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

C₂₃H₃₁N₃O₃S

429.58

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.

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

Toxicity: Standard Handling (A)

Supplied as a trifluoroacetate salt.

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

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.

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

100

≥90% (HPLC)

solid (Glassy)

Calbiochem^®

OK to freeze

DMSO: 10 mg/mL

ambient

−20℃

250 μg in Plastic ampoule
Packaged under inert gas

10 - Combustible liquids

WGK 3