G5294
钛-2133
≥98% (HPLC), geranylgeranyltransferase I inhibitor, solid
别名:
N-[[4-(Imidazol-4-yl)methylamino]-2-(1-naphthyl)benzoyl]leucine trifluoroacetate salt
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关于此项目
经验公式（希尔记法）:
C27H28N4O3 · C2HF3O2
化学文摘社编号:
分子量:
570.56
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
solid
产品名称
钛-2133, ≥98% (HPLC), solid
Quality Segment
assay
≥98% (HPLC)
form
solid
color
white to beige
mp
103-118.5 °C
solubility
DMSO: 25 mg/mL, H2O: insoluble
storage temp.
−20°C
SMILES string
OC(=O)C(F)(F)F.CC(C)C[C@H](NC(=O)c1ccc(NCc2c[nH]cn2)cc1-c3cccc4ccccc34)C(O)=O
InChI
1S/C27H28N4O3.C2HF3O2/c1-17(2)12-25(27(33)34)31-26(32)23-11-10-19(29-15-20-14-28-16-30-20)13-24(23)22-9-5-7-18-6-3-4-8-21(18)22;3-2(4,5)1(6)7/h3-11,13-14,16-17,25,29H,12,15H2,1-2H3,(H,28,30)(H,31,32)(H,33,34);(H,6,7)/t25-;/m0./s1
InChI key
FXXUNOYBYJFSRB-UQIIZPHYSA-N
Gene Information
human ... FNTA(2339), PGGT1B(5229)
Application
GGTI-2133 has been used
- To understand the role of geranylgeranyl transferase in the regulation of CXC chemokine production and neutrophil recruitment in the lung.
- To study the importance of geranylgeranylation in cell adhesion.
- To measure ligand-induced ADP-ribosylation factor 6 (Arf6) activation in breast cancer cells.
Biochem/physiol Actions
GGTase I mediates prenylation to induce the oncogenic functions of the Ras and Rho proteins. Thus, GGTase I inhibitors can be utilized as effective anticancer drugs. They are also useful in treating inflammation, atherosclerosis, multiple sclerosis and other diseases.
GGTI-2133 is a cell-permeable non-thiol peptidomimetic that acts as a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I; IC50 = 38 nM) with a 140-fold selectivity over farnesyltransferase (FTase; IC50 = 5.4 μM).
signalword
Warning
hcodes
Hazard Classifications
Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
target_organs
Respiratory system
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
dust mask type N95 (US), Eyeshields, Gloves
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| G5294-1MG | 04061833633984 |
| G5294-5MG | 04061832981673 |