GGTI298 Trifluoroacetate
Based on 9 publication(s) in Google Scholar
GGTI298 Trifluoroacetate is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, which can inhibit Rap1A with IC50 of 3 μM; little effect on Ha-Ras with IC50 of >20 μM.
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- Reinheit: 99.61%
- CAS. Nr.: 1217457-86-7
- Formel: C29H34F3N3O5S
- Molecular Weight:593.66
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) GGTI298 Trifluoroacetate
More- Immunity. 2026 May 13:S1074-7613(26)00171-8. [Abstract]
- Nat Commun. 2025 Nov 21;16(1):10263. [Abstract]
- Redox Biol. 2026 Mar:90:104029. [Abstract]
- J Neuroinflammation. 2024 Nov 14;21(1):295. [Abstract]
- Mol Cell Proteomics. 2023 Aug;22(8):100593. [Abstract]
- Int Immunopharmacol. 2023 Apr:117:110014. [Abstract]
- Arthritis Res Ther. 2024 Dec 19;26(1):222. [Abstract]
- iScience. 2026 Jun 5;29(6):116268. [Abstract]
- J Oral Biosci. 2023 Dec;65(4):347-355. [Abstract]
Customer Validation & Images
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Cell Imaging/Staining
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WB
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IP
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In Vivo Efficacy Study
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Histological Imaging/Staining
Biologische Aktivität
IC50: 3 μM (Rap1A, in vivo), > 20 μM (Ha-Ras, in vivo)[3]
RhoA inhibitor (GGTI298 Trifluoroacetate) significantly reduces cAMP agonist-stimulated apical K+ conductance[1]. Knockdown of DR4 abolishes NF-κB activation, leading to sensitization of DR5-dependent apoptosis induced by the combination of GGTI298 Trifluoroacetate and TRAIL. GGTI298 Trifluoroacetate/TRAIL activates NF-κB and inhibits Akt. Knockdown of DR5, prevents GGTI298/TRAIL-induced IκBα and p-Akt reduction, suggesting that DR5 mediates reduction of IκBα and p-Akt induced by GGTI298/TRAIL. In contrast, DR4 knockdown further facilitates GGTI298/TRAIL-induced p-Akt reduction[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1217457-86-7
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Appearance Solid
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Molecular Weight 593.66
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Formel C29H34F3N3O5S
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Color White to yellow
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SMILES
CC(C)C[C@@H](C(OC)=O)NC(C1=CC=C(NC[C@@H](N)CS)C=C1C2=C3C=CC=CC3=CC=C2)=O.O=C(O)C(F)(F)F
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (9)
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Journal Impact Factor
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Most Recent
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Immunity
Modulation of the mevalonate pathway by TCR engagement regulates T follicular helper cell generation in homeostasis and autoimmunity. [Abstract]2026 May 13:S1074-7613(26)00171-8. PMID: 42134327 -
Nat Commun
Remodeling of the immune microenvironment is linked to adverse outcome in pediatric T cell acute lymphoblastic leukemia. [Abstract]2025 Nov 21;16(1):10263. PMID: 41271691 -
Redox Biol
Upregulated GBP2 exacerbates Parkinson's disease pathogenesis by impairing NIX-dependent mitophagy. [Abstract]2026 Mar:90:104029. PMID: 41570768
GGTI298 Trifluoroacetate purchased from MedChemExpress. Usage Cited in: Redox Biol. 2026 Mar:90:104029. [Abstract]
SH-SY5Y cells were transfected with Flag-GBP2, Flag-GBP2-ΔCAAX, or treated with the geranylgeranylation inhibitor GGTI298 Trifluoroacetate (10 μM) for 48 h.
GGTI298 Trifluoroacetate purchased from MedChemExpress. Usage Cited in: Redox Biol. 2026 Mar:90:104029. [Abstract]
SH-SY5Y cells were transfected with Flag-GBP2, Flag-GBP2-ΔCAAX, or treated with the geranylgeranylation inhibitor GGTI298 Trifluoroacetate (10 μM) for 48 h.
GGTI298 Trifluoroacetate purchased from MedChemExpress. Usage Cited in: Redox Biol. 2026 Mar:90:104029. [Abstract]
Co-IP assays in HEK293T cells show that GGTI298 Trifluoroacetate treatment or expression of the GBP2-ΔCAAX mutant impairs the interaction between GBP2 and NIX.
GGTI298 Trifluoroacetate purchased from MedChemExpress. Usage Cited in: Redox Biol. 2026 Mar:90:104029. [Abstract]
Behavioral tests (open field, pole, rotarod) demonstrate that GGTI298 Trifluoroacetate (12 mg/kg daily for fourteen consecutive days, ip) treatment ameliorates MPTP-induced motor deficits.
GGTI298 Trifluoroacetate purchased from MedChemExpress. Usage Cited in: Redox Biol. 2026 Mar:90:104029. [Abstract]
IHC for TH in the substantia nigra and striatum show that GGTI298 Trifluoroacetate (12 mg/kg daily for fourteen consecutive days, ip) treatment preserves dopaminergic neurons.
