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GGTI-2133

SIGMA/G5294 - ≥98% (HPLC), solid

Synonym: N-[[4-(Imidazol-4-yl)methylamino]-2-(1-naphthyl)benzoyl]leucine trifluoroacetate salt

CAS Number: 1217480-14-2
Empirical Formula (Hill Notation): C27H28N4O3 · C2HF3O2
Molecular Weight: 570.56
MDL Number: MFCD07776925
Linear Formula: C27H28N4O3 · C2HF3O2
Product Type: Chemical
Catalog Number PKG Qty. Price Quantity
45-G5294-1MG 1 mg
 $227.00
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45-G5294-5MG 5 mg
 $857.00
1/EA		 Add To Favorites
This picture is provided solely for illustration purposes, it may have been created or edited with AI. Optical properties of the actual product may deviate. Relevant product information is printed on labeled products and other accompanying or available information material. This image depicts G5294-1MG

 

assay ≥98% (HPLC)
color white to beige
form solid
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
mp 103-118.5 °C
Quality Level 100 
SMILES string OC(=O)C(F)(F)F.CC(C)C[C@H](NC(=O)c1ccc(NCc2c[nH]cn2)cc1-c3cccc4ccccc34)C(O)=O
solubility DMSO: 25 mg/mL
  H2O: insoluble
storage temp. −20°C
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.
Biochem/physiol Actions: 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).
Packaging: 1, 5 mg in glass bottle
Purity ≥98% (HPLC)
mp 103-118.5 °C
Storage Temp. −20°C
UNSPSC 12352200

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