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LY294002 Chemical Structure
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Biological Activity
LY 294002 has been shown to be a potent inhibitor of PI 3-kinase activity, acting as a competitive inhibitor for ATP binding site of the enzyme. LY 294002 inhibits cell proliferation of choroidal melanoma OCM-1 cells, the IC50 was observed about 10 μM, a concentration higher than, but compatible with, the one (1.4 μM) reported for in vitro inhibition of PI 3-kinase activity. [1]
LY 294002 is also an inhibitor of casein kinase II. Application of LY 294002 causes a substantial acceleration of MEPP frequency (150 μM) at the frog neuromuscular junction, through a mechanism that is independent of intraterminal calcium. LY 294002 causes the release of MEPPs through a perturbation of synaptotagmin function. [2]
References on LY294002
- [1] FEBS Letters 1998;422:385-390
- [2] Purinergic Signalling 2005;1: 389–394
Chemical Information
| Molecular Weight (WM): | 307.34 |
|---|---|
| Formula: | C19H17NO3 |
| CAS No.: | 154447-36-6 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥36mg/mL |
| Water <1mg/mL | |
| Ethanol ≥21mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
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Selleck's high quality products have been used in several published research findings, including the following:
Novel phosphoinositide 3-kinase/mTOR dual inhibitor, NVP-BGT226, displays potent growth-inhibitory activity against human head and neck cancer cells in vitro and in vivo.
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Average Customer Review
(3 customer reviews)
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We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.
We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.
Data independently produced by Saraswati Sukumar of Johns Hopkins University School of Medicine---LY294002 purchased from Selleck LY294002 purchased from Selleck
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Click to enlarge
different signal-inhibitory profile by applying 120 nmol/L BGT226, 20 mmol/L LY294002, or 100 nmol/L rapamycin in FaDu cells. - different signal-inhibitory profile by applying 120 nmol/L BGT226, 20 mmol/L LY294002, or 100 nmol/L rapamycin in FaDu cells.
Data from [Clin Cancer Res 2011.November;17:7116-26] LY294002 purchased from Selleck
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Click to enlarge
T47Dcells were pretreated with 100ng/ml EGF for 20 min and then treated with the indicated concentrations of LY294002 for 24 hours.
T47Dcells were pretreated with 100ng/ml EGF for 20 min and then treated with the indicated concentrations of LY294002 for 24 hours.
Data independently produced by Dr. Zhang of Tianjin Medical University LY294002 purchased from Selleck
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We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.
|
Data independently produced by Saraswati Sukumar of Johns Hopkins University School of Medicine---LY294002 purchased from Selleck
| different signal-inhibitory profile by applying 120 nmol/L BGT226, 20 mmol/L LY294002, or 100 nmol/L rapamycin in FaDu cells. |
Data from [Clin Cancer Res 2011.November;17:7116-26]
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