345878
GGTI-286
A potent, cell-permeable, and selective inhibitor of GGTase I.
别名:
GGTI-286, N-4-[2(R)-Amino-3-mercaptopropyl]amino-2-phenylbenzoyl-(L)-leucine methyl ester, TFA
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关于此项目
经验公式（希尔记法）:
C23H31N3O3S
化学文摘社编号:
分子量:
429.58
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
产品名称
GGTI-286, A potent, cell-permeable, and selective inhibitor of GGTase I.
InChI key
IENQPUVVSDIXCT-UTKZUKDTSA-N
InChI
1S/C23H31N3O3S/c1-15(2)11-21(23(28)29-3)26-22(27)19-10-9-18(25-13-17(24)14-30)12-20(19)16-7-5-4-6-8-16/h4-10,12,15,17,21,25,30H,11,13-14,24H2,1-3H3,(H,26,27)/t17-,21+/m1/s1
SMILES string
SC[C@H](N)CNc1cc(c(cc1)C(=O)N[C@@H](CC(C)C)C(=O)OC)c2ccccc2
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
Quality Level
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
Disclaimer
Toxicity: Standard Handling (A)
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.
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.
Packaging
Packaged under inert gas
Physical form
Supplied as a trifluoroacetate salt.
Preparation Note
Following reconstitution aliquot and freeze (-70°C). Stock solutions are stable for up to 1 week at -70°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
10 - Combustible liquids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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