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化驗
≥98% (HPLC)
形狀
powder
顏色
white to tan
溶解度
DMSO: ≥14 mg/mL
儲存溫度
2-8°C
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 密鑰
RIGXBXPAOGDDIG-UHFFFAOYSA-N
應用
Pit-1 may be used in PIP3-mediated cell signaling studies.
生化／生理作用
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.
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
特點和優勢
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.
訊號詞
Warning
危險聲明
危險分類
Acute Tox. 4 Oral - Aquatic Acute 1
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
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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