GGTI-286
GGTI-286 Basic information
- Product Name:
- GGTI-286
- Synonyms:
-
- GGTI-286
- N-4-[2(R)-AMINO-3-MERCAPTOPROPYL]AMINO-2-PHENYLBENZOYL-(L)-LEUCINE METHYL ESTER, TFA
- GGTI-286 (GGTI286)
- L-Leucine, N-[[5-[[(2R)-2-amino-3-mercaptopropyl]amino][1,1'-biphenyl]-2-yl]carbonyl]-, methyl ester
- CAS:
- 171744-11-9
- MF:
- C23H31N3O3S
- MW:
- 429.58
- Mol File:
- Mol File
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GGTI-286 Chemical Properties
- Boiling point:
- 626.9±55.0 °C(Predicted)
- Density
- 1.164±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- pka
- 9.81±0.10(Predicted)
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GGTI-286 Usage And Synthesis
Biological Activity
GGTI-286, a potent and cell-permeable GGTase I inhibitor, is 25-fold more potent (IC50=2 μM) than the corresponding methyl ester of FTI-276 . GGTI-286 selectively inhibits geranylgeranylation of Rap1A over farnesylation of H-Ras in NIH3T3 cells (IC50s =2 and >30 μM, respectively). GGTI-286 also potently inhibits oncogenic K-Ras4B stimulation with an IC50 of 1 μM[1].
References
[1]. E C Lerner, et al. Disruption of oncogenic K-Ras4B processing and signaling by a potent geranylgeranyltransferase I inhibitor. J Biol Chem. 1995 Nov 10;270(45):26770-3. [2]. Naoyuki Nishiya, et al. A zebrafish chemical suppressor screening identifies small molecule inhibitors of the Wnt/β-catenin pathway. Chem Biol. 2014 Apr 24;21(4):530-540.