GGTI-286 (TFA)

• UNSPSC Description:

  GGTI-286 TFA, 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 TFA selectively inhibits geranylgeranylation of Rap1A over farnesylation of H-Ras in NIH3T3 cells (IC50s=2 and >30 μM, respectively). GGTI-286 TFA also potently inhibits oncogenic K-Ras4B stimulation with an IC50 of 1 μM[1][2].

• Target Antigen:

  Others

• Type:

  Reference compound

• Related Pathways:

  Others

• Field of Research:

  Cancer

• Assay Protocol:

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

• Purity:

  92.45

• Solubility:

  10 mM in DMSO

• Smiles:

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

• Molecular Weight:

  543.60

• 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  4°C (Powder, sealed storage, away from moisture)

• Clinical Information:

  No Development Reported