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
• 经验公式（希尔记法）: C₂₃H₃₁N₃O₃S
• CAS号: 171744-11-9
• 分子量: 429.58
• 分類程式碼代碼: 12352200
• NACRES: NA.77

属性

• 品質等級: 100
• 化驗: ≥90% (HPLC)
• 形狀: solid (Glassy)
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze
• 溶解度: DMSO: 10 mg/mL
• 運輸包裝: ambient
• 儲存溫度: −20°C

说明

一般說明

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.

生化／生理作用

Cell permeable: yes

Primary Target
Geranylgeranyltransferase (GGTase)

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 2 µM against GGTase

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

外觀

Supplied as a trifluoroacetate salt.

重構

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

其他說明

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.

法律資訊

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

安全信息

• 儲存類別代碼: 10 - Combustible liquids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable