ser473 residue and less strongly on the Akt Thr308 residue without affecting total Akt protein expression. PHT-427 also shows antiproliferation in Panc-1 cells (IC50 = 65 μM).

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in DMSO (82 mg/ml), water (< 1 mg/ml), and ethanol (60 mg/ml).
Storage :
Store at -20° C
Boiling Point :
~535.0 °C at 760 mmHg (Predicted)
Density :
~1.2 g/cm3 (Predicted)
Refractive Index :
n20D 1.56 (Predicted)
IC50 :
Akt1: IC50 = 6.3 µM (human); BXPC-3: IC50 = 57 µM (human)
Ki Data :
RAC-alpha serine/threonine-protein kinase: Ki= 2.4 µM (mouse); Akt: Ki= 2.7 µM; PDK-1: Ki= 5.2 µM
pK Values :
pKa: 6.03 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
44240850
SMILES :
CCCCCCCCCCCCC1=CC=C(C=C1)S(=O)(=O)NC2=NN=CS2

Download SDS (MSDS)

Certificate of Analysis

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