440204
LY 294002
InSolution, ≥98%, 10 mM, reversible and specific inhibitor of PI 3-kinase
別名:
InSolution LY 294002, 2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one, BRD2 Inhibitor IV, BRD3 Inhibitor III, BRD4 Inhibitor IV
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この商品について
実験式（ヒル表記法）:
C19H17NO3
CAS番号:
分子量:
307.34
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
liquid
Quality level:
Storage condition:
OK to freeze, protect from light
SMILES string
N4(CCOCC4)c1[o]c2c([c](c1)=O)cccc2c3ccccc3
InChI
1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2
InChI key
CZQHHVNHHHRRDU-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
liquid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
shipped in
wet ice
storage temp.
−20°C
Quality Level
関連するカテゴリー
General description
Cell permeable: Yes
Primary Target: phosphatidylinositol 3-kinase
Product competes with ATP.
Reversible: Yes
Target IC50: 1.4 µM against phosphatidylinositol3-kinase
LY294002 is a chemical compound known for its potentinhibitory effects on a variety of proteins, particularly as a strong inhibitorof phosphoinositide 3-kinases (PI3Ks). While it is frequently utilized in research related to the PI3K/AKT signaling pathway, LY294002 is generallyregarded as a non-selective tool for investigating PI3K functions. This flavonoid derivative acts as a competitive andreversible inhibitor of the ATP binding site of PI3K, exhibiting an IC50 approximately 500-fold higher than that of wortmannin, at 1.4 μM. LY294002 doesnot inhibit several ATP-dependent enzymes, including PI4K, EGF receptor tyrosinekinase, c-src, MAP kinase, S6 kinase, diacylglycerol kinase, protein kinase A, protein kinase C, and ATPase. It acts as an antagonist of the aryl hydrocarbonreceptor (AHR), a ligand-activated transcription factor. By binding to AHR, LY294002 inhibits transcriptional activation, thereby preventing gene expression.
Primary Target: phosphatidylinositol 3-kinase
Product competes with ATP.
Reversible: Yes
Target IC50: 1.4 µM against phosphatidylinositol3-kinase
LY294002 is a chemical compound known for its potentinhibitory effects on a variety of proteins, particularly as a strong inhibitorof phosphoinositide 3-kinases (PI3Ks). While it is frequently utilized in research related to the PI3K/AKT signaling pathway, LY294002 is generallyregarded as a non-selective tool for investigating PI3K functions. This flavonoid derivative acts as a competitive andreversible inhibitor of the ATP binding site of PI3K, exhibiting an IC50 approximately 500-fold higher than that of wortmannin, at 1.4 μM. LY294002 doesnot inhibit several ATP-dependent enzymes, including PI4K, EGF receptor tyrosinekinase, c-src, MAP kinase, S6 kinase, diacylglycerol kinase, protein kinase A, protein kinase C, and ATPase. It acts as an antagonist of the aryl hydrocarbonreceptor (AHR), a ligand-activated transcription factor. By binding to AHR, LY294002 inhibits transcriptional activation, thereby preventing gene expression.
Application
LY294002 has been used as a phosphatidylinositol3-kinase (PI3K) inhibitor:
- to induce viral reactivation in a model ofherpes simplex virus type 1 (HSV-1) latency
- to investigate its effects on transforminggrowth factor (TGF)-β1-induced differentiation of cat corneal fibroblasts
- to investigate its role in the insulin-like growthfactor I (IGF-1) signaling pathway and on the phosphorylation of glycogensynthase kinase-3β (GSK-3β)
Biochem/physiol Actions
Primary Target
phosphatidylinositol 3-kinase
phosphatidylinositol 3-kinase
Product competes with ATP.
Reversible: yes
Target IC50: 1.4 µM against phosphatidylinositol 3-kinase
Cell permeable: yes
Packaging
Packaged under inert gas
Physical form
A 10 mM (1 mg/325 µl) solution of LY 294002 (Cat. No. 440202) in DMSO.
