GGTI-286-CAS 171744-11-9-Calbiochem

产品说明

一般描述

A potent, cell-permeable, and selective GGTase-I inhibitor. This methyl ester derivative of GGTI-287 (Cat. No. 345880) is 25-fold more potent (IC₅₀ = 2 µM versus 50 µM) than FTI-277 (Cat. No. 344555) inhibiting the processing of the geranylgeranylated protein Rap1A. Selectively antagonizes oncogenic K-Ras4B (IC₅₀ = 2 µM). GGTI-286 has also been shown to have a significant antiproliferative effect in human malignant glioma cells.
A potent, cell-permeable, and selective inhibitor of GGTase I. This methyl ester derivative of GGTI-287 (Cat. No. 345880) is about 25-fold more potent (IC₅₀ = 2 µM vs. 50 µM) than FTI-277 (Cat. No. 344555) in inhibiting the processing of the geranylgeranylated protein Rap1A. Selectively antagonizes oncogenic K-Ras4B (IC₅₀ = 2 µM). GGTI-286 has also been shown to have a significant antiproliferative effect in human malignant glioma cells.

包装

250 μg in Plastic ampoule
Packaged under inert gas

生化/生理作用

Target IC₅₀: 2 µM against GGTase
Product does not compete with ATP.
Cell permeable: yes
Primary Target
Geranylgeranyltransferase (GGTase)
Reversible: no

警告

Toxicity: Standard Handling (A)

外形

Supplied as a trifluoroacetate salt.

重悬

Following reconstitution aliquot and freeze (-70°C). Stock solutions are stable for up to 1 week at -70°C.

其他说明

Bredel, M., et al. 1998. Neurosurgery 43, 124.
Qian, Y., et al. 1998. Bioorg. Med. Chem.6, 293.
Lerner, E.C., et al. 1997. Oncogene 15, 1283.
Lerner, E.C., et al. 1995. J. Biol. Chem. 270, 26770.

法律信息

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

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