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Empirische Formel (Hill-System):
C18H24N2OS
CAS-Nummer:
Molekulargewicht:
316.46
UNSPSC Code:
12352200
MDL number:
Quality Segment
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
orange-yellow
solubility
DMSO: 100 mg/mL, acetic acid: soluble, methanol: soluble
shipped in
ambient
storage temp.
−20°C
InChI
1S/C18H24N2OS/c1-17(2,3)13-8-11(7-12(10-19)16(20)22)9-14(15(13)21)18(4,5)6/h7-9,22H,20H2,1-6H3/b16-12+
InChI key
LCUMYVYIHXYBIA-FOWTUZBSSA-N
General description
A cell-permeable, reversible, and substrate competitive inhibitor of nerve growth factor (NGF)-dependent p140c-trk tyrosine phosphorylation (EC50 = 10 µM) as well as NGF-induced phospholipase C-γ1 phosphorylation. Also blocks NGF-induced neurite outgrowth in PC12 cells. Does not affect the tyrosine phosphorylation of epidermal growth factor receptor or platelet-derived growth factor receptor. Inhibits insulin secretion in a dose-dependent manner.
A cell-permeable, reversible, and substrate competitive inhibitor of nerve growth factor (NGF)-dependent pp140c-trk tyrosine phosphorylation (EC50 = 10 µM), as well as NGF-induced phospholipase C-γ1 phosphorylation. Also shown to inhibit HER2 (IC50 = 1 µM). Does not affect the tyrosine phosphorylation of epidermal growth factor receptor or platelet-derived growth factor receptor. Also inhibits insulin secretion in a dose-dependent manner.
Biochem/physiol Actions
Primary Target
(NGF)-dependent p140c-trk tyrosine phosphorylation
(NGF)-dependent p140c-trk tyrosine phosphorylation
Product does not compete with ATP.
Reversible: yes
Cell permeable: yes
EC50 = 10 µM inhibiting nerve growth factor (NGF)-dependent p140c-trk tyrosine phosphorylation
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
From Catalog:
Solubility- removed acetic acid, MeOH
From Catalog:
Solubility- removed acetic acid, MeOH
Other Notes
Konrad, R.J., et al. 1996. J. Biol. Chem. 271, 24179.
Levitzki, A. and Gazit, A. 1995. Science. 267, 1782.
Ohmichi, M., et al. 1993. Biochemistry32, 4650.
Levitzki, A. and Gazit, A. 1995. Science. 267, 1782.
Ohmichi, M., et al. 1993. Biochemistry32, 4650.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Lagerklasse
10-13 - German Storage Class 10 to 13
Analysenzertifikate (COA)
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Jun Wang et al.
Current chemical genomics, 1, 27-33 (2008-01-01)
Trk receptor tyrosine kinases are required for signal transduction initiated by neurotrophins leading to cell proliferation, differentiation, survival and death. Alterations in Trk kinase activity have been linked to various diseases. To address the need for cell-based assays for screening