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Merck

440202

LY 294002

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

동의어(들):

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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크기 선택

제품정보 (DICE 배송 시 비용 별도)

실험식(Hill 표기법):
C19H17NO3
CAS 번호:
154447-36-6
Molecular Weight:
307.34
MDL number:
MFCD00270881
UNSPSC Code:
12352200
NACRES:
NA.77

주요 문서

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제품 이름

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

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관련 카테고리

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).

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

Preparation Note

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

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.


Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

저장 등급

11 - Combustible Solids

wgk

WGK 2

flash_point_f

487.4 °F

flash_point_c

253.0 °C

시험 성적서(COA)

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관련 콘텐츠

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.

An Introduction to Inhibitors and Their Biological Applications - 1st Edition

An Introduction to Inhibitors and Their Biological Applications

JAK/STAT Signaling Research Focus

The Janus kinase (JAK)/signal transducers and activators of transcription (STAT) signaling pathway plays an important role in cell proliferation, cell differentiation, cell migration, and cell death. It is the principal signaling mechanism for a variety of cytokines and growth factors. Constitutive activation or dysregulation of JAK/STAT signaling can result in inflammatory disease, erythrocytosis, gigantism, and leukemia.

Bulk Product Guide
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국제 무역 품목 번호

SKUGTIN
440202-5MGCN07790788050290
440202-25MGCN04055977186673
440202-10MGCN04055977186666

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