| Identification | Back Directory | [Name]
GGTI-286 | [CAS]
171744-11-9 | [Synonyms]
GGTI-286
GGTI-286
(GGTI286)
N-4-[2(R)-AMINO-3-MERCAPTOPROPYL]AMINO-2-PHENYLBENZOYL-(L)-LEUCINE METHYL ESTER, TFA
L-Leucine, N-[[5-[[(2R)-2-amino-3-mercaptopropyl]amino][1,1'-biphenyl]-2-yl]carbonyl]-, methyl ester | [Molecular Formula]
C23H31N3O3S | [MDL Number]
MFCD09037530 | [MOL File]
171744-11-9.mol | [Molecular Weight]
429.58 |
| Chemical Properties | Back Directory | [Boiling point ]
626.9±55.0 °C(Predicted) | [density ]
1.164±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 20mg/mL, clear | [form ]
solid (Glassy) | [pka]
9.81±0.10(Predicted) | [color ]
white to light brown |
| Hazard Information | Back Directory | [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]. | [storage]
Store at -20°C | [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. |
|
|