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3,5-dimethyl PIT-1

CAT: 0931-T35491-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0931-T35491-01Size:1 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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CAS Number
701947-53-7
Target
Apoptosis, Others, PI3K
Related Pathways
Others, PI3K/Akt/mTOR signaling, Apoptosis
Bioactivity
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.
Smiles
CC1=CC(=CC(C)=C1)C(=O)NC(=S)NC1=C(O)C=CC(=C1)[N+]([O-])=O
Molecular Formula
C16H15N3O4S
Molecular Weight
345.37
Shipping Conditions
Ice Packs
Storage Temperature
-20°C

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