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GGTI-2133 is a potent mimetic peptidyl geranylgeranyltransferase type I inhibitor (GGTase I) with an IC50 value of 38 nM.GGTI-2133 inhibits the invasion of inflammatory cells into the airways in experimental asthma in mice.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $247 | In Stock | |
5 mg | $619 | In Stock | |
10 mg | $953 | In Stock | |
25 mg | $1,490 | In Stock | |
50 mg | $1,980 | In Stock | |
100 mg | $2,760 | In Stock |
Description | GGTI-2133 is a potent mimetic peptidyl geranylgeranyltransferase type I inhibitor (GGTase I) with an IC50 value of 38 nM.GGTI-2133 inhibits the invasion of inflammatory cells into the airways in experimental asthma in mice. |
In vitro | BSM tissues isolated from the repeatedly antigen-challenged mice were cultured for 48 h in the absence or presence of GGTI-2133. Under these conditions, the putative geranylgeranylated RhoA was decreased in a GGTI-2133 concentration-dependent manner. The in vitro incubation with GGTI-2133 also inhibited BSM hyperresponsiveness induced by antigen exposure. These findings suggest that GGTI-2133 inhibits antigen-induced BSM hyperresponsiveness, probably by reducing downstream signal transduction of RhoA.[1] |
In vivo | Animals also were treated with GGTI-2133 (5 mg/kg; i.p.; once a day; mice with experimental asthma) during the antigen inhalation period. Repeated antigen inhalation caused a BSM hyperresponsiveness to acetylcholine with the increased expressions of RhoA and the anti-farnesyl-positive 21-kDa proteins, probably geranylgeranylated RhoA. The in vivo GGTI-2133 treatments significantly inhibited BSM hyperresponsiveness induced by antigen exposure.[1] |
Alias | GGTI2133, GGTI 2133 |
Molecular Weight | 456.54 |
Formula | C27H28N4O3 |
Cas No. | 191102-79-1 |
Smiles | C(N[C@@H](CC(C)C)C(O)=O)(=O)C1=C(C=2C3=C(C=CC2)C=CC=C3)C=C(NCC4=CN=CN4)C=C1 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (109.52 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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