A selective nonphosphoinositide inhibitor with favorable solubility in vivo that specifically disrupts PIP3/Akt PH domain binding (IC50 = 27 μM); suppresses PI3K-PDK1-Akt-dependent phosphorylation

3,5-dimethyl PIT-1 – 5 mg

Brand:
Cayman
CAS:
701947-53-7
Storage:
-20
UN-No:
Non-Hazardous - /

PtdIns-(3,4,5)-P3 (PIP3) serves as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains such as phosphatidylinositol 3-kinase (PI3K) or PTEN. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking and initiates an intricate signaling cascade that has been implicated in cancer.{12235} 3,5-dimethyl PIT-1 is a dimethyl analog of PIT-1, the selective inhibitor of PIP3/Akt PH domain binding, that is designed for more favorable solubility in vivo. 3,5-dimethyl PIT-1 inhibits PI3K/Akt signaling (IC50 = 27 μM), suppressing PI3K-PDK1-Akt-dependent phosphorylation, which has been shown to reduce cell viability and induce apoptosis in PTEN-deficient U87MG glioblastoma cells (IC50 = 36 μM).{18957} 4T1 breast cancer growth is significantly attenuated in BALB/c mice with a dose of 1 mg/kg of 3,5-dimethyl PIT-1 per day.  

 

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SKU: 10727 - 5 mg Category:

Description

A selective nonphosphoinositide inhibitor with favorable solubility in vivo that specifically disrupts PIP3/Akt PH domain binding (IC50 = 27 μM); suppresses PI3K-PDK1-Akt-dependent phosphorylation, which reduces cell viability and induces apoptosis in PTEN-deficient U87MG glioblastoma cells (IC50 = 36 μM)

Formal name: N-[[(2-hydroxy-5-nitrophenyl)amino]thioxomethyl]-3,5-dimethyl-benzamide

Synonyms: 

Molecular weight: 345.4

CAS: 701947-53-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling

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