LY 294002A potent blocker of PI 3-kinase/Akt signaling

LY 294002 (CAS 154447-36-6)

LY 294002 | CAS 154447-36-6 is rated 5.0 out of 5 by 1.
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Synonym: 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one
Application: A potent blocker of PI 3-kinase/Akt signaling
CAS Number: 154447-36-6
Purity: ≥98%
Molecular Weight: 307.34
Molecular Formula: C19H17NO3
* Refer to Certificate of Analysis for lot specific data (including water content).
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LY294002 is a potent inhibitor of PI 3-kinase, a protein in the phosphoinositide 3-kinase family of intercellular signal regulating enzymes. This compound is selective for PI 3-kinase p110 β (PI 3-Kβ) and PI 3-kinase p110 α (PI 3-Kα), although it will inhibit other PI 3 kinases at higher concentrations (IC50 = 310 nM and 730 nM for PI 3-Kβ and PI 3-Kα, respectively). The pathway associated with these receptors is implicated in cancer and diabetes, and LY294002 is an important tool for studying this relationship. Reports indicate that LY294002 encourages apoptosis in such cells by blocking the PI 3-kinase/Akt signaling pathway which has been strongly related to cancer survival and proliferation. LY 294002 is an inhibitor of Pim-1, PI 3-kinase p110 δ and PI 3-kinase p110 γ.


References

1. Vanhaesebroeck, B., et al. 1997. Proc. Natl. Acad. Sci. U.S.A. 94: 4330-4335. PMID: 9113989
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Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in DMSO (25 mg/ml warm), ethanol (25 mg/ml warm), chloroform, water (< 50 ug/ml) at 25° C, PBS pH 7.2 (< 50 ug/ml), DMF (~16 mg/ml ), and DMSO:PBS(1:1, pH 7.2) (~0.5 mg/ml ).
Storage :
Store at -20° C
Melting Point :
191.76° C (Predicted)
Boiling Point :
~494.6° C at 760 mmHg (Predicted)
Density :
~1.3 g/cm3 (Predicted)
Refractive Index :
n20D 1.63 (Predicted)
IC50 :
Purified PI3K: IC50 = 1.4 µM; Pim-1 kinase : IC50 = 4.0 µM; p110α: IC50 = 0.63 µM; proliferation of choroidal melanoma OCM-1 cells: IC50 = 10 µM; DNA-dependent protein kinase: IC50 = 1.5 µM (human); Serine/threonine-protein kinase PLK3: IC50 = 3 µM (human); PI3K: EC5050 = 1.5 µM (human HeLa cells)
Ki Data :
DNA-dependent protein kinase: Ki= 6 µM (human); PI3-kinase p110-alpha subunit: Ki= 6 µM (human); ATP binding site of Escherichia coli D-alanine-D-alanine ligase B: Ki= 1400 µM
pK Values :
pKb: 0.55
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
3973
MDL Number :
MFCD00270881
SMILES :
C1COCCN1C2=CC(=O)C3=C(O2)C(=CC=C3)C4=CC=CC=C4

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LY 294002  Product Citations

See how others have used LY 294002. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 93 total

PMID: # 30627006  Zhang, Q.|Chen, K.|Wu, T.|Song, H.| et al. 2019. Korean J. Physiol. Pharmacol. 23: 21-28.

PMID: # 30659232  Salahuddin, S.|Fath, EK.|Biel, N.|Ray, A.|Moss, CR.|Patel, A.|Patel, S.|Hilding, L.|Varn, M.|Ross, T.|Cramblet, WT.|Lowrey, A.|Pagano, JS.|Shackelford, J.|Bentz, GL.| et al. 2019. Sci Rep. 9: 208.

PMID: # 30891489  Jia, Y.|Miyamoto, S.|Soda, Y.|Takishima, Y.|Sagara, M.|Liao, J.|Hirose, L.|Hijikata, Y.|Miura, Y.|Hara, K.|Iwanaga, A.|Ota, Y.|Tani, K.| et al. 2019. Mol Ther Oncolytics. 12: 246-258.

PMID: # 31115571  Yu, G.|Wang, C.|Song, X.|Liu, S.|Zhang, Y.|Fan, L.|Yang, Y.|Huang, Y.|Song, J.| et al. 2019. Mol Med Rep. 20: 341-349.

PMID: # 31022663  Hsieh, MJ.|Wang, CW.|Lin, JT.|Chuang, YC.|Hsi, YT.|Lo, YS.|Lin, CC.|Chen, MK.| et al. 2019. Phytomedicine. 58: 152805.

PMID: # 30606984  Hamada, K.|Maeda, Y.|Mizutani, A.|Okada, S.| et al. 2019. Biol. Pharm. Bull. 42: 130-138.

PMID: # 30614032  Luo, Z.|Zhang, M.|Niu, X.|Wu, .|Tang, J.| et al. 2019. J. Cell. Biochem. 120: 10175-10185.

PMID: # 31063758  White, SM.|Avantaggiati, ML.|Nemazanyy, I.|Di Poto, C.|Yang, Y.|Pende, M.|Gibney, GT.|Ressom, HW.|Field, J.|Atkins, MB.|Yi, C.| et al. 2019. Dev. Cell. 49: 425-443.e9.

PMID: # 30911300  Aboalola, D.|Han, VKM.| et al. 2019. Stem Cells Int. 2019: 9245938.

PMID: # 30668359  Lin, FZ.|Wang, SC.|Hsi, YT.|Lo, YS.|Lin, CC.|Chuang, YC.|Lin, SH.|Hsieh, MJ.|Chen, MK.| et al. 2019. Phytomedicine. 54: 1-8.

Citations 1 to 10 of 93 total

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This chemical, LY 294002 (CAS 154447-36-6), ships ambient.
Answered by: Chemical Support 1
Date published: 2017-03-22
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Rated 5 out of 5 by from Selzman Selzman, et. al. (PubMed ID 12234797 ) utilized LY 294002, a specific PI3 kinase antagonist, from Santa Cruz Biotechnology to determine the significance of PI3 Kinase signaling is to MCP-1-induced VSMC proliferation. After treatment, BrdU uptake was measured. -SCBT Publication Review
Date published: 2015-06-11
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