
CAS Number145-73-3
Synonymsaquatholplus; 7-oxa-bicyclo[2.2.1]heptane-2,3-dicarboxylic acid; 7-Oxabicyclo[2.2.1]heptane-2,3-dicarboxylicacid; Aquathol; Hydout; 7-oxabicyclo[2.2.1]heptane-2,3-dicarboxylic acid; ENDOTHAL; ACCELERATE; MFCD00137362; Niagrathal; Hydrothol; Hydrothal; EINECS 205-660-5; (1Ξ,2Ξ,3Ξ,4Ξ)-7-oxabicyclo[2.2.1]heptane-2,3-dicarboxylic acid; ENDOTHALL; Emdothal
Molecular FormulaC8H10O5
Molecular Weight186.16200
Purity98%
Density1.431
Boiling Point350ºC(e)
Melting Point144ºC
Symbol
Signal WordWarning
| Chemical & Physical Properties | |
|---|---|
| CAS Number | 145-73-3 |
| Catalog No. | 2A-9010321 |
| Chinese Name | 草多索 |
| Synonyms | aquatholplus; 7-oxa-bicyclo[2.2.1]heptane-2,3-dicarboxylic acid; 7-Oxabicyclo[2.2.1]heptane-2,3-dicarboxylicacid; Aquathol; Hydout; 7-oxabicyclo[2.2.1]heptane-2,3-dicarboxylic acid; ENDOTHAL; ACCELERATE; MFCD00137362; Niagrathal; Hydrothol; Hydrothal; EINECS 205-660-5; (1Ξ,2Ξ,3Ξ,4Ξ)-7-oxabicyclo[2.2.1]heptane-2,3-dicarboxylic acid; ENDOTHALL; Emdothal |
| Molecular Formula | C8H10O5 |
| Molecular Weight | 186.16200 |
| Purity | 98 |
| Density | 1.431 |
| Boiling Point | 350ºC(e) |
| Melting Point | 144ºC |
| Storage Condition | Store in a dry and cool place. |
| Packaging | II |
| Application | Endothall (Endothal) is a protein phosphatase 2A (PP2A) inhibitor with IC50s of PP2A and PP1 of 90 nM and 5µM respectively. It can be used as a herbicide. Endothelin is also useful in cancer chemother |
| HTC | 2932190013 |
| SMILES | O=C(O)C1C2CCC(O2)C1C(=O)O |
| InChI | InChI=1S/C8H10O5.2Na/c9-7(10)5-3-1-2-4(13-3)6(5)8(11)12;;/h3-6H,1-2H2,(H,9,10)(H,11,12);;/q;2*+1/p-2 |
| InChI Key | GXEKYRXVRROBEV-UHFFFAOYSA-N |
| Hazard Symbols | 6.1(a) |
| Bioactivity | Endothall (Endothal) is a protein phosphatase 2A (PP2A) inhibitor with IC50s of 90 nM and 5 µM for PP2A and PP1, respectively. Endothall can be used as an herbicide. Endothall also is useful in cancer chemotherapy[1]. Related Catalog Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphatase In Vitro Endothall, an organic acid, is the least toxic structural analogue of Cantharidin that still inhibits PP2A[2]. Endothall inhibits preferentially hepatocellular carcinoma (HCC) growth and these new rat hepatocellular carcinoma lines may be useful for further biochemical and pharmacological studies on PP2A inhibitors, and for testing new forms of treatment of hepatic cell carcinomas. The HR-2, HR-3, HR-4, and Zajdela hepatocellular carcinomas are most sensitive to Endothall (IC50 of 1.7, 1.2, 0.9, and 1.7 µg/mL), whereas newborn rat hepatocytes growing exponentially in primary culture (IC50=6.2 µg/mL), rat DHD/K12 colon carcinoma cells (IC50=3.6 µg/mL), or human HT-29 colon carcinoma cells (IC50=4.9 µg/mL) were less sensitive[2]. Endothall inhibits the growth of HCC lines in culture more than that of normal hepatocytes or colon carcinomas, inducing mitotic arrest, followed by cell death. Endothall causes dose- and time-dependent cytostasis specifically in G2/M[2]. Endothall (3 µg/mL) inhibits the cell cycle at G2/M and subsequent apoptotic cell death[2]. In Vivo Endothall exhibits acute LD50 of 14 mg/kg in mice[2]. References [1]. Janetti R Signorelli, et al. Protein phosphatases decrease their activity during capacitation: a new requirement for this event. PLoS One. 2013 Dec 2;8(12):e81286. [2]. J P Thièry, et al. Hepatocellular carcinoma cell lines from diethylnitrosamine phenobarbital-treated rats. Characterization and sensitivity to endothall, a protein serine/threonine phosphatase-2A inhibitor. Hepatology. 1999 May;29(5):1406-17. Chemical & Physical Properties Density 1.431 Boiling Point 350ºC(e) Melting Point 144ºC Molecular Formula C8H10O5 Molecular Weight 186.16200 Flash Point 190.5ºC Exact Mass 186.05300 PSA 83.83000 Vapour Pressure 2.88E-09mmHg at 25°C Index of Refraction 1.568 InChIKey GXEKYRXVRROBEV-UHFFFAOYSA-N SMILES O=C(O)C1C2CCC(O2)C1C(=O)O |
| Use of | Endothall (Endothal) is a protein phosphatase 2A (PP2A) inhibitor with IC50s of 90 nM and 5 µM for PP2A and PP1, respectively. Endothall can be used as an herbicide. Endothall also is useful in cancer chemotherapy[1]. Properties Name endothal Synonym More Synonyms Endothall Biological Activity Description Endothall (Endothal) is a protein phosphatase 2A (PP2A) inhibitor with IC50s of 90 nM and 5 µM for PP2A and PP1, respectively. Endothall can be used as an herbicide. Endothall also is useful in cancer chemotherapy[1]. Related Catalog Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphatase References [1]. Janetti R Signorelli, et al. Protein phosphatases decrease their activity during capacitation: a new requirement for this event. PLoS One. 2013 Dec 2;8(12):e81286. [2]. J P Thièry, et al. Hepatocellular carcinoma cell lines from diethylnitrosamine phenobarbital-treated rats. Characterization and sensitivity to endothall, a protein serine/threonine phosphatase-2A inhibitor. Hepatology. 1999 May;29(5):1406-17. Chemical & Physical Properties Molecular Formula C8H10O5 Exact Mass 186.05300 PSA 83.83000 Index of Refraction 1.568 InChIKey GXEKYRXVRROBEV-UHFFFAOYSA-N |
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| Transport Info | Product name: Chemical name |
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