Preparation Note
Following initial thaw, aliquot and freeze (-20°C).
Other Notes
Dittman, A., et al. 2013. ACS Chem. Biol.9, 495.
Baumann, P., and West, S.C. 1998. Proc. Natl. Acad. Sci. USA95, 14066.
Cardone, M.H., et al. 1998. Science282, 1318.
Vlahos, C.J., et al. 1995. J. Immunol.154, 2413.
Yano, H., et al. 1995. Biochem. J.312, 145.
Vlahos, C.J., et al. 1994. J. Biol. Chem.269, 5241.
Selected Citations
Lee, J., et al. 2009. Cell Stem Cell5, 76.
Baumann, P., and West, S.C. 1998. Proc. Natl. Acad. Sci. USA95, 14066.
Cardone, M.H., et al. 1998. Science282, 1318.
Vlahos, C.J., et al. 1995. J. Immunol.154, 2413.
Yano, H., et al. 1995. Biochem. J.312, 145.
Vlahos, C.J., et al. 1994. J. Biol. Chem.269, 5241.
Selected Citations
Lee, J., et al. 2009. Cell Stem Cell5, 76.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Irritant (B)
保管分類
10 - Combustible liquids
wgk
WGK 1
flash_point_f
188.6 °F - (refers to pure substance)
flash_point_c
87 °C - (refers to pure substance)
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
Group 4: Flammable liquids + Type 3 petroleums + Hazardous rank III + Water insoluble liquid
fsl
440204-1MG:
jan
試験成績書（COA）
製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。
Xiaohua Wu et al.
Molecules (Basel, Switzerland), 26(13) (2021-07-03)
Astragalus membranaceus is a famous herb found among medicinal and food plants in East and Southeastern Asia. The Nrf2-ARE assay-guided separation of an extract from Jing liqueur led to the identification of a nontoxic Nrf2 activator, methylnissolin-3-O-β-d-glucopyranoside (MNG, a component
Abdelkader Essafi et al.
Methods in molecular biology (Clifton, N.J.), 462, 201-211 (2009-01-24)
This chapter describes methods for studying downstream events of the PI3K/Akt signaling cascade, focusing on the FoxO transcription factors. These approaches also represent alternative means for gauging the phosphoinositide-3 kinase/Akt activity. We describe protocols for the fractionation of cytoplasmic and
Christina L Sherry et al.
Journal of immunology (Baltimore, Md. : 1950), 178(2), 663-670 (2007-01-05)
Dysregulated inflammation is a complication of type 2 diabetes (T2D). In this study, we show that augmented LPS-induced TNF-alpha production by resident peritoneal macrophages (PerMphi) in type 2 diabetic (db/db) mice is dependent on elevated glucose and requires p38 MAPK.
Anna Bellizzi et al.
Molecular therapy. Nucleic acids, 35(3), 102282-102282 (2024-08-23)
Although our understanding of herpes simplex virus type 1 (HSV-1) biology has been considerably enhanced, developing therapeutic strategies to eliminate HSV-1 in latently infected individuals remains a public health concern. Current antiviral drugs used for the treatment of HSV-1 complications
Yasuhisa Murai et al.
iScience, 24(10), 103173-103173 (2021-10-26)
Schlafen11 (SLFN11) is referred to as interferon (IFN)-inducible. Based on cancer genomic databases, we identified human acute myeloid and lymphoblastic leukemia cells with gain-of-function mutations in the Janus kinase (JAK) family as exhibiting high SLFN11 expression. In these cells, the
グローバルトレードアイテム番号
| カタログ番号 | GTIN |
|---|---|
| 440204-1MGCN | 04055977186710 |
ライフサイエンス、有機合成、材料科学、クロマトグラフィー、分析など、あらゆる分野の研究に経験のあるメンバーがおります。.
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