Nucleotide Analogs - Jena Bioscience

It also inhibits the activities of myosin light chain
kinase (MLCK), PI4-Kinase and phospholipase C
(PLC) but at concentrations about 100-fold higher
than those required for PI3K inhibition.
Purity: 98%
Molecular formula: C 23 H 24 O 8
Molecular weight: 428.4 g/mol
Solubility: 25 mg/ml in DMSO, 5 mg/ml in ethanol.
Store: -20 °C
Selected references:
Arcaro A. and Wymann M.P. (1993) Wortmannin is a potent
phosphatidylinositol 3-kinase inhibitor: the role of phosphatidylinositol
3,4,5-trisphosphate in neutrophil responses. Biochem.
J. 296:297.
Wymann M.P. and Arcaro A. (1994) Platelet-derived growth factor-induced
phosphatidylinositol 3-kinase activation mediates
actin rearrangements in fi broblasts. Biochem J. 298:517.
Walker et al. (2000) Structural Determinants of Phosphoinositide
3-Kinase Inhibition by Wortmannin, LY294002, Quercetin,
Myricetin, and Staurosporine. Mol. Cell. 6:909.
Houle S. and Marceau F. (2003) Wortmannin alters the intracellular
traffi cking of the bradykinin B2 receptor: role of phosphoinositide
3-kinase and Rab5. Biochem. J. 375:151.
LY294002
2-(4-Morpholinyl)-8-phenyl-
4H-1-benzopyran-4-one
(PI3K-Inhibitor)
Cat. No. Amount Price (€)
INH-002 1 mg 35,--
Lyophilized.
O
O
LY294002 is a cell-permeable compound that acts as
a potent and selective inhibitor of phosphatidylinositol
3-kinase (PI3K). It is active with purifi ed preparations,
cytosolic fractions and suitable for use with intact
cells.
LY294002 blocks the catalytic activity of PI3-Kinase
with an IC 50 of 1.4 µM and without affection of other
kinases including PKC, PKA, MAPK, S6 kinase,
EGFR, Src, or PI4-Kinase.
For intact cells like neutrophils, a concentration of
50 µM completely abolishes the PI3K activity.
It also inhibits the activities of myosin light chain
kinase (MLCK), PI4-Kinase and phospholipase C
(PLC) but at concentrations about 100-fold higher
than those required for PI3K inhibition.
Purity: 99%
Molecular formula: C 19 H 17 NO 3
Molecular weight: 307.4 g/mol
Solubility: 25 mg/ml in DMSO, methanol or ethanol.
Store: -20 °C
Selected references:
Vlahos et al. (1994) A specifi c inhibitor of phosphatidylinositol
3-kinase, 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one
(LY294002). Biochem. J. 269:5241.
Walker et al. (2000) Structural Determinants of Phosphoinositide
3-Kinase Inhibition by Wortmannin, LY294002, Quercetin,
Myricetin, and Staurosporine. Mol. Cell. 6:909.
Vlahos et al. (1995) Investigation of neutrophil signal transduction
using a specifi c inhibitor of phosphatidylinositol 3-kinase. J.
Immunol. 154:2413.
Semba et al. (2002) The in vitro and in vivo effects of 2-(4-morpholinyl)-8-phenyl-chromone
(LY294002), a specifi c inhibitor of
phosphatidylinositol 3’-kinase, in human colon cancer cells.
Clin. Cancer Res. 8:1957.
N
O
Quercetin
2-(3,4-dihydroxyphenyl)-
3,5,7-trihydroxy-4H-1benzopyran-4-one
(Protein kinase inhibitor)
Cat. No. Amount Price (€)
INH-003 100 mg 20,--
HO
OH O
Lyophilized. Dihydrate.
O
OH
OH
OH
Synomyms: 3,3’,4’,5,7-Pentahydroxyfl avone
Quercetin is a fl avonoid with anticancer activity. It
inhibits mitochondrial ATPase, phosphodiesterase, PI3kinase
activity (IC 50 = 3.8 µM) and slightly PIP kinase
activity. It has antiproliferative effects on cancer cell
lines; reduces cancer cell growth via type II estrogen
receptors and has been reported to arrest human
leukemic T cells in late G 1 phase of the cell cycle.
It induces apoptosis in K562, Molt-4, Raji, A549 and
MCAS tumor cell lines.
Purity: 98%
Molecular formula: C 15 H 10 O 7 ·2H 2 O
Molecular weight: 338.26 g/mol
Solubility: DMSO, acetic acid, aqueous alkali.
Store: -20 °C
Selected references:
Walker et al. (2000) Structural Determinants of Phosphoinositide
3-Kinase Inhibition by Wortmannin, LY294002, Quercetin,
Myricetin, and Staurosporine. Mol. Cell. 6:909.
De et al. (2004) Comparative evaluation of cancer chemopreventive
effi cacy of alpha-tocopherol and quercetin in a murine
model. J. Exp. Clin. Cancer Res. 23:251.
