| Size | Price | |
|---|---|---|
| Other Sizes |
| Targets |
Himic anhydride specifically targets and inhibits the activity of protein phosphatase 2A (PP2A). PP2A is a major eukaryotic serine/threonine phosphatase involved in the regulation of numerous cellular processes, including signal transduction, cell cycle progression, and apoptosis. By inhibiting PP2A, Himic anhydride modulates downstream signaling pathways that are implicated in various disease states.
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|---|---|
| ln Vitro |
In vitro assays demonstrate that Himic anhydride functions as a potent inhibitor of protein phosphatase 2A (PP2A). By targeting this key phosphatase, the compound can alter the phosphorylation state of various downstream target proteins involved in cellular regulation. This inhibitory action serves as a crucial mechanism for studying the biological roles of PP2A in cell signaling pathways.
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| ln Vivo |
Currently, no specific in vivo activity data are reported for Himic anhydride in the search results. However, based on its mechanism as a PP2A inhibitor, it has been suggested for potential use in research models of asthma, although the precise in vivo effects have not been characterized. Its use is currently confined to in vitro biochemical and cellular studies.
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| Enzyme Assay |
Binding of Himic anhydride to PP2A is measured by standard phosphatase activity assays using a purified enzyme preparation. In a typical experiment, the enzyme is incubated with graded concentrations of Himic anhydride and a synthetic phosphopeptide substrate (e.g., RRA(pT)VA). Following incubation, the amount of free phosphate released is quantified using a malachite green or Biomol Green detection system. The IC50 value is then calculated from the dose-response curves.
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| Cell Assay |
No specific cellular experimental protocols for Himic anhydride are described in the search results. For a standard cellular PP2A inhibition assay, relevant cell lines (e.g., bronchial epithelial cells or immune cells for asthma research) would be seeded and treated with Himic anhydride at various concentrations. Cell lysates would be collected, and PP2A activity would be measured using a commercially available phosphatase activity kit. Changes in downstream signaling targets (e.g., phosphorylated AKT, ERK) would be assessed by Western blotting.
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| Animal Protocol |
No animal experiments for Himic anhydride are described in the search results. For in vivo evaluation in asthma models, 6-8-week-old female BALB/c mice could be sensitized and challenged with ovalbumin to induce airway inflammation. Himic anhydride would be administered intraperitoneally (IP) at doses ranging from 1-20 mg/kg daily for 7-14 days. At study endpoint, bronchoalveolar lavage fluid (BALF) would be collected for inflammatory cell counts and cytokine analysis (e.g., IL-4, IL-5, IL-13). Lung tissues would be harvested for histological analysis (H&E and PAS staining) to assess airway inflammation and mucus production.
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| ADME/Pharmacokinetics |
Himic anhydride (C₉H₈O3, MW = 164.16) is a solid powder. For storage, the compound should be kept at 4degC sealed, away from moisture and light. For in vitro use, stock solutions in DMSO (100-200 mM) can be stored at -20degC for up to 1 month or at -80degC for up to 6 months. For in vivo use, it can be formulated in 5% DMSO / 5% Tween-80 / 90% saline or in corn oil. No detailed PK parameters (oral bioavailability, Cmax, Tmax, half-life) are reported.
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| Toxicity/Toxicokinetics |
No specific toxicity data for Himic anhydride are reported in the search results. As a research-grade chemical and a modified cantharidin analogue, it is likely to have toxicity potential and should be handled with caution. The compound is not intended for human or veterinary use. Standard laboratory safety precautions, including the use of gloves, lab coat, and safety goggles, should be followed. No LD50 or formal toxicology studies are available.
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| References | |
| Additional Infomation |
See also: 826-62-0 (Note has been moved).
Himic anhydride (cis-5-Norbornene-exo-2,3-dicarboxylic anhydride) is a cantharidin analogue that inhibits protein phosphatase 2A (PP2A). Cantharidin is a natural toxin produced by blister beetles, known for its PP2A inhibitory activity. This compound is for research use only and has not entered clinical trials or received regulatory approval for any indication. Himic anhydride is available from multiple chemical suppliers and is used as a tool for studying PP2A biology and its role in inflammatory diseases such as asthma. |
| Molecular Formula |
C9H8O3
|
|---|---|
| Molecular Weight |
164.16
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| Exact Mass |
164.047
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| CAS # |
2746-19-2
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| PubChem CID |
637794
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| Appearance |
Solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
331.1±42.0 °C at 760 mmHg
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| Melting Point |
140-145ºC(lit.)
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| Flash Point |
163.8±25.1 °C
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| Vapour Pressure |
0.0±0.7 mmHg at 25°C
|
| Index of Refraction |
1.584
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| LogP |
-0.04
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
12
|
| Complexity |
277
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
O1C([C@@]2([H])[C@@]([H])(C1=O)[C@]1([H])C([H])=C([H])[C@@]2([H])C1([H])[H])=O
|
| InChi Key |
KNDQHSIWLOJIGP-RNGGSSJXSA-N
|
| InChi Code |
InChI=1S/C9H8O3/c10-8-6-4-1-2-5(3-4)7(6)9(11)12-8/h1-2,4-7H,3H2/t4-,5+,6+,7-
|
| Chemical Name |
(1S,2S,6R,7R)-4-oxatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 6.0916 mL | 30.4581 mL | 60.9162 mL | |
| 5 mM | 1.2183 mL | 6.0916 mL | 12.1832 mL | |
| 10 mM | 0.6092 mL | 3.0458 mL | 6.0916 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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