GGTI-286

Modify Date: 2024-01-08 10:55:40

GGTI-286 Structure
GGTI-286 structure
Common Name GGTI-286
CAS Number 171744-11-9 Molecular Weight 429.58
Density 1.2±0.1 g/cm3 Boiling Point 626.9±55.0 °C at 760 mmHg
Molecular Formula C23H31N3O3S Melting Point N/A
MSDS N/A Flash Point 332.9±31.5 °C

 Use of GGTI-286


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 (HY-15873A). 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].

 Names

Name Methyl N-[(5-{[(2R)-2-amino-3-sulfanylpropyl]amino}-2-biphenylyl)carbonyl]-L-leucinate
Synonym More Synonyms

 GGTI-286 Biological Activity

Description 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 (HY-15873A). 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].
Related Catalog
Target

IC50: 2 μM (Geranylgeranylation of Rap1A) in NIH3T3 cells[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.

 Chemical & Physical Properties

Density 1.2±0.1 g/cm3
Boiling Point 626.9±55.0 °C at 760 mmHg
Molecular Formula C23H31N3O3S
Molecular Weight 429.58
Flash Point 332.9±31.5 °C
Exact Mass 429.208618
LogP 3.76
Vapour Pressure 0.0±1.8 mmHg at 25°C
Index of Refraction 1.588

 Safety Information

Hazard Codes Xi

 Synonyms

L-Leucine, N-[[5-[[(2R)-2-amino-3-mercaptopropyl]amino][1,1'-biphenyl]-2-yl]carbonyl]-, methyl ester
Methyl N-[(5-{[(2R)-2-amino-3-sulfanylpropyl]amino}-2-biphenylyl)carbonyl]-L-leucinate
methyl N-[(5-{[(2R)-2-amino-3-sulfanylpropyl]amino}biphenyl-2-yl)carbonyl]-L-leucinate
GGTI-286
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  • Product Name: GGTI-286
  • Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

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