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GGTI 2418 sodium

Chemical Structure : GGTI 2418 sodium

CAS No.: 1044590-78-4

GGTI 2418 sodium (GGTI2418;PTX 100)

Catalog No.: PC-62153Not For Human Use, Lab Use Only.

GGTI 2418 sodium (PTX 100) is a highly potent, competitive, and selective peptidomimetic inhibitor of geranylgeranyltransferase I (GGTI) with IC50 of 9.5 nM, displays 5,600-fold selectivity over FTase.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

GGTI 2418 sodium (PTX 100) is a highly potent, competitive, and selective peptidomimetic inhibitor of geranylgeranyltransferase I (GGTI) with IC50 of 9.5 nM, displays 5,600-fold selectivity over FTase; demonstrates competitive inhibition of GGTase I against the H-Ras-CVLL protein with a Ki of 4.4 nM; suppresses the growth of human breast tumors in nude mouse xenografts; increases p27(Kip1) and induces significant regression of breast tumors.

Physicochemical Properties

M.Wt 463.514
Formula C23H30N5NaO4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

((S)-2-benzyl-4-((4-methyl-1H-imidazol-5-yl)methyl)-3-oxopiperazine-1-carbonyl)-L-leucine, sodium salt

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.

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