GGTI298
Based on 9 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.
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- CAS 番号: 180977-44-0
- 分子式: C27H33N3O3S
- 分子量:479.63
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 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]
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
生物活性
IC50: 3 μM (Rap1A, in vivo), > 20 μM (Ha-Ras, in vivo)[3]
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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] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 180977-44-0
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性状 Solid
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分子量 479.63
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
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 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
プロトコル
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.
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 indicated. The viable cell number is determined using the sulforhodamine B assay.
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 modified 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 fitted with a disposable needle through the ligated end of the loop as the ligatured is tightened: pure CT (1 μg; positive control), saline (negative control), CT (1 μg) + TRAM-34 (different concentrations in μM as indicated in Fig. 7), CT (1 μg) + H1152 (1 μM), and CT (1 μg) + GGTI298 (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. The fluid from each loop is collected, and the ratio of the amount of fluid contained in the loop with respect to the length of the loop (fluid accumulation ratio in g/cm) is calculated as a reflection of the efficacy of various inhibitors.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
GGTI298 関連分類
HY-100876 関連分類
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