GGTI-2133 TFA
Based on 1 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- CAS No.: 1217480-14-2
- Formula: C29H29F3N4O5
- Molecular Weight:570.56
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) GGTI-2133 TFA
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Biological Activity
Description
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male BALB/c mice (8 weeks of age) were actively sensitized byintraperitoneal injections of 8 ug ovalbumin with 2 mg Imject Alum on days 0 and 5[2].
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Dosage:5 mg/kg
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Administration:Intraperitoneal injection; once a day; for 10 days from Day 11 to Day 20
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Result:Inhibited the antigen-induced eosinophil infiltration into airways almost completely.
Chemical Information
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CAS No. 1217480-14-2
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Molecular Weight 570.56
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Formula C29H29F3N4O5
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Rep
ENKD1 modulates innate immune responses through enhanced geranylgeranyl pyrophosphate synthase activity. [Abstract]2025 Mar 5;44(3):115397. PMID: 40048432
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Purity & Documentation
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)