GGTI 298 TFA salt

Catalog No.S7466

For research use only.

GGTI 298 is a geranylgeranyltransferase I inhibitor with ability to arrest human tumor cells in the G1 phase of the cell cycle and induce apoptosis.

GGTI 298 TFA salt Chemical Structure

CAS No. 1217457-86-7

Selleck's GGTI 298 TFA salt has been cited by 6 Publications

Purity & Quality Control

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Biological Activity

Description GGTI 298 is a geranylgeranyltransferase I inhibitor with ability to arrest human tumor cells in the G1 phase of the cell cycle and induce apoptosis.
Targets
GGTase I [2]
In vitro

The geranylgeranyltransferase I inhibitor GGTI-298 has been shown to arrest human tumor cells in the G1 phase of the cell cycle and induce apoptosis. Treatment of the human lung carcinoma cell line Calu-1 with GGTI-298 results in inhibition of the phosphorylation of retinoblastoma protein, a critical step for G1/S transition. The kinase activities of two G1/S cyclin-dependent kinases, CDK2 and CDK4, are inhibited in Calu-1 cells treated with GGTI-298. GGTI-298 has little effect on the expression levels of CDK2, CDK4, CDK6, cyclins D1 and E, but decreases the levels of cyclin A. GGTI-298 increases the levels of the cyclin-dependent kinase inhibitors p21 and p15 and had little effect on those of p27 and p16. GGTI-298 promotes binding of p21 and p27 to CDK2 while decreasing their binding to CDK6. Its treatment results in an increased binding of p15 to CDK4, which is paralleled with decreased binding to p27. Pretreatment of fibroblasts with GGTI-298, blocks PDGF- and epidermal growth factor-dependent tyrosine phosphorylation of their corresponding tyrosine kinase receptors. GGTI-298 has antiproliferative effects on fibroblasts, epithelial, and smooth muscle cells, and this cell growth inhibition appears to be mediated through a G1 phase arrest[1].

Assay
Methods Test Index PMID
Western blot p-IκB-α / IκB-α 22069517
Growth inhibition assay Cell viability 22069517
Immunofluorescence YAP 25745361
In vivo GGTI-298 inhibits tumor growth in nude mice[1].

Protocol (from reference)

Cell Research:[1]
  • Cell lines: human lung carcinoma cell line Calu-1
  • Concentrations: 15 μM
  • Incubation Time: 48 h
  • Method: Cells were treated with GGTI-298 (15 μM) for 48 h, harvested, and lysed in HEPES lysis buffer. Proteins were then resolved by 12.5% or 7% SDS-PAGE gel and immunoblotted with antibodies. The ECL blotting system was used for detection of positive antibody reactions.
Animal Research:[3]
  • Animal Models: Nude mice
  • Dosages: 1.16 mg/kg
  • Administration: s.c.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 593.66
Formula

C27H33N3O3S.C2HF3O2

CAS No. 1217457-86-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)CC(C(=O)OC)NC(=O)C1=C(C=C(C=C1)NCC(CS)N)C2=CC=CC3=CC=CC=C32.C(=O)(C(F)(F)F)O

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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