345878

GGTI-286

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

• Sinônimo(s): GGTI-286, N-4-[2(R)-Amino-3-mercaptopropyl]amino-2-phenylbenzoyl-(L)-leucine methyl ester, TFA
• Fórmula empírica (Notação de Hill): C₂₃H₃₁N₃O₃S
• Número CAS: 171744-11-9
• Peso molecular: 429.58
• Número MDL: MFCD28899665
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥90% (HPLC)
• Formulário: solid (Glassy)
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze
• solubilidade: DMSO: 10 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: −20°C
• cadeia de caracteres 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
• chave InChI: IENQPUVVSDIXCT-UTKZUKDTSA-N

Descrição

Descrição geral

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.

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
Geranylgeranyltransferase (GGTase)

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 2 µM against GGTase

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

forma física

Supplied as a trifluoroacetate salt.

Reconstituição

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

Outras notas

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.

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 10 - Combustible liquids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable