GGTI-2133
Based on 1 publication(s) in Google Scholar
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.
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- Pureté : 98.52%
- CAS No.: 191102-79-1
- Formule: C27H28N4O3
- Masse moléculaire:456.54
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) GGTI-2133
More
Activité biologique
Description
IC50 & Target
Geran ylgeranyltransferase (GGTase)
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. 191102-79-1
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Appearance Solid
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Masse moléculaire 456.54
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Formule C27H28N4O3
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Color White to off-white
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
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
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (219.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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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
Pureté et documentation
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Fiche technique (276 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instruction de manipulation (2659 KB)
Références
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.1904 mL | 10.9519 mL | 21.9039 mL | 54.7597 mL |
| 5 mM | 0.4381 mL | 2.1904 mL | 4.3808 mL | 10.9519 mL | |
| 10 mM | 0.2190 mL | 1.0952 mL | 2.1904 mL | 5.4760 mL | |
| 15 mM | 0.1460 mL | 0.7301 mL | 1.4603 mL | 3.6506 mL | |
| 20 mM | 0.1095 mL | 0.5476 mL | 1.0952 mL | 2.7380 mL | |
| 25 mM | 0.0876 mL | 0.4381 mL | 0.8762 mL | 2.1904 mL | |
| 30 mM | 0.0730 mL | 0.3651 mL | 0.7301 mL | 1.8253 mL | |
| 40 mM | 0.0548 mL | 0.2738 mL | 0.5476 mL | 1.3690 mL | |
| 50 mM | 0.0438 mL | 0.2190 mL | 0.4381 mL | 1.0952 mL | |
| 60 mM | 0.0365 mL | 0.1825 mL | 0.3651 mL | 0.9127 mL | |
| 80 mM | 0.0274 mL | 0.1369 mL | 0.2738 mL | 0.6845 mL | |
| 100 mM | 0.0219 mL | 0.1095 mL | 0.2190 mL | 0.5476 mL |
GGTI-2133 Related Classifications
HY-12369 Related Classifications
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