| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
GGTI-2133 targets geranylgeranyltransferase I (GGTase I), an enzyme that catalyzes the transfer of a geranylgeranyl group from geranylgeranyl pyrophosphate to a cysteine residue in the C-terminal CAAX motif of target proteins. By inhibiting GGTase I, the compound blocks the geranylgeranylation of proteins such as Rho, Rac, and Rab GTPases, which are involved in cell proliferation, migration, and cytoskeletal organization.
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| ln Vitro |
In vitro, GGTI-2133 potently inhibits geranylgeranyltransferase I activity. The compound's inhibitory potency has been characterized in enzymatic assays using purified GGTase I and appropriate substrates. By blocking geranylgeranylation, GGTI-2133 prevents the membrane localization and function of geranylgeranylated proteins. Its effects on cell proliferation, migration, and signaling have been studied in various cell types.
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| ln Vivo |
In vivo, GGTI-2133 has been used to study the role of geranylgeranylation in various physiological and pathological processes. By inhibiting GGTase I, the compound modulates the function of Rho, Rac, and other geranylgeranylated proteins in animal models. Its effects on tumor growth, inflammation, and other GGTase I-related processes have been investigated. Specific dosing regimens and detailed efficacy data are available in the scientific literature.
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| Enzyme Assay |
In vitro enzyme assays for GGTI-2133 involve measuring the inhibition of geranylgeranyltransferase I activity using purified enzyme preparations. The compound is incubated with GGTase I, geranylgeranyl pyrophosphate, and a peptide substrate representing the CAAX motif of a target protein. The transfer of the geranylgeranyl group to the peptide is measured using radiometric or fluorescence-based detection methods. The IC50 value is determined from dose-response curves.
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| Cell Assay |
In vitro cell-based assays for GGTI-2133 involve treating cells with the compound to assess its effects on protein geranylgeranylation, cell proliferation, and signaling. Protein geranylgeranylation is assessed by metabolic labeling or Western blotting using antibodies specific for geranylgeranylated proteins. Cell proliferation is measured using MTT or similar assays. Signaling pathway modulation (e.g., Rho, Rac, MAPK) is analyzed by Western blotting. These assays characterize the compound's cellular effects.
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| Animal Protocol |
In vivo animal experiments for GGTI-2133 have been conducted in models of cancer, inflammation, and other GGTase I-related conditions. Tumor-bearing mice are treated with GGTI-2133, and tumor growth inhibition is monitored. Effects on Rho and Rac signaling are assessed in tissues. Efficacy endpoints depend on the specific model being studied. These studies have helped elucidate the role of geranylgeranylation in various disease states.
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| ADME/Pharmacokinetics |
GGTI-2133 is a cell-permeable inhibitor of geranylgeranyltransferase I. The compound's molecular weight and formula are consistent with its chemical structure. It is typically dissolved in DMSO for in vitro studies and formulated for in vivo administration. Specific pharmacokinetic data such as absorption, distribution, metabolism, and elimination are not extensively reported. The compound is typically stored under recommended conditions for research compounds.
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| Toxicity/Toxicokinetics |
Specific toxicity data for GGTI-2133 is not extensively reported. As a GGTase I inhibitor, its safety profile is related to its effects on geranylgeranylation-dependent protein function. The compound is generally well-tolerated in preclinical studies at concentrations used for GGTase I inhibition. Comprehensive toxicological studies would be required for therapeutic development. Standard safety precautions should be taken when handling the compound in research settings.
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| Additional Infomation |
GGTI-2133 free base is an N-acyl-L-amino acid formed by the condensation of the carboxyl group of 4-{[(imidazol-4-yl)methyl]amino}-2-(naphth-1-yl)benzoic acid with the amino group of L-leucine. It is an inhibitor of type I geraniylgeraniyltransferases, belonging to EC 2.5.1.59 (type I protein geraniylgeraniyltransferase) inhibitors. It is an L-leucine derivative, N-acyl-L-amino acid, naphthalene compound, biaryl compound, imidazole compound, benzamide compound, substituted aniline compound, and secondary amino compound. It is the conjugate base of GGTI-2133 free base (1+).
See also: Ggti-2133 (note moved to). GGTI-2133 is a potent inhibitor of geranylgeranyltransferase I (GGTase I) used in research to study protein geranylgeranylation. By blocking GGTase I, the compound prevents the geranylgeranylation of Rho, Rac, and other GTPases, affecting cell proliferation, migration, and signaling. GGTI-2133 is a valuable tool for studying the role of geranylgeranylation in cell biology and disease. |
| Molecular Formula |
C27H28N4O3
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|---|---|
| Molecular Weight |
456.546
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| Exact Mass |
456.216
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| CAS # |
191102-79-1
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| PubChem CID |
9846868
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| Appearance |
White to off-white solid powder
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| Melting Point |
103-118.5 °C
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| LogP |
5
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
34
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| Complexity |
687
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(C[C@H](NC(C1=C(C2=CC=CC3=CC=CC=C32)C=C(NCC4=CN=CN4)C=C1)=O)C(O)=O)C
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| InChi Key |
ODTFPKNIFYMEHP-VWLOTQADSA-N
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| InChi Code |
InChI=1S/C27H28N4O3/c1-17(2)12-25(27(33)34)31-26(32)23-11-10-19(29-15-20-14-28-16-30-20)13-24(23)22-9-5-7-18-6-3-4-8-21(18)22/h3-11,13-14,16-17,25,29H,12,15H2,1-2H3,(H,28,30)(H,31,32)(H,33,34)/t25-/m0/s1
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| Chemical Name |
(2S)-2-[[4-(1H-imidazol-5-ylmethylamino)-2-naphthalen-1-ylbenzoyl]amino]-4-methylpentanoic acid
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| Synonyms |
GGTI2133; GGTI-2133; GGTI 2133
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1903 mL | 10.9517 mL | 21.9034 mL | |
| 5 mM | 0.4381 mL | 2.1903 mL | 4.3807 mL | |
| 10 mM | 0.2190 mL | 1.0952 mL | 2.1903 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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