191102-79-1
Chemical Structure
GGTI-2133
- CAS No.: 191102-79-1
- Formula:C27H28N4O3
- Molecular Weight:456.54
IUPAC Name: (4-(((1H-imidazol-5-yl)methyl)amino)-2-(naphthalen-1-yl)benzoyl)-L-leucine
InChIKey: ODTFPKNIFYMEHP-VWLOTQADSA-N
SMILES: CC(C)C[C@@H](C(O)=O)NC(C1=CC=C(NCC2=CN=CN2)C=C1C3=C4C=CC=CC4=CC=C3)=O
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
GGTI-2133 | 98.52% | 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. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [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. [Content Brief]
- [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. [Content Brief]