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J Neuroinflammation
Prolactin deficiency drives diabetes-associated cognitive dysfunction by inducing microglia-mediated synaptic loss. [Abstract]2024 Nov 14;21(1):295. PMID: 39543619 -
Mol Cell Proteomics
Prenylated PALM2 Promotes the Migration of Esophageal Squamous Cell Carcinoma Cells through Activating Ezrin. [Abstract]2023 Aug;22(8):100593. PMID: 37328063 -
Int Immunopharmacol
Activation of the Epac/Rap1 signaling pathway alleviates blood-brain barrier disruption and brain damage following cerebral ischemia/reperfusion injury. [Abstract]2023 Apr:117:110014. PMID: 36931001 -
Arthritis Res Ther
KLF2 controls the apoptosis of neutrophils and is associated with disease activity of systemic lupus erythematosus. [Abstract]2024 Dec 19;26(1):222. PMID: 39702240 -
iScience
Targeting Rap1-YAP1 mechanosignaling for ameliorating acute IOP elevation-induced trabecular meshwork dysfunction. [Abstract]2026 Jun 5;29(6):116268. PMID: 42291280 -
J Oral Biosci
Simvastatin inhibits proliferation and promotes apoptosis of oral squamous cell carcinoma through KLF2 signal. [Abstract]2023 Dec;65(4):347-355. PMID: 37625505
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (168.45 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (4.21 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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 (4.21 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Protokoll
The given cells are lysed with reporter lysis buffer and subjected to luciferase activity assay using luciferase assay system in a luminometer. Relative luciferase activity is normalized to protein content[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cells are seeded in 96-well cell culture plates and treated the next day with the agents (including GGTI298 Trifluoroacetate). The viable cell number is determined using the sulforhodamine B assay[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
The ileal loop experiment is performed in 6-8-week-old mice by a modifing rabbit ileal loop assay. Following gut sterilization, the animals are kept fasted for 24 h prior to surgery and fed only water ad libitum. Anesthesia is induced by a mixture of ketamine (35 mg/kg of body weight) and xylazine (5 mg/kg of body weight). A laparotomy is performed, and the experimental loops of 5-cm length are constricted at the terminal ileum by tying with non-absorbable silk. The following fluids are instilled in each loop by means of a tuberculin syringe fitting with a disposable needle through the ligated end of the loop: pure CT (1 μg; positive control), saline (negative control), CT (1 μg)+TRAM-34 (different concentrations in μM), CT (1 μg)+ H1152 (1 μM), and CT (1 μg)+GGTI298 Trifluoroacetate (different concentrations in μM), a specific inhibitor of Rap1A. The intestine is returned to the peritoneum, and the mice are sutured and returned to their cages. After 6 h, these animals are sacrificed by cervical dislocation, and the loops are excised[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Sheikh IA, et al. The Epac1 signaling pathway regulates Cl- secretion via modulation of apical KCNN4c channels in diarrhea. J Biol Chem. 2013 Jul 12;288(28):20404-15. [Content Brief]
[2]. Chen S, et al. Dissecting the roles of DR4, DR5 and c-FLIP in the regulation of geranylgeranyltransferase I inhibition-mediated augmentation of TRAIL-induced apoptosis. Mol Cancer. 2010 Jan 29;9:23. [Content Brief]
[3]. McGuire TF, et al. Platelet-derived growth factor receptor tyrosine phosphorylation requires protein geranylgeranylation but not farnesylation. J Biol Chem. 1996 Nov 1;271(44):27402-7. [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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6845 mL | 8.4223 mL | 16.8447 mL | 42.1116 mL |
| 5 mM | 0.3369 mL | 1.6845 mL | 3.3689 mL | 8.4223 mL | |
| 10 mM | 0.1684 mL | 0.8422 mL | 1.6845 mL | 4.2112 mL | |
| 15 mM | 0.1123 mL | 0.5615 mL | 1.1230 mL | 2.8074 mL | |
| 20 mM | 0.0842 mL | 0.4211 mL | 0.8422 mL | 2.1056 mL | |
| 25 mM | 0.0674 mL | 0.3369 mL | 0.6738 mL | 1.6845 mL | |
| 30 mM | 0.0561 mL | 0.2807 mL | 0.5615 mL | 1.4037 mL | |
| 40 mM | 0.0421 mL | 0.2106 mL | 0.4211 mL | 1.0528 mL | |
| 50 mM | 0.0337 mL | 0.1684 mL | 0.3369 mL | 0.8422 mL | |
| 60 mM | 0.0281 mL | 0.1404 mL | 0.2807 mL | 0.7019 mL | |
| 80 mM | 0.0211 mL | 0.1053 mL | 0.2106 mL | 0.5264 mL | |
| 100 mM | 0.0168 mL | 0.0842 mL | 0.1684 mL | 0.4211 mL |
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