An inhibitor of PIP3/protein binding
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3,5-dimethyl PIT-1

Item No. 10727

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[[(2-hydroxy-5-nitrophenyl)amino]thioxomethyl]-3,5-dimethyl-benzamide
CAS Number
701947-53-7
Molecular Formula
C16H15N3O4S
Formula Weight
345.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 20 mg/mlEthanol: 0.2 mg/ml
λmax
202, 274 nm
SMILES
O=C(NC(NC1=C(O)C=CC([N+]([O-])=O)=C1)=S)C2=CC(C)=CC(C)=C2
InChi Code
InChI=1S/C16H15N3O4S/c1-9-5-10(2)7-11(6-9)15(21)18-16(24)17-13-8-12(19(22)23)3-4-14(13)20/h3-8,20H,1-2H3,(H2,17,18,21,24)
InChi Key
CGWBCAQMXJFWBU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $29

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    5 mg

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    10 mg

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    25 mg

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    Cayman Chemical
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    Product Description

    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.1 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).2 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Vivanco, I., and Sawyers, C.L. The phosphatidylinositol 3-kinase-AKT pathway in human cancer. Nat. Rev. Cancer 2(7), 489-501 (2002).

    2. Miao, B., Skidan, I., Yang, J., et al. Small molecule inhibition of phosphatidylinositol-3,4,5-triphosphate (PIP3) binding to pleckstrin homology domains. Proc. Natl. Acad. Sci. USA 107(46), 20126-20131 (2010).