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GGTI-2418

Chemical Structure : GGTI-2418

CAS No.: 501010-06-6

GGTI-2418 (GGTI 2418, PTX 100)

Catalog No.: PC-62152Not For Human Use, Lab Use Only.

GGTI-2418 (GGTI 2418, 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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Biological Activity

GGTI-2418 (GGTI 2418, 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.
GGTI 2418 demonstrates competitive inhibition of GGTase I against the H-Ras-CVLL protein with a Ki of 4.4 nM.
GGTI 2418 suppresses the growth of human breast tumors in nude mouse xenografts.
GGTI 2418 increases p27(Kip1) and induces significant regression of breast tumors.

Physicochemical Properties

M.Wt 441.532
Formula C23H31N5O4
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-((S)-2-benzyl-4-((4-methyl-1H-imidazol-5-yl)methyl)-3-oxopiperazine-1-carboxamido)-4-methylpentanoic acid

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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