Catalog No. size PriceQuantity
M7026-2 2mg solid $80
M7026-10 10mg solid $324


GGTI-298 is a potent geranylgeranyltransferase-I (GGTase-I) inhibitor with potential antitumor actrivity. GGTI-298 disrupts MAP kinase activation and G(1)-S transition in Ki-Ras-overexpressing transformed adrenocortical cells. GGTI-298 induces hypophosphorylation of retinoblastoma and partner switching of cyclin-dependent kinase inhibitors. A potential mechanism for GGTI-298 antitumor activity. GGTI-298 arrests human tumor cells in G0/G1 and induces p21(WAF1/CIP1/SDI1) in a p53-independent manner. GGTI-298 induces G0-G1 block and apoptosis whereas FTI-277 causes G2-M enrichment in A549 cells.

Product information

CAS Number: 1217457-86-7

Molecular Weight: 593.66

Formula: C29H34F3N3O5S


GGTI-298 trifluoride salt



GGTI 298


Chemical Name: methyl(4-(((R)-2-amino-3-mercaptopropyl)amino)-2-(naphthalen-1-yl)benzoyl)-L-leucinate 2,2,2-trifluoroacetate

Smiles: CC(C)C[C@@H](C(O)=O)N(C)C(=O)C1=CC=C(C=C1C1=CC=CC2=CC=CC=C21)NC[C@@H](N)CS.OC(=O)C(F)(F)F


InChi: InChI=1S/C27H33N3O3S.C2HF3O2/c1-17(2)13-25(27(32)33)30(3)26(31)23-12-11-20(29-15-19(28)16-34)14-24(23)22-10-6-8-18-7-4-5-9-21(18)22;3-2(4,5)1(6)7/h4-12,14,17,19,25,29,34H,13,15-16,28H2,1-3H3,(H,32,33);(H,6,7)/t19-,25+;/m1./s1

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

RhoA inhibitor (GGTI298 Trifluoroacetate) significantly reduces cAMP agonist-stimulated apical K+ conductance. Knockdown of DR4 abolishes NF-κB activation, leading to sensitization of DR5-dependent apoptosis induced by the combination of GGTI298 Trifluoroacetate and TRAIL. GGTI298 Trifluoroacetate/TRAIL activates NF-κB and inhibits Akt. Knockdown of DR5, prevents GGTI298/TRAIL-induced IκBα and p-Akt reduction, suggesting that DR5 mediates reduction of IκBα and p-Akt induced by GGTI298/TRAIL. In contrast, DR4 knockdown further facilitates GGTI298/TRAIL-induced p-Akt reduction.

In Vivo:

The vivo mouse ileal loop experiments show fluid accumulation is reduced in a dose-dependent manner by TRAM-34, GGTI298 Trifluoroacetate, or H1152 when inject together with cholera toxin into the loop.


  1. Allal C, Pradines A, Hamilton AD, Sebti SM, Favre G. Farnesylated RhoB prevents cell cycle arrest and actin cytoskeleton disruption caused by the geranylgeranyltransferase I inhibitor GGTI-298. Cell Cycle. 2002 Nov-Dec;1(6):430-7. PubMed PMID: 12548020.
  2. Lau CP, Wong KC, Huang L, Li G, Tsui SK, Kumta SM. A mouse model of luciferase-transfected stromal cells of giant cell tumor of bone. Connect Tissue Res. 2015 Nov;56(6):493-503. doi: 10.3109/03008207.2015.1075519. PubMed PMID: 26327464.
  3. Coxon FP, Helfrich MH, Van't Hof R, Sebti S, Ralston SH, Hamilton A, Rogers MJ. Protein geranylgeranylation is required for osteoclast formation, function, and survival: inhibition by bisphosphonates and GGTI-298. J Bone Miner Res. 2000 Aug;15(8):1467-76. PubMed PMID: 10934645.

Products are for research use only. Not for human use.

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