3,5-dimethyl PIT-1 T35491

Product Introduction
Bioactivity


英文名: 3,5-dimethyl PIT-1

描述: 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. 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). 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMF : 30 mg/mL
DMF:PBS(pH 7.2)(1:1) : 0.5 mg/mL
DMSO : 20 mg/mL
Ethanol : 0.2 mg/mL


关键字: 3,5 dimethyl PIT 1 | 3,5dimethyl PIT1 | 3,5-dimethyl PIT-1

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