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GGTI298 Trifluoroacetate

Catalog No. T6844 CAS 1217457-86-7

Synonyms: GGTI 298 TFA salt, GGTI 298

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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GGTI298 Trifluoroacetate, CAS 1217457-86-7

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Purity: 98%

Biological Description

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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&IC50	Rap1A:3 μM, Ha-Ras:>20 μM.
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].
In vivo	GGTI-298 inhibits tumor growth in nude mice[1].
Cell Research	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)

Synonyms	GGTI 298 TFA salt, GGTI 298
Molecular Weight	593.66
Formula	C27H33N3O3S·C2HF3O2
CAS No.	1217457-86-7

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 14.8 mg/mL (25 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Sun J, et al. J Biol Chem. 1999, 274(11):6930-4. 2. Stark WW Jr, et al. Am J Physiol. 1998, 275(1 Pt 1):L55-63. 3. Lau CP, et al. Connect Tissue Res. 2015, 56(6):493-503. 4. Zhang Yajuan, et al. Macrophage-Associated PGK1 Phosphorylation Promotes Aerobic Glycolysis and Tumorigenesis[J]. Molecular cell. 2018 Jul 19;71(2):201-215.e7.

Citations

1. Zhang Y, Yu G, Chu H, et al. Macrophage-Associated PGK1 Phosphorylation Promotes Aerobic Glycolysis and Tumorigenesis. Molecular Cell. 2018, 71(2): 201-215. e7

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Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

GGTI298 Trifluoroacetate 1217457-86-7 Apoptosis GPCR/G Protein MAPK Metabolism Transferase Ras GGTI-298 Trifluoroacetate GGTI 298 TFA salt GGTI-298 inhibit GGTI298 Inhibitor GGTI 298 inhibitor

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