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GGTI 2418 sodium

Names

[ CAS No. ]:
1044590-78-4

[ Name ]:
GGTI 2418 sodium

Biological Activity

[Description]:

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.

[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. View Related Products by Target Other Targets

Chemical & Physical Properties

[ Molecular Formula ]:
C23H30N5NaO4

[ Molecular Weight ]:
463.514


Related Compounds