| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
Jaspamycin targets protein kinase A (PKA), a key enzyme in cAMP signaling that regulates various cellular processes including metabolism, gene expression, and cell growth. It binds to the R site of PKA (PKAR) and acts as a potent activator. The compound also exhibits antimicrobial, antiviral, and anticancer activities by inhibiting RNA synthesis through incorporation into RNA molecules. Its anti-parasite activity is particularly notable.
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| ln Vitro |
In vitro, Jaspamycin is a potent activator of PKA with an EC₅0 of 6.5 nM and a Kd of 8 nM in Trypanosoma brucei. It exhibits antimicrobial, antiviral, and anticancer activities by inhibiting RNA synthesis through incorporation into RNA molecules, disrupting proper transcription processes. Its anti-parasite activity makes it a valuable tool for studying parasite biology and developing anti-parasitic therapies.
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| ln Vivo |
In vivo studies of Jaspamycin are focused on evaluating its anti-parasite efficacy in animal models of parasitic infections. As a potent PKA activator with anti-parasite activity, the compound may have potential for treating parasitic diseases. Further in vivo studies are needed to fully characterize its efficacy, safety, and pharmacokinetic profile.
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| Enzyme Assay |
For in vitro binding assays, Jaspamycin can be evaluated using PKA binding assays to measure its affinity for the R site of PKA. The compound is incubated with recombinant PKA regulatory subunit at various concentrations. Binding affinity (Kd) is determined using surface plasmon resonance (SPR), isothermal titration calorimetry (ITC), or fluorescence polarization assays. Functional activity as a PKA activator is assessed using kinase activity assays.
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| Cell Assay |
For in vitro cellular experiments, Jaspamycin is tested in parasite cell lines or mammalian cell lines to evaluate its effects on PKA activity and cell growth. Cells are cultured in appropriate media and treated with various concentrations of the compound. PKA activity is assessed by measuring phosphorylation of PKA substrates using Western blotting. Cell viability and proliferation are assessed using standard assays. The compound's effects on RNA synthesis can be evaluated using incorporation of labeled nucleotides.
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| Animal Protocol |
For in vivo animal experiments, Jaspamycin can be administered to animals via various routes including oral gavage, intravenous injection, or intraperitoneal injection. The compound's anti-parasite efficacy can be evaluated in animal models of parasitic infections. Typical doses may range from 1 to 50 mg/kg. Parasite load, survival, and inflammatory markers are assessed. Pharmacodynamic markers such as PKA activity are measured in tissues.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Jaspamycin are not extensively characterized in the literature. As a small molecule with a molecular weight of 292.25, it may have reasonable bioavailability and tissue distribution. The compound is a natural product and nucleoside antibiotic. Detailed parameters such as Cₘₐₓ, Tₘₐₓ, AUC, half-life, and clearance would need to be determined through comprehensive PK studies.
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| Toxicity/Toxicokinetics |
Toxicological data for Jaspamycin are limited, as it is primarily a research tool. As a nucleoside antibiotic that inhibits RNA synthesis, its toxicity would depend on its selectivity for parasite versus host cells. Comprehensive toxicology studies including acute and repeated-dose toxicity, genotoxicity, and cardiotoxicity assessments would be needed for further development. Appropriate safety precautions should be taken when handling this compound.
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| References | |
| Additional Infomation |
Jaspamycin is a research compound used to study PKA biology and develop anti-parasitic therapies. No clinical trials or regulatory approvals have been reported for this compound as a therapeutic agent. It is available from various chemical suppliers for research purposes only. The compound is a naturally occurring metabolite from the marine sponge Jaspis splendens with anti-parasite activity and is a potent PKA activator.
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| Molecular Formula |
C12H12N4O5
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|---|---|
| Molecular Weight |
292.2475
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| Exact Mass |
292.081
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| CAS # |
22242-96-2
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| PubChem CID |
136670059
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.91g/cm3
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| Boiling Point |
724.3ºC at 760 mmHg
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| Flash Point |
391.8ºC
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| Vapour Pressure |
5.1E-22mmHg at 25°C
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| Index of Refraction |
1.827
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| LogP |
-2.1
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
21
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| Complexity |
517
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C1=C(C2=C(N1[C@H]3[C@@H]([C@@H]([C@H](O3)CO)O)O)N=CNC2=O)C#N
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| InChi Key |
SKDKFLFSBDYEDO-WOUKDFQISA-N
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| InChi Code |
InChI=1S/C12H12N4O5/c13-1-5-2-16(10-7(5)11(20)15-4-14-10)12-9(19)8(18)6(3-17)21-12/h2,4,6,8-9,12,17-19H,3H2,(H,14,15,20)/t6-,8-,9-,12-/m1/s1
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| Chemical Name |
7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-4-oxo-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
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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 : ~41.67 mg/mL (~142.58 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.12 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 20.8 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: ≥ 2.08 mg/mL (7.12 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 20.8 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: ≥ 2.08 mg/mL (7.12 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 | 3.4217 mL | 17.1086 mL | 34.2173 mL | |
| 5 mM | 0.6843 mL | 3.4217 mL | 6.8435 mL | |
| 10 mM | 0.3422 mL | 1.7109 mL | 3.4217 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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