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AG 879 - CAS 148741-30-4 - Calbiochem

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.

Synonym(s):

AG 879 - CAS 148741-30-4 - Calbiochem, α-Cyano-(3,5-di- t-butyl-4-hydroxy)thiocinnamide

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About This Item

Empirical Formula (Hill Notation):
C18H24N2OS
CAS Number:
148741-30-4
Molecular Weight:
316.46
MDL number:
MFCD00236450
UNSPSC Code:
12352200

Quality Level

100

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

Cell permeable: yes
EC50 = 10 µM inhibiting nerve growth factor (NGF)-dependent p140c-trk tyrosine phosphorylation
Primary Target
(NGF)-dependent p140c-trk tyrosine phosphorylation
Product does not compete with ATP.
Reversible: yes

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

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.

Legal Information

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

Storage Class

10-13 - German Storage Class 10 to 13

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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

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