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GGTI-2418

Chemical Structure : GGTI-2418

CAS No.: 501010-06-6

GGTI-2418 (GGTI 2418, PTX 100)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 441.532
分子式 C23H31N5O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
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

参考文献

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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