2. Apoptosis
  3. Apoptosis
  4. GGTI298

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

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GGTI298 Related Antibodies

Top Publications Citing Use of Products

    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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    Description

    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.

    IC50 & Target

    IC50: 3 μM (Rap1A, in vivo), > 20 μM (Ha-Ras, in vivo)[3]
    Cellular Effect
    Cell Line Type Value Description References
    HepG2 IC50
    30 μM
    Compound: GGTI-298
    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
    		[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.

    GGTI298 Related Antibodies
    In Vivo

    The vivo mouse ileal loop experiments show fluid accumulation is reduced in a dose-dependent manner by TRAM-34, GGTI298, or H1152 when injected together with cholera toxin into the loop[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    479.63

    Formula

    C27H33N3O3S
    CAS No.
    Appearance

    Solid

    Color

    White to gray

    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Purity & Documentation
    References
    Kinase Assay
    [2]

    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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [2]

    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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
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    GGTI298 Related Classifications

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    × = ×
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    GGTI298180977-44-0GGTI 298GGTI-298ApoptosisInhibitorinhibitorinhibit

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