GGTI-2133 ≥98% (HPLC), solid ยี่ห้อ Sigma

PROPERTIES

Quality Level

100

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)

DESCRIPTION

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.[1]

To study the importance of geranylgeranylation in cell adhesion.[2]

To measure ligand-induced ADP-ribosylation factor 6 (Arf6) activation in breast cancer cells.[3]

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).

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.[4] They are also useful in treating inflammation, atherosclerosis, multiple sclerosis and other diseases.[5]