1. GPCR/G Protein
  2. Ras

GGTI298 Trifluoroacetate 

目录号: HY-15871
产品使用指南

GGTI298 是有效的 GGTase I 抑制剂,能够抑制 geranylgeranylated Rap1A 的过程,对 farnesylated Ha-Ras 的过程也有一定影响,在体内,IC50 值分别为 3 和 > 20 μM。

MCE 的所有产品仅用作科学研究,我们不为任何个人用途提供产品和服务
GGTI298 Trifluoroacetate Chemical Structure

GGTI298 Trifluoroacetate Chemical Structure

CAS No. : 1217457-86-7

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

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  

* Please select Quantity before adding items.

Other Forms of GGTI298 Trifluoroacetate:

Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 技术信息

  • 参考文献

Description

GGTI298 is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, strongly inhibiting the processing of geranylgeranylated Rap1A with little effect on processing of farnesylated Ha-Ras, with IC50 values of 3 and > 20 μM in vivo, respectively.

IC50 & Target

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

In Vitro

Both RhoA inhibitor (GGTI298 Trifluoroacetate) 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[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, 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[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 injected together with cholera toxin into the loop[1].

References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
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. 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 indicated. The viable cell number is determined using the sulforhodamine B assay. 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 modified 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 fitted with a disposable needle through the ligated end of the loop as the ligatured is tightened: pure CT (1 μg; positive control), saline (negative control), CT (1 μg) + TRAM-34 (different concentrations in μM as indicated in Fig. 7), 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. The fluid from each loop is collected, and the ratio of the amount of fluid contained in the loop with respect to the length of the loop (fluid accumulation ratio in g/cm) is calculated as a reflection of the efficacy of various inhibitors. 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

Please store the product under the recommended conditions in the Certificate of Analysis.

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.

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称:

 

* 需求量:

* 客户姓名:

 

* Email:

   电话:

 

* 公司或机构名称:

   留言给我们:

Bulk Inquiry

Inquiry Information

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