| Size | Price | Stock | Qty |
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| 10mg |
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| Targets |
Cytokinin receptor[1]. Parasiter[1]
PI-55 targets the Arabidopsis cytokinin receptors CRE1/AHK4 and AHK3, which are part of the two-component signaling system involved in cytokinin perception. These receptors are histidine kinases that bind cytokinins and initiate a phosphorelay cascade leading to the activation of downstream response regulators. PI-55 is structurally related to the cytokinin 6-benzylaminopurine (BAP) and competitively inhibits the binding of BAP to the receptors. By blocking cytokinin binding, PI-55 prevents receptor activation and downstream cytokinin signaling. The compound shows specificity for Arabidopsis cytokinin receptors, making it a useful tool for studying cytokinin biology in plants. The molecular target is the cytokinin-binding pocket of the receptor proteins. |
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| ln Vitro |
PI-55 at high (10 μM and 100 μM) doses, which results in an inadequate inhibition of the development of the early haustorial structure, particularly when cytokinin activity stimulates it. When BAP is added to PI-55 treatment, P. ramosa becomes less aggressive overall when compared to when BAP is given alone. This suggests that histidine kinase receptors homologous to CRE1/AHK4 and AHK3 are involved in the signaling pathway that leads to the production of early haustorial structures[1].
In vitro, PI-55 has been shown to competitively inhibit the binding of BAP to Arabidopsis-specific receptors CRE1/AHK4 and AHK3. The compound's ability to block cytokinin receptor activation has been demonstrated in various plant-based assays. PI-55 inhibits cytokinin-induced responses in Arabidopsis, including cytokinin-mediated gene expression and physiological responses such as shoot regeneration and senescence delay. The compound is used to study the role of cytokinins in plant development and stress responses. In vitro assays have characterized PI-55 as a potent and specific cytokinin receptor inhibitor, with activity comparable to other known cytokinin antagonists. |
| ln Vivo |
In vivo, PI-55 has been used to study the role of cytokinins in plant-parasite interactions. The compound inhibits cytokinin-induced haustorium formation and increases parasite aggressiveness in plant-pathogen systems. This suggests that cytokinin signaling plays a role in the establishment and development of parasitic interactions. In Arabidopsis, PI-55 treatment blocks cytokinin-mediated responses, allowing researchers to dissect the specific contributions of cytokinin signaling to various physiological processes. The compound has been used in studies investigating the role of cytokinins in root development, shoot branching, and stress tolerance. PI-55 is typically applied to plants via foliar spray or root irrigation in experimental settings.
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| Enzyme Assay |
In vitro binding assays for PI-55 are performed using recombinant Arabidopsis cytokinin receptors (CRE1/AHK4, AHK3) expressed in heterologous systems. The assay involves incubating the receptor protein with a radiolabeled or fluorescently labeled cytokinin (e.g., [³H]-trans-zeatin or fluorescent BAP) in the presence of varying concentrations of PI-55. The displacement of the labeled ligand is measured, and the IC50 for PI-55 is determined. Surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC) can be used to measure the binding affinity (Kd) of PI-55 to the receptor proteins. The assay includes positive controls (unlabeled BAP or other cytokinins) and negative controls (vehicle only).
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| Cell Assay |
In vitro cell-based assays for PI-55 are performed using Arabidopsis cell cultures or plant tissues to assess cytokinin signaling inhibition. Arabidopsis seedlings or cultured cells are treated with PI-55 (typically 1-100 μM) in the presence or absence of cytokinins (e.g., BAP, kinetin, zeatin). Cytokinin-mediated responses are measured, including the expression of cytokinin-responsive genes (e.g., ARR5, ARR6) by qRT-PCR, or physiological responses such as chlorophyll retention (senescence delay) or shoot regeneration. Phosphorylation of downstream response regulators (e.g., ARR1, ARR2) is assessed by Western blotting. The compound's ability to block cytokinin-induced responses is compared to vehicle controls and known cytokinin antagonists.
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| Animal Protocol |
In vivo animal studies are not applicable for PI-55, as the compound is used exclusively in plant biology research. Plant studies are conducted in Arabidopsis thaliana or other plant species. PI-55 is typically applied to plants via foliar spray, root drench, or by incorporation into growth media at concentrations ranging from 1 to 100 μM. The effects on plant growth and development are monitored, including shoot and root growth, leaf senescence, flowering time, and stress responses. In plant-pathogen interaction studies, the effects of PI-55 on haustorium formation and parasite aggressiveness are assessed. Phenotypic analysis and gene expression studies are performed to characterize the effects of cytokinin receptor inhibition.
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| ADME/Pharmacokinetics |
Pharmacokinetic studies are not applicable for PI-55, as the compound is used in plant biology research rather than as a pharmaceutical. In plant studies, the compound's uptake, distribution, and metabolism would be relevant but are not typically characterized in detail. PI-55 is soluble in DMSO (5.83 mg/mL, 22.84 mM) and can be formulated in aqueous solutions with co-solvents for plant applications. The compound's stability in plant tissues and its persistence in the environment would depend on factors such as plant metabolism and degradation. For research use, PI-55 is stored at -20°C and protected from light.
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| Toxicity/Toxicokinetics |
Toxicological studies are not applicable for PI-55 in the context of mammalian toxicity, as the compound is used exclusively in plant research. However, as a chemical reagent, standard safety precautions should be followed when handling PI-55. The compound may cause skin and eye irritation, and appropriate personal protective equipment (gloves, safety goggles, lab coat) should be used. PI-55 should be handled in a well-ventilated area, and exposure should be minimized. The compound is for research use only and not for human or veterinary applications. No specific toxicological data for PI-55 have been reported in the literature.
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| References | |
| Additional Infomation |
PI-55 is a specific cytokinin receptor inhibitor that has been used as a research tool to study cytokinin signaling in plants. Cytokinins are plant hormones that play critical roles in cell division, shoot and root development, leaf senescence, and stress responses. By providing a specific inhibitor of cytokinin receptors, PI-55 enables researchers to dissect the role of cytokinin signaling in various physiological processes without the complications of genetic approaches (e.g., mutants with compensatory effects). The compound has been used in studies investigating the role of cytokinins in plant development, plant-pathogen interactions, and stress tolerance. PI-55 is available from chemical suppliers for research purposes only.
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| Molecular Formula |
C13H13N5O
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|---|---|
| Molecular Weight |
255.275221586227
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| Exact Mass |
255.112
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| CAS # |
1122579-42-3
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| PubChem CID |
67541360
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
1.9
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
19
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| Complexity |
303
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OC1C(C)=CC=CC=1CNC1=C2C(=NC=N1)N=CN2
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| InChi Key |
LYHDZSQXAKLVHV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H13N5O/c1-8-3-2-4-9(11(8)19)5-14-12-10-13(16-6-15-10)18-7-17-12/h2-4,6-7,19H,5H2,1H3,(H2,14,15,16,17,18)
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| Chemical Name |
2-methyl-6-[(7H-purin-6-ylamino)methyl]phenol
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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 |
| 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) |
DMSO : 25 mg/mL (97.93 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (3.92 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1 mg/mL (3.92 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (3.92 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9173 mL | 19.5863 mL | 39.1727 mL | |
| 5 mM | 0.7835 mL | 3.9173 mL | 7.8345 mL | |
| 10 mM | 0.3917 mL | 1.9586 mL | 3.9173 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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