345878
GGTI-286
A potent, cell-permeable, and selective inhibitor of GGTase I.
Synonym(s):
GGTI-286, N-4-[2(R)-Amino-3-mercaptopropyl]amino-2-phenylbenzoyl-(L)-leucine methyl ester, TFA
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About This Item
Empirical Formula (Hill Notation):
C23H31N3O3S
CAS Number:
Molecular Weight:
429.58
UNSPSC Code:
12352200
Recommended Products
Quality Level
Assay
≥90% (HPLC)
form
solid (Glassy)
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
solubility
DMSO: 10 mg/mL
shipped in
ambient
storage temp.
−20°C
General description
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Geranylgeranyltransferase (GGTase)
Geranylgeranyltransferase (GGTase)
Product does not compete with ATP.
Reversible: no
Target IC50: 2 µM against GGTase
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Physical form
Supplied as a trifluoroacetate salt.
Reconstitution
Following reconstitution aliquot and freeze (-70°C). Stock solutions are stable for up to 1 week at -70°C.
Other Notes
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.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
10 - Combustible liquids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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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