GGTI-286

• 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][2].

• 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.

• Shipping Conditions:

  Room temperature

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• CAS Number:

  171744-11-9