Antibodies
LY294002
- 貨號 Cat. No.
- S1055
- 規格 Size
- 10~200mg
- 品牌 Brand
- Selleckchem
Description
LY294002
LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.twBiological Activity
| Description | LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. | |||||
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| Targets | p110α | p110δ | p110β | |||
| IC50 | 0.5 μM | 0.57 μM | 0.97 μM[1] | |||
| In vitro | LY294002 inactivates Akt/PKB, consequently inhibiting cell proliferation and inducing apoptosis. LY294002 demonstrates a remarkable growth-inhibitory and apoptosis-inducing effect in these colon cancer cell lines, with decreased expression of phosphorylated Akt (Ser473). [2]LY294002 induces marked nuclear pyknosis and diminished cytoplasmic volume in the tumor cells. Thus, LY294002 markedly inhibits ovarian cancer cell proliferation in vitro. LY294002 induces specific G1 arrest in cell growth, leading to almost complete inhibition of melanoma cell proliferation and partial inhibition of MG-63 (osteosarcoma cell line) proliferation. The effect of LY294002 on cell cycle progression may provide insights into a possible link between the PI3K activation pathway and cancer cell cycle regulation. [3] | |||||
| In vivo | LY294002 also results in suppression of tumor growth and induction of apoptosis, especially in the LoVo tumors, and therefore shows remarkable effectiveness in the mouse peritonitis carcinomatosa model. [2]LY294002 significantly inhibits growth and ascites formation of ovarian carcinoma. [3] | |||||
| Features | ||||||
Protocol(Only for Reference)
Kinase Assay: [4]
| kinase assays | PI3K inhibition by LY294002 is determined in a radiometric assay using purified, recombinant enzymes with 1 μM ATP. The kinase reaction is carried out for 1 hour at room temperature (24oC) and is terminated by addition of PBS. IC50 values are subsequently determined using a sigmoidal dose–response curve fit (variable slope). CK2 and GSK3β (glycogen synthase kinase 3β) inhibition is established by kinase selectivity screening. LY294002 is tested against the Upstate panel of kinases in 10 μM ATP. |
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Cell Assay: [2]
| Cell lines | Colon cancer cell lines DLD-1, LoVo, HCT15, and Colo205 |
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| Concentrations | 0–50 μM |
| Incubation Time | 0–48 hours |
| Method | 1.0×105 cells (100 μL volume/well) are inoculated into 96-well microtiter plates. LY294002 is added to triplicate wells and cultured at 37oC for 0–48 hours. After treatment, 10 μL of Premix WST-1 are added to each microculture well, and the plates are incubated for 60 minutes at 37oC, after which absorbance at 450 nm is measured with a microplate reader. |
Animal Study: [3]
| Animal Models | Two groups of athymic nude mice (5–7 weeks) are inoculated i.p. with OVCAR-3 cells |
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| Formulation | Dissolved in DMSO plus 0.25 ml of PBS |
| Dosages | 0–100 mg/kg |
| Administration | Administered via i.p. |
References
Chemical Information
| Molecular Weight (MW) | 307.34 |
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| Formula | C19H17NO3 |
| CAS No. | 154447-36-6 |
| Synonyms | N/A |
Solubility (25°C) * <1 mg/ml means slightly soluble or insoluble
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| Storage | 2 years -20°CPowder |
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| 6 months-80°Cin DMSO | |
| Chemical Name | 2-morpholino-8-phenyl-4H-chromen-4-one |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
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| Mass(mg) | 0.30734 | 3.0734 | 6.1468 | 9.2202 |
Customer Reviews (8)
 Click to enlarge | Rating | |
| Source | Biochim Biophys Acta, 2012, 1823(5), 987-96. LY294002 purchased from Selleck | |
| Method | Immunofluorescence | |
| Cell Lines | HC11 cells | |
| Concentrations | 50 μM | |
| Incubation Time | 1 h | |
| Results | whole ADRP levels, estimated by Western blot , decreased only in the presence of MK -2206 and LY294002. In most cases, ADRP decorated the surface of small lipid droplets and appeared as little patches on large cytoplasmic lipid droplets. With the exception of SP600125, which induced a strong ADRP coating of almost all cytoplasmic lipid droplets (although this inhibitor did not increase ADRP synthesis), variation in the distribution of ADRP at the surface of lipid droplet was difficult to estimate, notably because the signal was faint and uneven. |
Product Citations (22)
Dynamic expression profiling of Type I and Type III Interferon-stimulated hepatocytes reveals a stable hierarchy of gene expression. [Bolen CR, et al. Hepatology 2013;10.1002/hep.26657]
PubMed: 23929627
Phosphoinositide 3 kinase inhibition restores neutrophil accuracy in the elderly: towards targeted treatments for immunesenescence. [Sapey E, et al. Blood 2014;123(2):239-48]
PubMed: 24191150
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. [Chang KY, et al. Clin Cancer Res 2011;17(22):7116-26]
