Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
パッケージサイズ | 在庫状況 | 単価(税別) |
---|---|---|
1 mg | 約 35 days | ¥ 15,000 |
5 mg | 約 35 days | ¥ 64,000 |
10 mg | 約 35 days | ¥ 112,000 |
25 mg | 約 35 days | ¥ 243,500 |
説明 | 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. |
分子量 | 345.37 |
分子式 | C16H15N3O4S |
CAS No. | 701947-53-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMF: 30 mg/mL
Ethanol: 0.2 mg/mL
DMSO: 20 mg/mL
DMF:PBS(pH 7.2)(1:1): 0.5 mg/mL
You can also refer to dose conversion for different animals. 詳細
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3,5-dimethyl PIT-1 701947-53-7 3,5 dimethyl PIT 1 3,5dimethyl PIT1 Inhibitor inhibitor inhibit