345878

GGTI-286

A potent, cell-permeable, and selective inhibitor of GGTase I.

• Synonim(y): GGTI-286, N-4-[2(R)-Amino-3-mercaptopropyl]amino-2-phenylbenzoyl-(L)-leucine methyl ester, TFA
• Wzór empiryczny (zapis Hilla): C₂₃H₃₁N₃O₃S
• Numer CAS: 171744-11-9
• Masa cząsteczkowa: 429.58
• Numer MDL: MFCD28899665
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Poziom jakości: 100
• Próba: ≥90% (HPLC)
• Formularz: solid (Glassy)
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze
• rozpuszczalność: DMSO: 10 mg/mL
• Warunki transportu: ambient
• temp. przechowywania: −20°C
• ciąg SMILES: SC[C@H](N)CNc1cc(c(cc1)C(=O)N[C@@H](CC(C)C)C(=O)OC)c2ccccc2
• 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
• Klucz InChI: IENQPUVVSDIXCT-UTKZUKDTSA-N

Opis

Opis ogólny

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.

Działania biochem./fizjol.

Cell permeable: yes

Primary Target
Geranylgeranyltransferase (GGTase)

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 2 µM against GGTase

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Postać fizyczna

Supplied as a trifluoroacetate salt.

Rekonstytucja

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

Inne uwagi

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.

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 10 - Combustible liquids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable