Farnesylthioacetic acid
Farnesylthioacetic acid is a competitive, non-substrate inhibitor of Prenylcysteine α-carboxyl methyltransferase. It acts as a non-substrate competitive inhibitor of Arabidopsis thaliana Prenylcysteine α-carboxyl methyltransferase and blocks methyltransferase activity. Farnesylthioacetic acid does not inhibit protein farnesyltransferase activity in Arabidopsis. It induces Apoptosis. Farnesylthioacetic acid regulates the subcellular localization of Ras protein, reducing the proportion of cytoplasmic Ras protein without disrupting membrane binding. It enhances ABA-induced seed dormancy, delays seed germination, and promotes maximum stomatal closure at lower exogenous ABA concentrations. Farnesylthioacetic acid can be used in studies related to promyelocytic leukemia.
For research use only. We do not sell to patients.
- CAS No.: 135784-48-4
- Formula: C17H28O2S
- Molecular Weight:296.47
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
90 μM
Compound: 11
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Agonist activity at human TRPA1 channel expressed in CHO cells assessed as increase in intracellular calcium levels
Agonist activity at human TRPA1 channel expressed in CHO cells assessed as increase in intracellular calcium levels
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[PMID: 20356305] |
Farnesylthioacetic acid (2-25 μM; 8 h-2 days) potently inhibits the growth of promyelocytic leukemia HL-60 cells, achieving complete inhibition at a concentration of 5 μM after 2 days, and induces dose-dependent apoptosis, which is characterized by accumulation of cells in sub-G1 phase, increased annexin V binding, and formation of DNA ladder bands[1].
Farnesylthioacetic acid (10-100 μM; 30 min) potently inhibits methylation of the 20-23 kDa protein in HL-60 cell extracts, with an IC50 of 30 μM, while it exhibits weak or no inhibitory effects on histones of other molecular weights[1].
Farnesylthioacetic acid (10 μM; 8 h) increases the proportion of ras protein in the membrane fraction of promyelocytic leukemia HL-60 cells, while reducing the level of cytoplasmic ras protein, without altering the total abundance of ras protein[1].
Farnesylthioacetic acid (100 μM) exhibits no inhibitory effect on protein farnesyltransferase activity in crude extracts of cultured Arabidopsis thaliana cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human promyelocytic HL-60 leukemic cells
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Concentration:2 μM; 5 μM; 10 μM; 25 μM
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Incubation Time:8 h; 12 h; 2 days
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Result:Inhibited HL-60 cell growth in a dose-dependent manner, with complete inhibition at 5 μM after 2 days.
Induced dose-dependent appearance of a sub-G1 cell population: 16% of cells were in sub-G1 with 5 μM, 26% with 10 μM, and 49% with 25 μM after 8 h.
Increased annexin V-FITC binding in a dose-dependent manner, with early apoptotic cells making up 23% of the population with 2 μM, 22% with 5 μM, and 42% with 10 μM after treatment.
Induced internucleosomal DNA degradation, forming the characteristic apoptotic DNA laddering pattern after incubation with 10 μM for 12 h.
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Cell Line:human promyelocytic HL-60 leukemic cells
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Concentration:10 μM
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Incubation Time:8 h
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Result:Did not reduce membrane-associated ras protein levels; instead, increased the proportion of ras in the membrane fraction and decreased the proportion in the cytosolic fraction.
Did not alter total ras protein levels in whole cell lysates, and calmodulin subcellular distribution remained unchanged, confirming fractionation integrity.
Chemical Information
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CAS No. 135784-48-4
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Appearance Viscous Liquid
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Molecular Weight 296.47
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Formula C17H28O2S
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Color Colorless to light yellow
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SMILES
C/C(C)=C\CC/C(C)=C/CC/C(C)=C/CSCC(O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL (337.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.43 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.43 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (270 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Pérez-Sala D, et al. Analogs of farnesylcysteine induce apoptosis in HL-60 cells. FEBS Lett. 1998;426(3):319-324. [Content Brief]
[2]. Narasimha Chary S, et al. Prenylcysteine alpha-carboxyl methyltransferase expression and function in Arabidopsis thaliana. Plant J. 2002;32(5):735-747. [Content Brief]
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 (stored under nitrogen). 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 |
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| DMSO | 1 mM | 3.3730 mL | 16.8651 mL | 33.7302 mL | 84.3256 mL |
| 5 mM | 0.6746 mL | 3.3730 mL | 6.7460 mL | 16.8651 mL | |
| 10 mM | 0.3373 mL | 1.6865 mL | 3.3730 mL | 8.4326 mL | |
| 15 mM | 0.2249 mL | 1.1243 mL | 2.2487 mL | 5.6217 mL | |
| 20 mM | 0.1687 mL | 0.8433 mL | 1.6865 mL | 4.2163 mL | |
| 25 mM | 0.1349 mL | 0.6746 mL | 1.3492 mL | 3.3730 mL | |
| 30 mM | 0.1124 mL | 0.5622 mL | 1.1243 mL | 2.8109 mL | |
| 40 mM | 0.0843 mL | 0.4216 mL | 0.8433 mL | 2.1081 mL | |
| 50 mM | 0.0675 mL | 0.3373 mL | 0.6746 mL | 1.6865 mL | |
| 60 mM | 0.0562 mL | 0.2811 mL | 0.5622 mL | 1.4054 mL | |
| 80 mM | 0.0422 mL | 0.2108 mL | 0.4216 mL | 1.0541 mL | |
| 100 mM | 0.0337 mL | 0.1687 mL | 0.3373 mL | 0.8433 mL |
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