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GGTI-286 

Cat. No. M28832

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GGTI-286  Structure

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Quality Control & Documentation
Biological Activity

GGTI-286, a potent and cell-permeable GGTase I inhibitor, is 25-fold more potent (IC50=2 μM) than the corresponding methyl ester of FTI-276. GGTI-286 selectively inhibits geranylgeranylation of Rap1A over farnesylation of H-Ras in NIH3T3 cells (IC50s=2 and >30 μM, respectively). GGTI-286 also potently inhibits oncogenic K-Ras4B stimulation with an IC50 of 1 μM.

Chemical Information
Molecular Weight 429.58
Formula C23H31N3O3S
CAS Number 171744-11-9
Solubility (25°C) DMSO 50 mg/mL (ultrasonic)
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
References

[1] Hiroki Iida, et al. PLoS One. Tramadol regulates the activation of human platelets via Rac but not Rho/Rho-kinase

[2] Atsushi Kimura, et al. Sci Rep. Nuclear β-catenin translocation plays a key role in osteoblast differentiation of giant cell tumor of bone

[3] Naoyuki Nishiya, et al. Chem Biol. A zebrafish chemical suppressor screening identifies small molecule inhibitors of the Wnt/β-catenin pathway

[4] M Bredel, et al. Neurosurgery. Inhibition of Ras and related G-proteins as a therapeutic strategy for blocking malignant glioma growth

[5] E C Lerner, et al. J Biol Chem. Disruption of oncogenic K-Ras4B processing and signaling by a potent geranylgeranyltransferase I inhibitor

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  Catalog
Abmole Inhibitor Catalog




Keywords: GGTI-286  supplier, Ras, inhibitors, activators

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