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Key Product Details
| Description: | Allosteric activator of protein phosphatase 2A (PP2A) |
| Chemical Name: | (2-Chloro-10H-phenothiazin-10-yl)(4-methoxyphenyl)methanone |
| Purity: | ≥98% (HPLC) |
| Molecular Weight: | 367.85 |
Biological Activity
Allosteric activator of protein phosphatase 2A (PP2A) (EC50 ~ 0.12 μM); activates PP2A-B56ε subunit. Inhibits proliferation of lymphoblastic leukemia (T-ALL) cell lines including KOPT-Ki, SUPT-13 and RPMI-8402 (IC50 values are 0.3 - 0.8 μM). Inhibits tubulin polymerization in vitro (IC50 = 0.87 μM). Blocks cell cycle causing prometaphase arrest in vitro. Inhibits T-ALL tumor growth in a transgenic zebrafish model and a mouse T-ALL xenograft model.
Technical Data
| M. Wt | 367.85 |
| Formula | C20H14ClNO2S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 105925-39-1 |
| PubChem ID | 2359994 |
| InChi Key | CSWHYHPUEDNIQY-UHFFFAOYSA-N |
| Smiles | COC1=CC=C(C(N2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl)=O)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 18.39 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 367.85.
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 5.44 mL | 27.18 mL | 54.37 mL |
| 2.5 mM | 1.09 mL | 5.44 mL | 10.87 mL |
| 5 mM | 0.54 mL | 2.72 mL | 5.44 mL |
| 25 mM | 0.11 mL | 0.54 mL | 1.09 mL |
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References
References are publications that support the biological activity of the product.
- Prinz N-benzoylated phenoxazines and phenothiazines: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. J.Med.Chem. 2011 PMID: 21563750
- Mori Protein phosphatase 2A as a potential target for treatment of adult T cell leukemia. Curr.Cancer Drug Targets. 2013 PMID: 24015987
- Morita Allosteric activators of protein phosphatase 2A display broad antitumor activity mediated by dephosphorylation of MYBL2. Cell. 2020 PMID: 32315619
Citations
Currently there are no citations for iHAP1.
