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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
GGTI 298 TFA (GGTI-298), the trifluoroacetic acid salt of GGTI 298, is a novel and potent geranylgeranyltransferase I (GGTase-I) inhibitor with ability to arrest human tumor cells in the G1 phase of the cell cycle and induce apoptosis. It has potential antitumor actrivity. GGTI 298 strongly inhibiting the processing of geranylgeranylated Rap1A with little effect on processing of farnesylated Ha-Ras, with IC50 values of 3 and > 10 μM, respectively. GGTI-298 has little effect on the expression levels of CDK2, CDK4, CDK6, cyclins D1 and E, but decreases the levels of cyclin A.
| ln Vitro |
The apical K+ conductance increased by cAMP agonist is considerably reduced by RhoA inhibitor (GGTI298 Trifluoroacetate)[1]. When GGTI298 Trifluoroacetate and TRAIL are used to cause DR5-dependent apoptosis, DR4 knockdown eliminates NF-κB activation and makes the cell more susceptible to this process. Trifluoroacetate/TRAIL (GGTI298 ) inhibits Akt and increases NF-κB. IκBα and p-Akt reduction produced by GGTI298/TRAIL are prevented by DR5 knockdown, indicating that DR5 mediates the reduction of these molecules induced by GGTI298/TRAIL. On the other hand, DR4 knockdown makes GGTI298 /TRAIL-induced p-Akt decrease even easier[2].
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| ln Vivo |
In vivo mouse ileal loop experiments demonstrate that injections of TRAM-34, GGTI298 Trifluoroacetate, or H1152 in conjunction with cholera toxin reduce fluid accumulation in a dose-dependent manner[1].
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| 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.
[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. [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 |
| Molecular Formula |
C27H33N3O3S.C2HF3O2
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| Molecular Weight |
593.66
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| CAS # |
1217457-86-7
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| Related CAS # |
GGTI298;180977-44-0
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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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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (4.21 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (4.21 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6845 mL | 8.4223 mL | 16.8447 mL | |
| 5 mM | 0.3369 mL | 1.6845 mL | 3.3689 mL | |
| 10 mM | 0.1684 mL | 0.8422 mL | 1.6845 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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