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Merck
CN

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:
171744-11-9
Molecular Weight:
429.58
MDL number:
MFCD28899665
UNSPSC Code:
12352200
NACRES:
NA.77

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Product Name

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

100

Related Categories

Biochem/physiol Actions

Cell permeable: yes
Primary Target
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.

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

Storage Class

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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