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GGTI-2133

Catalog No. T24088 CAS 191102-79-1

Synonyms: GGTI2133, GGTI 2133

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.

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GGTI-2133, CAS 191102-79-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 293.00
5 mg	In stock	$ 722.00
10 mg	In stock	$ 987.00
25 mg	In stock	$ 1,490.00
50 mg	In stock	$ 1,980.00
100 mg	In stock	$ 2,760.00

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Purity: 99.80%

ee: 100%

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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]

Synonyms	GGTI2133, GGTI 2133
Molecular Weight	456.54
Formula	C27H28N4O3
CAS No.	191102-79-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (109.52 mM)

References and Literature

1. Chiba Y, et al. Inhibition of geranylgeranyltransferase inhibits bronchial smooth muscle hyperresponsiveness in mice. Am J Physiol Lung Cell Mol Physiol. 2009;297(5):L984-L991. 2. Merza M, et al. Inhibition of geranylgeranyltransferase attenuates neutrophil accumulation and tissue injury in severe acute pancreatitis. J Leukoc Biol. 2013;94(3):493-502. 3. Ohsawa M, et al. Involvement of protein isoprenylation in neuropathic pain induced by sciatic nerve injury in mice. Neurosci Lett. 2014;564:27-31. 4. Abdullah MI, et al. Inhibition of the mevalonate pathway augments the activity of pitavastatin against ovarian cancer cells. Sci Rep. 2017;7(1):8090.

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Keywords

GGTI-2133 191102-79-1 Metabolism Transferase GGTI2133 GGTI 2133 inhibitor inhibit

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