产品说明
一般描述
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.
包装
250 μg in Plastic ampoule
Packaged under inert gas
生化/生理作用
Target IC50: 2 µM against GGTase
Product does not compete with ATP.
Cell permeable: yes
Primary Target
Geranylgeranyltransferase (GGTase)
Reversible: no
警告
Toxicity: Standard Handling (A)
外形
Supplied as a trifluoroacetate salt.
重悬
Following reconstitution aliquot and freeze (-70°C). Stock solutions are stable for up to 1 week at -70°C.
其他说明
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.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C23H31N3O3S |
分子量 | 429.58 |
产品性质
质量水平 | 100 |
测定 | ≥90% (HPLC) |
形式 | solid (Glassy) |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze |
溶解性 | DMSO: 10 mg/mL |
运输 | ambient |
储存温度 | −20℃ |
安全信息
储存分类代码 | 10 - Combustible liquids |
WGK | WGK 3 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |