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G5169

Sigma-Aldrich

GGTI 298 trifluoroacetate salt hydrate

≥90% (HPLC), film

同義詞:

N-[[4-(2-(R)-Amino-3-mercaptopropyl)amino]-2-naphthylbenzoyl]leucine methyl ester trifluoroacetate salt hydrate

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About This Item

經驗公式（希爾表示法）:
C27H33N3O3S · C2HF3O2 · xH2O
CAS號碼:
1217457-86-7
分子量：:
593.66 (anhydrous basis)
MDL號碼:
MFCD06409252
分類程式碼代碼:
51111800
PubChem物質ID:
24724490
NACRES:
NA.77

品質等級

100

化驗

≥90% (HPLC)

形狀

film
lyophilized

雜質

<10% dimer

顏色

colorless

mp

99.5-100 °C

溶解度

DMSO: >20 mg/mL

儲存溫度

−20°C

SMILES 字串

OC(=O)C(F)(F)F.COC(=O)[C@H](CC(C)C)NC(=O)c1ccc(NC[C@@H](N)CS)cc1-c2cccc3ccccc23

InChI

1S/C27H33N3O3S.C2HF3O2/c1-17(2)13-25(27(32)33-3)30-26(31)23-12-11-20(29-15-19(28)16-34)14-24(23)22-10-6-8-18-7-4-5-9-21(18)22;3-2(4,5)1(6)7/h4-12,14,17,19,25,29,34H,13,15-16,28H2,1-3H3,(H,30,31);(H,6,7)/t19-,25+;/m1./s1

InChI 密鑰

WALKWJPZELDSKT-UFABNHQSSA-N

基因資訊

human ... PGGT1B(5229)

應用

GGTI 298 trifluoroacetate salt hydrate has been used as a geranylgeranyltransferase I (GGTase I) inhibitor:
  • to study the anticancer effects of statins along with GGTI 298
  • to study its combinatorial effects with FTI-277 on statin-mediated activation of extracellular signal-regulated kinase 5 (ERK5) in the human endothelium
  • to evaluate the effect of protein geranylgeranylation (GG) inhibition on the breast cancer stem cell (CSC) population

生化／生理作用

GGTI 298 is a cell-permeable, prodrug form of the geranylgeranyltransferase I (GGTase I) inhibitor GGTI-297. It inhibits the processing of Rap 1A without effecting the processing of H-Ras.

特點和優勢

This compound is a featured product for Cyclic Nucleotide research. Click here to discover more featured Cyclic Nucleotide products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

象形圖

Exclamation mark
GHS07

訊號詞

Warning

危險聲明

H315,H319,H335

危險分類

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

標靶器官

Respiratory system

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

個人防護裝備

dust mask type N95 (US), Eyeshields, Gloves

分析證明 (COA)

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Mohamad Assi et al.
International journal of molecular sciences, 21(17) (2020-09-06)
KRAS is a powerful oncogene responsible for the development of many cancers. Despite the great progress in understanding its function during the last decade, the study of KRAS expression, subcellular localization, and post-translational modifications remains technically challenging. Accordingly, many facets
Christophe Ginestier et al.
Stem cells (Dayton, Ohio), 30(7), 1327-1337 (2012-05-19)
There is increasing evidence that breast tumors are organized in a hierarchy, with a subpopulation of tumorigenic cancer cells, the cancer stem cells (CSCs), which sustain tumor growth. The characterization of protein networks that govern CSC behavior is paramount to
Rebecca Bertolio et al.
Nature communications, 10(1), 1326-1326 (2019-03-25)
Sterol regulatory element binding proteins (SREBPs) are a family of transcription factors that regulate lipid biosynthesis and adipogenesis by controlling the expression of several enzymes required for cholesterol, fatty acid, triacylglycerol and phospholipid synthesis. In vertebrates, SREBP activation is mainly
Rik van der Kant et al.
Cell stem cell, 24(3), 363-375 (2019-01-29)
Genetic, epidemiologic, and biochemical evidence suggests that predisposition to Alzheimer's disease (AD) may arise from altered cholesterol metabolism, although the molecular pathways that may link cholesterol to AD phenotypes are only partially understood. Here, we perform a phenotypic screen for
P Jiang et al.
British journal of cancer, 111(8), 1562-1571 (2014-08-06)
The increasing usage of statins (the 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors) has revealed a number of unexpected beneficial effects, including a reduction in cancer risk. We investigated the direct anticancer effects of different statins approved for clinical use on human breast
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