1. GPCR/G Protein
  2. Ras

GGTI298 Trifluoroacetate 

目录号: HY-15871 纯度: >98.0%

GGTI298 Trifluoroacetate 是有效的 GGTase I 抑制剂, 能够抑制 Rap1AIC50 值为3μM;对 Ha-Ras 的作用很小 IC50 值 > 20 μM。

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GGTI298 Trifluoroacetate Chemical Structure

GGTI298 Trifluoroacetate Chemical Structure

CAS No. : 1217457-86-7

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Size Price Stock Quantity
10 mM * 1 mL in DMSO ¥2351 In-stock
1 mg ¥900 In-stock
5 mg ¥1800 In-stock
10 mg ¥2800 In-stock
25 mg ¥5500 In-stock
50 mg ¥7500 In-stock
100 mg   Get quote  
200 mg   Get quote  

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GGTI298 Trifluoroacetate is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, which can inhibit Rap1A with IC50 of 3 μM; little effect on Ha-Ras with IC50 of >20 μM.

IC50 & Target

IC50: 3 μM (Rap1A, in vivo), > 20 μM (Ha-Ras, in vivo)[3]

In Vitro

RhoA inhibitor (GGTI298 Trifluoroacetate) significantly reduces cAMP agonist-stimulated apical K+ conductance[1]. Knockdown of DR4 abolishes NF-κB activation, leading to sensitization of DR5-dependent apoptosis induced by the combination of GGTI298 Trifluoroacetate and TRAIL. GGTI298 Trifluoroacetate/TRAIL activates NF-κB and inhibits Akt. Knockdown of DR5, prevents 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].

In Vivo

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

Preparing Stock Solutions
Concentration Volume Mass 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
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay

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

Cell Assay

Cells are seeded in 96-well cell culture plates and treated the next day with the agents (including GGTI298 Trifluoroacetate). The viable cell number is determined using the sulforhodamine B assay[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration

The ileal loop experiment is performed in 6-8-week-old mice by a modifing 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 fitting with a disposable needle through the ligated end of the loop: pure CT (1 μg; positive control), saline (negative control), CT (1 μg)+TRAM-34 (different concentrations in μM), CT (1 μg)+ H1152 (1 μM), and CT (1 μg)+GGTI298 Trifluoroacetate (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[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight








Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 150 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.


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GGTI298 Trifluoroacetate