Picq et al. (1982) Pentasubstituted quercetin analogues as
selective inhibitors of particulate 3’:5’-cyclic-AMP phosphodiesterase
from rat brain. J. Med. Chem. 25:1192.
Nguyen et al. (2004) The role of activated MEK-ERK pathway in
quercetin-induced growth inhibition and apoptosis in A549 lung
cancer cells. Carcinogenesis. 25:647.
Mertens-Talcott et al. (2003) Low concentrations of quercetin
and ellagic acid synergistically infl uence proliferation, cytotoxicity
and apoptosis in MOLT-4 human leukemia cells. J. Nutr.
133:2669.
Myricetin
3,5,7-trihydroxy-2-
(3,4,5-trihydroxyphenyl)-
4H-1-benzopyran-4-one
(Protein kinase inhibitor)
Cat. No. Amount Price (€)
INH-004 1 mg 18,--
Lyophilized.
HO
OH
O
O
OH
OH
OH
OH
Synomyms: 3,3’,4’,5,5’,7-Hexahydroxyfl avone,
Cannabiscetin
PI3 Kinase Family
Myricetin is a fl avonoid that differs from quercetin only
by the addition of a hydroxyl at the 5’-OH of the phenyl
moiety. It shows cytotoxic activity against several
human leukemic cell lines in vitro.
It strongly inhibits yeast α-glucosidase, glyoxalase I
in vitro, cow’s milk xanthine oxidase, and PI3-Kinase
(IC 50 = 1.8 µM).
Myricetin both modulates Na+/K+-ATPase-induced
vasodilatation acting as a functional inhibitor of Na+/
K+-ATPase activity and activates protein kinases,
including PKC, to induce contraction. These effects
appear to be related to the activation of PGH2-TXA2
receptors on vascular smooth muscle by the TXA2
released from endothelium.
Purity: 95%
Molecular formula: C15H10O8 Molecular weight: 318.24 g/mol
Solubility: DMSO
Store: -20 °C
Selected references:
Walker et al. (2000) Structural Determinants of Phosphoinositide
3-Kinase Inhibition by Wortmannin, LY294002, Quercetin,
Myricetin, and Staurosporine. Mol. Cell. 6:909.
Jimenez et al. (2002) Involvement of protein kinase C and Na+/
K+-ATPase in the contractile response induced by myricetin in
rat isolated aorta. Planta Med. 68:133.
Dimas et al. (2000) Biological activity of myricetin and
its derivatives against human leukemic cell lines in vitro.
Pharmacol Res. 42:475.
Ong K.C. and Khoo H.E. (1997) Biological effects of myricetin.
Gen. Pharmacol. 29:121.
Staurosporine
(Protein kinase inhibitor)
Streptomyces staurosporeus
Cat. No. Amount Price (€)
INH-005 50 µg 65,--
Lyophilized.
H
O
N
N
O
HN
N
CH 3
CH 3
OCH 3
Staurosporine is a potent cell permeable inhibitor of
many kinases including Protein Kinase C, Protein
Kinase A, CaM kinase, myosin light chain kinase, and
PI3K (IC 50 = 9 µM).
The biological effects of Staurosporine include cytotoxicity,
relaxation of smooth muscle, and regulation
of eNOS gene expression. It inhibits platelet aggregation
induced by collagen or ADP but has no effect on
thrombin-induced platelet aggregation. Staurosporine
induces apoptosis in human malignant glioma cell lines
and arrests normal cells at the G 1 checkpoint.
Purity: 98%
Molecular formula: C28H26N4O3 Molecular weight: 466.5 g/mol
Solubility: ethyl acetate, DMSO or DMF.
Store: -20 °C
Selected references:
Walker et al. (2000) Structural Determinants of Phosphoinositide
3-Kinase Inhibition by Wortmannin, LY294002, Quercetin,
Myricetin, and Staurosporine. Mol. Cell. 6:909.
Wan et al. (2002) PTEN augments staurosporine-induced apoptosis
in PTEN-null Ishikawa cells by downregulating PI3K/Akt
signaling pathway. Cell Death Differ. 9:414.
Lee S.K. and Stern P.H. (2000) Divergent effects of protein kinase
C (PKC) inhibitors staurosporine and bisindolylmaleimide I
(GF109203X) on bone resorption. Biochem. Pharmacol. 60:923.
Takano S. (1994) Staurosporine inhibits STA2-induced platelet
aggregation by inhibition of myosin light-chain phosphorylation
in rabbit washed platelets. Ann. N. Y. Acad. Sci. 714:315.
Matsumoto H. and Sasaki Y. (1989) Staurosporine a protein
kinase C inhibitor interferes with proliferation of arterial smooth
muscle cells. Biochem. Biophys. Res. Comm. 158:105.
Recombinant Proteins
187