| Field | Specification |
|---|---|
| Alternative names | Endothal |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C8H10O5 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Endothall (Endothal) is a protein phosphatase 2A (PP2A) inhibitor, with IC50 values of 90 nM for PP2A and 5 μM for PP1. It can be used as an herbicide and is also useful in cancer chemotherapy[1]. It is supplied as a white to off-white solid (C8H10O5, MW 186.16) at 96.6% purity.
Physical & Chemical Properties
| CAS Number | 145-73-3 |
|---|---|
| Molecular Formula | C8H10O5 |
| Molecular Weight | 186.16 g/mol |
| Purity | 96.6% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | OC(C1C(C2CCC1O2)C(O)=O)=O |
| Signaling Pathway | Metabolic Enzyme/Protease |
| Solubility | In Vitro: DMSO: 100 mg/mL (537.17 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) H2O: 100 mg/mL (537.17 mM; Requires sonication) |
| Storage | -20°C, sealed storage, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (537.17 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
| H2O | 100 mg/mL (537.17 mM) | requires sonication |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); sealed storage, away from moisture; avoid repeated freeze-thaw cycles.
If water is used as the stock solvent, dilute to the working solution and sterilize it through a 0.22 μm filter before use.
Data provided by the manufacturer.
In Vitro
Among structural analogues of Cantharidin, Endothall, an organic acid, is the least toxic one that still inhibits PP2A[2]. Growth of hepatocellular carcinoma (HCC) is inhibited preferentially by Endothall, so the new rat hepatocellular carcinoma lines may prove useful for further biochemical and pharmacological work on PP2A inhibitors and for the testing of new treatment forms for hepatic cell carcinomas. Sensitivity to Endothall is highest in the HR-2, HR-3, HR-4, and Zajdela hepatocellular carcinomas (IC50 of 1.7, 1.2, 0.9, and 1.7 μg/mL), while less sensitivity was seen in newborn rat hepatocytes growing exponentially in primary culture (IC50=6.2 μg/mL), as well as rat DHD/K12 colon carcinoma cells (IC50=3.6 μg/mL) and human HT-29 colon carcinoma cells (IC50=4.9 μg/mL)[2]. In culture, Endothall inhibits growth of HCC lines more strongly than growth of normal hepatocytes or colon carcinomas, and induces mitotic arrest followed by cell death. Endothall produces dose- and time-dependent cytostasis, specifically in G2/M[2]. Cell cycle inhibition at G2/M, followed by apoptotic cell death, is caused by Endothall (3 μg/mL)[2].
In Vivo
The acute LD50 of Endothall in mice is 14 mg/kg[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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