1217480-14-2
Chemical Structure
GGTI-2133 TFA
- CAS No.: 1217480-14-2
- Formula:C29H29F3N4O5
- Molecular Weight:570.56
IUPAC Name: (4-(((1H-imidazol-5-yl)methyl)amino)-2-(naphthalen-1-yl)benzoyl)-L-leucine compound with 2,2,2-trifluoroacetic acid (1:1)
InChIKey: FXXUNOYBYJFSRB-UQIIZPHYSA-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.O=C(O)C(F)(F)F
Biological Activity: GGTI-2133 TFA, a peptidomimetic, is a selective geranylgeranyltransferase I (GGTase-I) inhibitor with an IC50 of 38 nM. GGTI-2133 TFA shows 140-fold selectivity over farnesyltransferase (FTase) (IC50 of 5.4 μM). GGTI-2133 TFA inhibits the geranylation of Rap-1A with an IC50 of 10 μM. GGTI-2133 TFA can be used for the study of eosinophilic airway inflammation such as asthma[1][2].
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GGTI-2133 TFA | GGTI-2133 TFA, a peptidomimetic, is a selective geranylgeranyltransferase I (GGTase-I) inhibitor with an IC50 of 38 nM. GGTI-2133 TFA shows 140-fold selectivity over farnesyltransferase (FTase) (IC50 of 5.4 μM). GGTI-2133 TFA inhibits the geranylation of Rap-1A with an IC50 of 10 μM. GGTI-2133 TFA can be used for the study of eosinophilic airway inflammation such as asthma. | |||||||||||||||||||||
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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]
