1. GPCR/G Protein MAPK/ERK Pathway Apoptosis
  2. Ras Apoptosis
  3. GGTI298

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。

该游离形式化合物不稳定,推荐具有相同生物学活性的稳定盐形式 GGTI298 Trifluoroacetate

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GGTI298 Chemical Structure

GGTI298 Chemical Structure

CAS No. : 180977-44-0

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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

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]

体外研究
(In Vitro)

RhoA 抑制剂 (GGTI298) 和 ROCK 抑制剂 (H1152) 均显着降低 cAMP 激动剂刺激的 IK(ap),而后者还降低 T84WT 细胞中 KCNN4c 与顶膜标记麦芽凝集素的共定位[1]
DR4 的敲低会消除 NF-κB 的激活,从而导致 GGTI298 和 TRAIL 联合诱导的 DR5 依赖性细胞凋亡变得敏感。 GGTI298/TRAIL 激活 NF-κB 并抑制 Akt。敲除 DR5,可阻止 GGTI298/TRAIL 诱导的 IκBα 和 p-Akt 减少,表明 DR5 介导 GGTI298/TRAIL 诱导的 IκBα 和 p-Akt 减少。相比之下,DR4 敲低进一步促进 GGTI298/TRAIL 诱导的 p-Akt 减少[2]

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

体内研究
(In Vivo)

体内小鼠回肠环实验表明,当 TRAM-34、GGTI298 或 H1152 与霍乱毒素一起注射到环中时,液体积聚以剂量依赖性方式减少[1]

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

分子量

479.63

Formula

C27H33N3O3S

CAS 号
性状

固体

颜色

White to gray

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献
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 (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.

参考文献
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  • 稀释计算器

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
GGTI298
目录号:
HY-100876
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