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| Targets |
Pterosin B primarily targets SIK3 (salt-inducible kinase 3), a member of the AMPK-related kinase family involved in various cellular processes. It suppresses SIK3 downstream cascades by up-regulating phosphorylation levels in the SIK3 C-terminal regulatory domain. It has no effect on SIK1 or SIK2. By inhibiting SIK3, pterosin B modulates glucose production, glycogen content, and other metabolic processes.
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| ln Vitro |
In vitro, pterosin B is a potent and specific SIK3 signaling inhibitor. It up-regulates phosphorylation levels in the SIK3 C-terminal regulatory domain. In mouse hepatoma AML-12 cells, it decreases glycogen content and stimulates an association between PHKG2 and SIK3. It has no effect on SIK1 or SIK2. Its activity is typically evaluated using kinase activity assays and western blotting for phosphorylated SIK3 substrates.
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| ln Vivo |
In vivo, pterosin B prevents chondrocyte hypertrophy and osteoarthritis in mice. It inhibits cardiomyocyte hypertrophy, improves cognitive impairment, and lowers blood glucose. It reduces β-amyloid deposition. These diverse effects are mediated through SIK3 inhibition. However, specific in vivo efficacy data, including dosing regimens and animal models, are not extensively detailed in the available literature. Further studies are needed to fully characterize its in vivo pharmacological profile.
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| Enzyme Assay |
Cell-free assays for pterosin B involve evaluating its inhibitory activity against SIK3. Kinase activity is measured using radioactive or fluorescence-based assays with peptide substrates. Inhibition is assessed by incubating SIK3 with varying concentrations of pterosin B and measuring residual activity. The compound's specificity for SIK3 over SIK1 and SIK2 is confirmed. Its chemical purity and identity are confirmed by HPLC, NMR, and mass spectrometry.
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| Cell Assay |
In vitro cellular assays for pterosin B typically involve treating AML-12 mouse hepatoma cells or other cell types with various concentrations of the compound. SIK3 signaling is assessed by measuring phosphorylation of downstream targets by western blotting. Glycogen content is measured. Cell viability is assessed using standard assays. The compound's effects on glucose production, chondrocyte hypertrophy, and cardiomyocyte hypertrophy are evaluated in appropriate cell models.
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| Animal Protocol |
In vivo animal studies for pterosin B are conducted in models of osteoarthritis, cardiac hypertrophy, cognitive impairment, and diabetes. The compound is administered via various routes including oral gavage or intraperitoneal injection. Disease progression is monitored using appropriate endpoints. β-amyloid deposition is measured in brain tissues. Blood glucose levels are monitored. However, specific dosing regimens and experimental protocols are not extensively documented in the available literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of pterosin B include a molecular weight of 218.29 g/mol and molecular formula C14H18O2. As a small molecule, it is expected to have moderate oral bioavailability and tissue penetration, including brain penetration. The compound is typically stored as a solid at appropriate conditions. Detailed ADME parameters such as half-life, Cmax, and AUC are not extensively reported in the available literature.
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| Toxicity/Toxicokinetics |
The toxicity profile of pterosin B has not been extensively characterized in published literature. As a SIK3 inhibitor, potential toxicities may include effects on metabolism and glucose homeostasis. Standard preclinical safety studies would include acute and sub-chronic toxicity assessments in rodent models. The compound is intended for research use only and not for therapeutic applications in humans. Standard safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
Pterosin B has been reported to have been found in Pteris vittata, Pteris grenifera, and other organisms with available data.
Pterosin B is a potent and specific SIK3 signaling inhibitor from bracken fern. It prevents osteoarthritis, inhibits cardiac hypertrophy, improves cognitive impairment, lowers blood glucose, and reduces β-amyloid deposition. Its molecular formula is C14H18O2 with a molecular weight of 218.29 g/mol. Pterosin B is a research tool for studying SIK3 signaling and metabolic diseases. It is not for therapeutic use. |
| Molecular Formula |
C14H18O2
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|---|---|
| Molecular Weight |
218.29152
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| Exact Mass |
218.13
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| CAS # |
34175-96-7
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| PubChem CID |
115049
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| Appearance |
White to light yellow solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
396.5±41.0 °C at 760 mmHg
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| Flash Point |
169.3±20.2 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.560
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| LogP |
2.65
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
16
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| Complexity |
274
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@@H]1CC2=C(C1=O)C(=C(C(=C2)C)CCO)C
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| InChi Key |
SJNCSXMTBXDZQA-SECBINFHSA-N
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| InChi Code |
InChI=1S/C14H18O2/c1-8-6-11-7-9(2)14(16)13(11)10(3)12(8)4-5-15/h6,9,15H,4-5,7H2,1-3H3/t9-/m1/s1
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| Chemical Name |
(2R)-6-(2-hydroxyethyl)-2,5,7-trimethyl-2,3-dihydroinden-1-one
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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 : ~250 mg/mL (~1145.27 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (12.60 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 27.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: ≥ 2.75 mg/mL (12.60 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 27.5 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: ≥ 2.75 mg/mL (12.60 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 | 4.5811 mL | 22.9053 mL | 45.8106 mL | |
| 5 mM | 0.9162 mL | 4.5811 mL | 9.1621 mL | |
| 10 mM | 0.4581 mL | 2.2905 mL | 4.5811 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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