PHT-427 - Moligand™, 10mM in DMSO , Inhibitor of 3-phosphoinositide dependent protein kinase 1;Inhibitor of AKT serine/threonine kinase 2, CAS No.1191951-57-1, Inhibitor of 3-phosphoinositide dependent protein kinase 1;Inhibitor of AKT serine/threonine kinase 2

CAS: 1191951-57-1 Cat. No.: P409008 Molecular Weight: 409.61

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

4-dodecyl-N-(1,3,4-thiadiazol-2-yl)benzenesulfonamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

PHT-427 PHT-427 (CS-0223) is a dual Akt and PDPK1 inhibitor (high affinity binding for the PH domains of Akt and PDPK1) with K i of 2.7 μM and 5.2 μM, respectively.
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. 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.

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.
Cell Data

cell lines：

Concentrations：1-50 μM

Incubation Time：Incubation Time:

Powder Purity:≥99%

Specifications

Synonyms

4-dodecyl-N-(1, 3, 4-thiadiazol-2-yl)benzenesulfonamide

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

PHT-427 (CS-0223) is a dual Akt and PDPK1 inhibitor (high affinity binding for the PH domains of Akt and PDPK1) with K_i of 2.7 μM and 5.2 μM, respectively.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Inhibitor of 3-phosphoinositide dependent protein kinase 1;Inhibitor of AKT serine/threonine kinase 2

Names and Identifiers

• Isomeric SMILES: CCCCCCCCCCCCC1=CC=C(C=C1)S(=O)(=O)NC2=NN=CS2
• Molecular Weight: 409.61
• Reaxy-Rn: 19687633
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=19687633&ln=

Associated Targets(Human)

AKT2 Tchem RAC-beta serine/threonine-protein kinase (1 Activities)

Discover Target: AKT2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDPK1 Tchem 3-phosphoinositide-dependent protein kinase 1 (1 Activities)

Discover Target: PDPK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)