产品名称
Pit-1, ≥98% (HPLC)
SMILES string
S=C(Nc2c(c(cc(c2)[N+](=O)[O-])Cl)O)NC(=O)c1ccccc1
InChI
1S/C14H10ClN3O4S/c15-10-6-9(18(21)22)7-11(12(10)19)16-14(23)17-13(20)8-4-2-1-3-5-8/h1-7,19H,(H2,16,17,20,23)
InChI key
RIGXBXPAOGDDIG-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to tan
solubility
DMSO: ≥14 mg/mL
storage temp.
2-8°C
Quality Level
Application
Pit-1 may be used in PIP3-mediated cell signaling studies.
Biochem/physiol Actions
PIT-1 represents a new class of molecules referred to as PITenins, or PITs. PITs inhibit the binding of PIP3 to the PH domains of several target proteins, including Akt and PDK1, without affecting interactions against PIP2-selective PH domains. PIT-1 inhibits PI3K-PKD-1-Akt dependent phosphorylation in cell based assays, including the phosphorylation of Akt-1, 2 and 3.
PIT-1 is a PIP3-PH domain antagonist
Pit-1 is a small-molecule phosphatidylinositol-3,4,5-trisphosphate (PIP3) antagonist that binds and blocks the pleckstrin domain. It shows inhibitory effects on tumor angiogenesis and metastasis by interfering with the activation of Akt.
Features and Benefits
This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound is featured on the PKB/Akt page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
wgk
WGK 3
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral - Aquatic Acute 1
存储类别
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
B Miao et al.
Oncogene, 31(39), 4317-4332 (2011-12-20)
We have reported previously the development of small-molecule phosphatidylinositol-3,4,5-trisphosphate (PIP3) antagonists (PITs) that block pleckstrin homology (PH) domain interaction, including activation of Akt, and show anti-tumor potential. Here we show that the same molecules inhibit growth factor-induced actin remodeling, lamellipodia
Benchun Miao et al.
Proceedings of the National Academy of Sciences of the United States of America, 107(46), 20126-20131 (2010-11-03)
The PI3-kinase (PI3K) pathway regulates many cellular processes, especially cell metabolism, cell survival, and apoptosis. Phosphatidylinositol-3,4,5-trisphosphate (PIP3), the product of PI3K activity and a key signaling molecule, acts by recruiting pleckstrin-homology (PH) domain-containing proteins to cell membranes. Here, we describe
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