GGTI 298 TFA salt

Catalog No.S7466

GGTI 298 TFA salt Chemical Structure

Molecular Weight(MW): 593.66

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.

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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 ; 

PubMed: 22069517     


C8166, C91/PL, and TL-Om1 cells were treated with 10 μM GGTI-298 and whole cell extracts were prepared at 0, 8, 24, and 48 hours post-treatment. Immunoblots using antibodies to IκB, p-IκB or actin as indicated. Normalized densitometric volume is shown above each immunoblot set. 

22069517
Growth inhibition assay
Cell viability; 

PubMed: 22069517     


Control PBMCs and HTLV-1-transformed SP, C8166, C91/PL, and MT2 cells were treated for 72 hours with increasing amounts of GGTI-298 and cell viability measured as before. Error bars represent the standard error of the mean from three independent experiments performed in triplicate. For all GGTI298-treated cells p < 0.05 compared with mock-treated control, except MT2 cells treated with 2.5 and 5 μM GGTI-298.

22069517
Immunofluorescence
YAP; 

PubMed: 25745361     


Nuclear localization of YAP is inhibited by inhibition of Geranylgeranylation. MDA-MB-231 cells were treated with atorvastatin (panels d-f) or the geranylgeranyltransferase I inhibitor GGTI-298 (panels g-i) for 48 hrs. The cells were stained with anti-YAP (red) (panels a, d, and g) or DAPI (blue) (panels b, e, and h).

25745361
In vivo GGTI-298 inhibits tumor growth in nude mice[1].

Protocol

Cell Research:[1]
- Collapse
  • 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.
    (Only for Reference)
Animal Research:[3]
- Collapse
  • Animal Models: Nude mice
  • Formulation: stock in DMSO, dilute in saline
  • Dosages: 1.16 mg/kg
  • Administration: s.c.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (168.44 mM)
Ethanol 100 mg/mL (168.44 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 593.66
Formula

C27H33N3O3S.C2HF3O2

CAS No. 1217457-86-7
Storage powder
in solvent
Synonyms N/A

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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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Transferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID