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GGTI298

Name: GGTI298
Brand: TargetMol
SKU: T11397
Rating: 4.5 (1 reviews)

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Catalog No. T11397Cas No. 180977-44-0

GGTI298, a CAAZ peptidomimetic and potent geranylgeranyltransferase I (GGTase I) inhibitor, efficiently blocks the processing of geranylgeranylated Rap1A while exerting minimal impact on the processing of farnesylated Ha-Ras. The inhibitor displays in vivo IC50 values of 3 μM for Rap1A and >20 μM for Ha-Ras, respectively.

GGTI298

😃Good

Catalog No. T11397Cas No. 180977-44-0

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$1,820	10-14 weeks	10-14 weeks
50 mg	$2,380	10-14 weeks	10-14 weeks
100 mg	$3,100	10-14 weeks	10-14 weeks

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Product Introduction

Bioactivity

Description	GGTI298, a CAAZ peptidomimetic and potent geranylgeranyltransferase I (GGTase I) inhibitor, efficiently blocks the processing of geranylgeranylated Rap1A while exerting minimal impact on the processing of farnesylated Ha-Ras. The inhibitor displays in vivo IC50 values of 3 μM for Rap1A and >20 μM for Ha-Ras, respectively.
Targets&IC50	Ha-Ras:> 20 μM , Rap1A:3 μM
In vitro	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.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.?Knockdown of DR4 abolishes NF-κB activation, leading to sensitization of DR5-dependent apoptosis induced by the combination of GGTI298 and TRAIL.
In vivo	The in vivo mouse ileal loop experiments demonstrate that TRAM-34, GGTI298, or H1152, when co-administered with cholera toxin, significantly reduce fluid accumulation in a dose-dependent manner.

Chemical Properties

Molecular Weight	479.63
Formula	C₂₇H₃₃N₃O₃S
Cas No.	180977-44-0
Smiles	C(N[C@H](C(OC)=O)CC(C)C)(=O)C1=C(C=C(NC[C@H](CS)N)C=C1)C=2C3=C(C=CC2)C=CC=C3
Relative Density.	1.190 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 100 mg/mL (208.49 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0849 mL	10.4247 mL	20.8494 mL	104.2470 mL
5 mM	0.4170 mL	2.0849 mL	4.1699 mL	20.8494 mL
10 mM	0.2085 mL	1.0425 mL	2.0849 mL	10.4247 mL
20 mM	0.1042 mL	0.5212 mL	1.0425 mL	5.2124 mL
50 mM	0.0417 mL	0.2085 mL	0.4170 mL	2.0849 mL
100 mM	0.0208 mL	0.1042 mL	0.2085 mL	1.0425 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc