GGTI298
Based on 10 publication(s) in Google Scholar
GGTI298 is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, strongly inhibiting the processing of geranylgeranylated Rap1A with little effect on processing of farnesylated Ha-Ras, with IC50 values of 3 and > 20 μM in vivo, respectively.
The free form of the compound is prone to instability, it is advisable to consider the stable salt form (GGTI298 Trifluoroacetate) that retains the same biological activity.
For research use only. We do not sell to patients.
- CAS No.: 180977-44-0
- Formula: C27H33N3O3S
- Molecular Weight:479.63
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Storage:Powder -20°C, 3 years , 4°C, 2 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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GGTI298
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]
- J Cardiothorac Surg. 2026 Jun 30.
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
Biological Activity
Description
IC50 & Target
IC50: 3 μM (Rap1A, in vivo), > 20 μM (Ha-Ras, in vivo)[3]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HepG2 | IC50 |
30 μM
Compound: GGTI-298
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Antimalarial activity against Plasmodium berghei NK65 infected in human HepG2 cells after 48 hrs by RT-PCR
Antimalarial activity against Plasmodium berghei NK65 infected in human HepG2 cells after 48 hrs by RT-PCR
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[PMID: 20457823] |
In Vitro
Both RhoA inhibitor (GGTI298) and ROCK inhibitor (H1152) significantly reduce cAMP agonist-stimulated IK(ap), whereas the latter additionally reduces colocalization of KCNN4c with the apical membrane marker wheat germ agglutinin in T84WT cells[1].
Knockdown of DR4 abolishes NF-κB activation, leading to sensitization of DR5-dependent apoptosis induced by the combination of GGTI298 and TRAIL. GGTI298/TRAIL activates NF-κB and inhibits Akt. knockdown of DR5, preventes 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.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 180977-44-0
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Appearance Solid
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Molecular Weight 479.63
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Formula C27H33N3O3S
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Color White to gray
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (10)
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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 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 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 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 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 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 -
Purity & Documentation
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Data Sheet (277 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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