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  4. GGTI-2133

GGTI-2133 is an inhibitor for geranylgeranyltransferase I (GGTase-I) with an IC50 of 38 nM. GGTI-2133 inhibits the geranylation of Rap-1A with an IC50 of 10 μM.

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GGTI-2133 Chemical Structure

GGTI-2133 Chemical Structure

CAS No. : 191102-79-1

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1 mg USD 300 In-stock
5 mg USD 750 In-stock
10 mg USD 1150 In-stock
25 mg USD 1900 In-stock
50 mg USD 2750 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of GGTI-2133:

GGTI-2133 Related Antibodies

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Description

GGTI-2133 is an inhibitor for geranylgeranyltransferase I (GGTase-I) with an IC50 of 38 nM. GGTI-2133 inhibits the geranylation of Rap-1A with an IC50 of 10 μM[1].

IC50 & Target

Geran ylgeranyltransferase (GGTase)
Molecular Weight

456.54

Formula

C27H28N4O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)C[C@@H](C(O)=O)NC(C1=CC=C(NCC2=CN=CN2)C=C1C3=C4C=CC=CC4=CC=C3)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (219.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1904 mL 10.9519 mL 21.9039 mL
5 mM 0.4381 mL 2.1904 mL 4.3808 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1904 mL 10.9519 mL 21.9039 mL 54.7597 mL
5 mM 0.4381 mL 2.1904 mL 4.3808 mL 10.9519 mL
10 mM 0.2190 mL 1.0952 mL 2.1904 mL 5.4760 mL
15 mM 0.1460 mL 0.7301 mL 1.4603 mL 3.6506 mL
20 mM 0.1095 mL 0.5476 mL 1.0952 mL 2.7380 mL
25 mM 0.0876 mL 0.4381 mL 0.8762 mL 2.1904 mL
30 mM 0.0730 mL 0.3651 mL 0.7301 mL 1.8253 mL
40 mM 0.0548 mL 0.2738 mL 0.5476 mL 1.3690 mL
50 mM 0.0438 mL 0.2190 mL 0.4381 mL 1.0952 mL
60 mM 0.0365 mL 0.1825 mL 0.3651 mL 0.9127 mL
80 mM 0.0274 mL 0.1369 mL 0.2738 mL 0.6845 mL
100 mM 0.0219 mL 0.1095 mL 0.2190 mL 0.5476 mL
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GGTI-2133 Related Classifications

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.

Keywords:

GGTI-2133191102-79-1GGTI2133GGTI 2133OthersInhibitorinhibitorinhibit

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