Inhibitor SourceBook™ Second Edition

Other Inhibitors of Biological Interest
Inhibitors of Farnesyltrasferace (FTase), Geranylgeranyltransferase (GGTase), and Methyltransferase, continued
Product Cat. No. Comments Size Price
GGTI-287 345880 {N-4-[2(R)-Amino-3-mercaptopropyl]amino-2-phenylbenzoyl-(L)leucine,TFA}
A highly potent and selective GGTase inhibitor in vitro (IC 50 = 5 nM).
Inhibits FTase only at higher concentrations (IC 50 = 25 nM).
GGTI-297 345882 {N-4-[2(R)-Amino-3-mercaptopropyl]amino-2-naphthylbenzoyl-(L)leucine,
TFA}
A potent and selective GGTase I Inhibitor (IC 50 = 50 nM) relative to
FTase (IC 50 = 200 nM).
GGTI-298 345883 {N-4-[2(R)-Amino-3-mercaptopropyl]amino-2-naphthylbenzoyl-(L)-
Leucine methyl ester, TFA}
A cell-permeable prodrug form of GGTase I inhibitor, GGTI-297
(Cat. No. 345882). Inhibits the processing of Rap A (IC 50 = 3 mM)
but has no effect on the processing of H-Ras even at higher
concentrations ( 5 mM).
GGTI-2 33 345884 {4-[[N-(Imidazol-4-yl)methyleneamino]-2-(1-naphthyl)benzoyl]leucine}
A potent and selective non-thiol inhibitor of GGTase I (IC 50 = 38 nM)
with a 40-fold selectivity over FTase (IC 50 = 5.4 mM).
GGTI-2 47 345885 {4-[[N-(Imidazol-4-yl)methyleneamino]-2-(1naphthyl)benzoyl]leucine
methyl ester}
Gliotoxin, Gladiocladium
fimbriatum
The methyl ester derivative of GGTI-2 33 (Cat No. 345884).
Selectively inhibits GGTase I over FTase in whole cells. Blocks the
geranylgeranylation of Rap A with an IC value over 60-fold lower
50
than that required to disrupt the farnesylation of H-Ras
(IC = 500 nM for Rap A versus IC > 30 mM for H-Ras).
50 50
371715 {2,3,5a,6-Tetrahydro-6-hydroxy-3(hyroxymethyl)-2-methyl-10H-
3a,10a-epidithio-pyrazinol[1,2a]indole-1,4-dione}
An immunosuppressive secondary metabolite produced by several
pathogenic fungi that specifically inhibits NF-kB activation in B and
T cells at nanomolar concentrations.
a-Hydroxyfarnesylphosphonic Acid 390601 (HFPA)
A potent and selective competitive inhibitor of farnesyl-protein
transferase (IC = 30 nM). At higher concentrations, it inhibits
50
GGTase I (IC = 35.8 mM) and II (IC = 67 mM). Useful for inhibition
50 50
of Ras processing in vivo and in vitro.
L-744,832 422720 {(2S)-2-[[(2S)-2-[(2S,3S)-2-[(2R)-2-Amino-3mercaptopropyl]amino]-3-methylpentyl]oxy]-1-oxo-3phenylpropyl]amino]-4-(methylsulfonyl)-butanoic
Acid 1-Methylethyl
Ester; L-744,382}
A potent and selective thiol-containing peptidomimetic
farnesyltransferase (FTase) inhibitor with antitumor activities.
Rapidly blocks p70S6k activation and DNA synthesis, and promotes
apoptosis in transgenic mice, induces p2 expression and arrests
cells in G phase.
Manumycin A, Streptomyces
parvulus
Protein Arginine N-
Methyltransferase Inhibitor, AMI-
444170 A potent and selective inhibitor of FTase (IC = 5 mM) compared to
50
GGTase (IC = 80 mM).
50
539209 A cell-permeable, symmetrical sulfonated urea compound that acts
as a potent, specific and non-AdoMet (S-adenosyl-L-methionine,
SAM)-competitive inhibitor of protein arginine N-methyltransferases
(PRMTs; IC = 8.8 mM for PRMT and 3.03 for yeast-RMT p)
50
with minimal effect on lysine methyltransferases. Inhibits nuclear
receptor reporter gene activation in MCF-7 cells, and HIV- RT
polymerase (IC = 5 mM).
50
250 mg $ 5
250 mg $ 2
250 mg $ 5
250 mg $ 46
250 mg $ 4
mg $8
mg $ 42
5 mg $ 8
mg $77
5 mg $95
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