1. GPCR/G Protein
  2. Ras

GGTI298 Trifluoroacetate 

目录号: HY-15871 纯度: >98.0%
Data Sheet SDS 产品使用指南

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 ¥4571 In-stock
1 mg ¥1100 In-stock
5 mg ¥3500 In-stock
10 mg ¥5500 In-stock
25 mg ¥11000 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Description

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].

References
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
[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[2]. 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 (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
[1]

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.

References
Molecular Weight

593.66

Formula

C₂₉H₃₄F₃N₃O₅S

CAS No.

1217457-86-7

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

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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产品名称:
GGTI298 Trifluoroacetate
目录号:
HY-15871
需求量: