GGTI298 Trifluoroacetate

SKU: orb1685545

Description

GGTI298 Trifluoroacetate is a selective geranylgeranyltransferase I inhibitor. It blocks the cell cycle in G1 phase and promotes apoptosis in tumor cells, making it a useful tool for studying cancer mechanisms and potential therapies in both cellular and biochemical assays.

Research Area

Cell Biology, Metabolism Research, Pharmacology & Drug Discovery, Signal Transduction

Images & Validation

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Key Properties

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CAS Number	1217457-86-7
MW	593.66
Purity	>99.99% (May vary between batches)
Formula	C₂₇H₃₃N₃O₃S·C₂HF₃O₂
SMILES	OC(=O)C(F)(F)F.COC(=O)[C@H](CC(C)C)NC(=O)c1ccc(NC[C@@H](N)CS)cc1-c1cccc2ccccc12
Target	Ras,Apoptosis,Transferase
Solubility	10% DMSO+90% Corn Oil:1 mg/mL (1.68 mM);DMSO:14.8 mg/mL (24.93 mM)

Bioactivity

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Target IC50	Ha-Ras:>20 μM.\|Rap1A:3 μM
In Vivo	GGTI-298 inhibits tumor growth in nude mice.
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. Read more...
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) Read more...

Storage & Handling

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Storage	store at low temperature,keep away from moisture \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Apoptosis, GGTase I, GGTI 298 TFA, GGTI 298 TFA salt, GGTI 298 Trifluoroacetate, GGTI298, GGTI-298, GGTI298 Trifluoroacetate, GGTI-298 Trifluoroacetate, Ras

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Compound Identifiers

PubChem CID

16078971 ↗

Key Properties

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No computed properties available.

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