1. GPCR/G Protein
    Apoptosis
  2. Ras
    Apoptosis
  3. GGTI298 Trifluoroacetate

GGTI298 Trifluoroacetate 

Cat. No.: HY-15871 Purity: >98.0%
Handling Instructions

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.

For research use only. We do not sell to patients.

GGTI298 Trifluoroacetate Chemical Structure

GGTI298 Trifluoroacetate Chemical Structure

CAS No. : 1217457-86-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 235 In-stock
Estimated Time of Arrival: December 31
1 mg USD 90 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 280 In-stock
Estimated Time of Arrival: December 31
25 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 750 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

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

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].

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

Molecular Weight

593.66

Formula

C₂₉H₃₄F₃N₃O₅S

CAS No.

1217457-86-7

SMILES

CC(C)C[[email protected]@H](C(OC)=O)NC(C1=CC=C(NC[[email protected]@H](N)CS)C=C1C2=C3C=CC=CC3=CC=C2)=O.O=C(O)C(F)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (252.67 mM; Need ultrasonic and warming)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent 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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (4.21 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (4.21 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.21 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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
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Keywords:

GGTI298GGTI 298GGTI-298RasApoptosisInhibitorinhibitorinhibit

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Product Name:
GGTI298 Trifluoroacetate
Cat. No.:
HY-15871
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