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Merck

440202

LY 294002

≥98% (HPLC), solid, PI3K inhibitor, Calbiochem®

別名:

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:
154447-36-6
分子量:
307.34
MDL number:
MFCD00270881
UNSPSC Code:
12352200
NACRES:
NA.77

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製品名

LY 294002, LY294002, CAS 154447-36-6, is a cell-permeable, potent, reversible, and specific inhibitor of PI 3-kinase ((IC50 = 1.4 µM). Acts on the ATP-binding site.

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

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

off-white

solubility

DMSO: 20 mg/mL
ethanol: soluble

shipped in

ambient

storage temp.

−20°C

Quality Level

100

Preparation Note

Slight warming may be required to achieve complete solubilization.
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Dittman, A., et al. 2013. ACS Chem. Biol.9, 495.
Bechard, M., and Dalton. S. 2009. Mol. Cell. Biol.29, 2092.
Lianguzova, M.S. et al. 2007. Cell Biol. Int.31, 330.
Baumann, P., and West, S.C. 1998. Proc. Natl. Acad. Sci. USA 95, 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.


Biochem/physiol Actions

Cell permeable: yes
Primary Target
Phosphatidylinositol 3-kinase
Product competes with ATP.
Reversible: yes
Target IC50: 1.4 µM against phosphatidylinositol 3-kinase

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell-permeable, potent, reversible and specific phosphatidylinositol 3-kinase inhibitor (IC50 = 1.4 µM) that acts on the ATP-binding site of the enzyme. Also inhibits nonhomologous DNA end-joining (NHEJ) activity of the 460 kDa phosphatidylinositol 3-like kinase DNA-PKcs, which is the catalytic subunit of DNA-activated protein kinase. Does not affect the activities of EGF receptor kinase, MAP kinase, PKC, Pl 4-kinase, S6 kinase, and c-Src even at 50 µM. Promotes the nuclear accumulation of active GSK-3b. Reported to suppress the proliferation of murine embryonic stem cells. Blocks the proliferation of cultured rabbit aortic smooth muscle cells without inducing apoptosis. Shown to bind to the same site as I-BET (Cat. No. 40101050 ~ 10 µM). A 10 mM (1 mg/325 µl) solution of LY 294002 (Cat. No. 440204) in DMSO is also available.
A cell-permeable, potent, reversible, and specific phosphatidylinositol 3-kinase (PI 3-kinase) inhibitor that acts on the ATP-binding site of the enzyme (IC50 = 1.4 µM). Also inhibits nonhomologous DNA end-joining (NHED) in the 460 kDa phosphatidylinositol 3-like kinase DNA-PKcs, which is the catalytic subunit of DNA-activated protein kinase. Does not affect the activity of EGF receptor kinase, MAP kinase, PKC, PI 4-kinase, S6 kinase, and c-src at 50 µM. Promotes the nuclear accumulation of active GSK-3b. Reported to suppress the proliferation of murine embryonic stem cells. Blocks the proliferation of cultured rabbit aortic smooth muscle cells without inducing apoptosis. Reported to inhibit histamine secretion in RBL-2H3 cells (IC50 = 5 µM).

保管分類

11 - Combustible Solids

wgk

WGK 2

flash_point_f

487.4 °F

flash_point_c

253.0 °C

試験成績書（COA）

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S E Mikkelsen et al.
Journal of neurochemistry, 79(4), 767-776 (2001-11-28)
Several members of the S100 family of Ca(2+) binding proteins are at present known to be secreted and to have extracellular activities. We have investigated the neurite inducing potential of extracellularly added S100A12. Human recombinant S100A12 was found to dramatically
Shu Qi et al.
Cancer letters, 483, 98-113 (2020-03-29)
Liver metastases remain a major cause of death from gastrointestinal tract cancers and other malignancies, such as breast and lung carcinomas. Understanding the underlying biology is essential for the design of effective therapies. We previously identified the chemokine CCL7 and
Kelly H Forest et al.
Frontiers in molecular neuroscience, 14, 576038-576038 (2021-04-30)
Alzheimer's disease (AD) is the most common cause of dementia in the aging population. Evidence implicates elevated soluble oligomeric Aβ as one of the primary triggers during the prodromic phase leading to AD, effected largely via hyperphosphorylation of the microtubule-associated
Jyoti B Kaushal et al.
Cancers, 13(13) (2021-07-03)
Niclosamide (Nic), an FDA-approved anthelmintic drug, is reported to have anti-cancer efficacy and is being assessed in clinical trials for various solid tumors. Based on its ability to target multiple signaling pathways, in the present study, we evaluated the therapeutic
Lijun Xu et al.
The Prostate, 78(5), 353-364 (2018-01-14)
Obesity affects prostate cancer (PCa) progression, and the periprostatic adipose tissue adjacent to the prostate is considered a driving force of disease progression. Adipocytes are the main cell population in adipose tissues and their paracrine role contributes to PCa progression
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関連コンテンツ

Human Kinome & InhibitorSelect™ Libraries

Human Kinome Poster: The InhibitorSelect™ Protein Kinase Inhibitor Libraries provide broad coverage of the human kinome as shown here. The depicted human kinome dendrogram of 518 kinases are classified into five broad groups, 90 families, and 145 subfamilies. Inhibitor coverage was assigned based upon published data related to potency (IC50, EC50, Kd, etc.) for individual kinases harvested from the literature. Colored dots denote which library contains an inhibitor with demonstrated potent activity against the designated kinase and do not necessarily reflect known specificity of the inhibitor. Coverage of lipid and atypical kinases are depicted as a separate dendrogram. As shown, Calbiochem® Protein Kinase Inhibitor Libraries cover all major kinase families including TK, CMGC, CAMK, AGC, CK1, STE, TKL, as well as Lipid or Atypical kinase families.

Reprogramming Cell Fate and Function Novel Strategies for iPSC Generation, Characterization, and Differentiation
An Introduction to Inhibitors and Their Biological Applications - 1st Edition

An Introduction to Inhibitors and Their Biological Applications

Bulk Product Guide

グローバルトレードアイテム番号

カタログ番号GTIN
440202-25MGCN04055977186673
440202-5MGCN07790788050290
440202-10MGCN04055977186666

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