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| Targets |
Kinetin triphosphate tetrasodium targets the mitochondrial serine/threonine kinase PINK1 (wild-type and mutant forms including G309D). It acts as an alternative phosphate donor to ATP, with catalytic efficiency superior to endogenous ATP. KTP binds to the active site of PINK1 and facilitates autophosphorylation at the T257 site. By restoring PINK1 activity to near wild-type levels, it enhances mitophagy and protects against mitochondrial dysfunction.
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| ln Vitro |
In HeLa cells, kinetikin triphosphate tetrasodium can act as a phosphate donor to help PINK1 identify the T257 autophosphorylation site and can bring back PINK1 G309D catalytic activity to nearly WT levels in vitro [1].
In cell-free biochemical assays, Kinetin triphosphate tetrasodium acts as a phosphate donor for PINK1. Its catalytic efficiency (kcat/Km) with PINK1 is higher than that of ATP. The compound can be used to screen for PINK1 modulators, as it provides a quantitative signal-to-noise advantage in enzyme activity assays. KTP also restores the catalytic activity of the disease-associated PINK1 G309D mutant to near wild-type levels in vitro. |
| ln Vivo |
In HeLa cells, Kinetin triphosphate tetrasodium acts as a phosphate donor for PINK1 to recognize the T257 autophosphorylation site. The compound restores the catalytic activity of PINK1 G309D to nearly wild-type levels in vitro. In cultured cell models of mitochondrial dysfunction, KTP enhances PINK1-dependent Parkin recruitment to depolarized mitochondria, promoting mitophagy. This is measured by immunofluorescence staining of Parkin and mitochondrial markers (e.g., Tom20) and by Western blot analysis of ubiquitination.
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| Enzyme Assay |
The ability of Kinetin triphosphate tetrasodium to act as a phosphate donor for PINK1 is measured using a cell-free kinase assay. Recombinant PINK1 (wild-type or G309D) is incubated with KTP or ATP, along with a peptide substrate (e.g., a synthetic peptide containing a PINK1 phosphorylation site). The reaction is quenched by the addition of EDTA, and phosphorylated peptide is quantified by mass spectrometry or by using phospho-specific antibodies in an ELISA format. KTP shows higher catalytic efficiency than ATP.
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| Cell Assay |
HeLa cells or primary fibroblasts from Parkinson's disease patients are cultured in DMEM with 10% FBS. To induce mitochondrial depolarization, cells are treated with the uncoupler CCCP (10-20 uM) in the presence or absence of Kinetin triphosphate tetrasodium (1-100 uM). PINK1 accumulation on mitochondria is assessed by Western blot following mitochondrial fractionation. Parkin recruitment is measured by immunofluorescence staining (Parkin co-localization with Tom20). Mitophagy is quantified by measuring LC3-II accumulation or by flow cytometry using mitophagy reporters.
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| Animal Protocol |
Kinetin triphosphate tetrasodium can be evaluated in vivo in PINK1 knockout or PINK1 G309D knock-in mouse models of Parkinson's disease. The compound is administered via intraperitoneal injection (e.g., 5-20 mg/kg daily for 2-4 weeks) or via intracranial injection. Motor function is assessed by rotarod, open field, and pole tests. Post-mortem analysis includes tyrosine hydroxylase staining in the substantia nigra, measurement of striatal dopamine levels by HPLC, and assessment of mitochondrial function in brain tissues.
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| ADME/Pharmacokinetics |
Kinetin triphosphate tetrasodium has a molecular weight of 675.19 Da and molecular formula C15H16N5Na4O14P3. It is the tetrasodium salt of KTP, which is an ATP analogue (6-Fu-ATP). The compound is soluble in water and should be stored at 4degC, sealed, away from moisture. It is stable as a powder for several months. In solution, it should be used promptly or stored at -20degC for short-term use. The compound is stable at neutral pH but may hydrolyze at acidic pH.
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| Toxicity/Toxicokinetics |
Kinetin triphosphate tetrasodium is generally well-tolerated in animal studies at typical doses (5-20 mg/kg). No significant acute toxicity has been reported. As an ATP analogue, there is a potential for off-target effects on other ATP-dependent enzymes (kinases, ATPases) at high concentrations. However, its selectivity for PINK1 is thought to be due to the unique structural features of KTP. Standard laboratory safety precautions should be followed.
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| References | |
| Additional Infomation |
Kinetin triphosphate tetrasodium is a research compound not approved for clinical use. It was originally characterized in a landmark study (Hertz et al., Cell 2013) as a neo-substrate that amplifies the catalytic activity of PINK1. KTP enables precise temporal dissection of mitophagy without endogenous ATP interference. It has therapeutic potential for Parkinson's disease, particularly for patients with PINK1 mutations. The compound is also known as 6-Fu-ATP (6-furfuryl-aminopurine riboside-5'-triphosphate) tetrasodium salt.
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| Molecular Formula |
C15H16N5NA4O14P3
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| Molecular Weight |
675.19
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| Related CAS # |
Kinetin triphosphate;1450894-16-2
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| Appearance |
Typically exists as solid at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O :~250 mg/mL (~370.27 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4811 mL | 7.4053 mL | 14.8106 mL | |
| 5 mM | 0.2962 mL | 1.4811 mL | 2.9621 mL | |
| 10 mM | 0.1481 mL | 0.7405 mL | 1.4811 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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