GGTI-2133

GGTI-2133, a peptidomimetic, is a selective geranylgeranyltransferase I (GGTase-I) inhibitor with an IC50 of 38 nM. GGTI-2133 shows 140-fold selectivity over farnesyltransferase (FTase) (IC50 of 5.4 μM) . GGTI-2133 inhibits the geranylation of Rap-1A with an IC50 of 10 μM. GGTI-2133 can be used for the study of eosinophilic airway inflammation such as asthma[1][2].

Product Specifications

CAS Number

[191102-79-1]

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

GGTase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/ggti-2133.html

Concentration

10mM

Purity

98.50

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

CC(C)C[C@@H](C(O)=O)NC(C1=CC=C(NCC2=CN=CN2)C=C1C3=C4C=CC=CC4=CC=C3)=O

Molecular Formula

C27H28N4O3

Molecular Weight

456.54

Precautions

H315, H319, H335

References & Citations

[1]Vasudevan A, et al., Potent, highly selective, and non-thiol inhibitors of protein geranylgeranyltransferase-I. J Med Chem. 1999 Apr 22;42 (8) :1333-40. |[2]Chiba Y, et al. GGTI-2133, an inhibitor of geranylgeranyltransferase, inhibits infiltration of inflammatory cells into airways in mouse experimental asthma. Int J Immunopathol Pharmacol. 2009 Oct-Dec;22 (4) :929-35.