GGTI 2417

Names

[ Name ]:
GGTI 2417

[Synonym ]:
L-Leucine, N-[[(2S)-4-[(5-methyl-1H-imidazol-4-yl)methyl]-3-oxo-2-(phenylmethyl)-1-piperazinyl]carbonyl]-, methyl ester
MFCD25976817
Methyl N-({(2S)-2-benzyl-4-[(5-methyl-1H-imidazol-4-yl)methyl]-3-oxo-1-piperazinyl}carbonyl)-L-leucinate

Biological Activity

[Description]:

GGTI 2417 is the methyl ester prodrug of GGTI-2418, a highly potent, competitive, and selective inhibitor of GGTase I; exhibits potent inhibitory activity against Rap1 geranylgeranylation with IC50 of 400 nM; increases p27 protein levels and induces accumulation in the G0/G1 phase as well as apoptotic cell death in breast cancer cells, and prevents the degradation of nuclear p27.

[References]

References 1. Kuchay S, et al. Nature. 2017 Jun 22;546(7659):554-558. 2. Kazi A, et al. Mol Cell Biol. 2009 Apr;29(8):2254-63. 3. Falsetti SC, et al. Mol Cell Biol. 2007 Nov;27(22):8003-14. View Related Products by Target Other Targets

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
755.3±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₄H₃₃N₅O₄

[ Molecular Weight ]:
455.550

[ Flash Point ]:
410.6±32.9 °C

[ Exact Mass ]:
455.253265

[ LogP ]:
2.61

[ Vapour Pressure ]:
0.0±2.5 mmHg at 25°C

[ Index of Refraction ]:
1.578

Related Compounds

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