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][2].

Product Specifications

CAS Number

[171744-11-9]

UNSPSC

12352005

Hazard Statement

H410

Target

Ras

Type

Reference compound

Related Pathways

GPCR/G Protein; MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/ggti-286.html

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

CC(C)C[C@@H](C(OC)=O)NC(C1=CC=C(NC[C@@H](N)CS)C=C1C2=CC=CC=C2)=O

Molecular Formula

C23H31N3O3S

Molecular Weight

429.58

Precautions

P273-P391-P501

References & Citations

[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.