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Description: Allosteric activator of protein phosphatase 2A (PP2A)
Chemical Name: (2-Chloro-10H-phenothiazin-10-yl)(4-methoxyphenyl)methanone
Purity: ≥98% (HPLC)
Biological Activity for iHAP1
iHAP1 is an 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.
Compound Libraries for iHAP1
iHAP1 is also offered as part of the Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for iHAP1
| 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.
Product Datasheets for iHAP1
References for iHAP1
References are publications that support the biological activity of the product.
Prinz et al (2011) N-benzoylated phenoxazines and phenothiazines: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. J.Med.Chem. 54 4247 PMID: 21563750
Mori et al (2013) Protein phosphatase 2A as a potential target for treatment of adult T cell leukemia. Curr.Cancer Drug Targets. 13 829 PMID: 24015987
Morita et al (2020) Allosteric activators of protein phosphatase 2A display broad antitumor activity mediated by dephosphorylation of MYBL2. Cell. 181 702 PMID: 32315619
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Keywords: iHAP1, iHAP1 supplier, iHAP, PP2A, allosteric, activitor, activators, PP2A-B56e, protein, phosphatase, 2A, T-ALL, prometaphase, cell, cycle, inhibitors, inhibits, Protein, Ser/Thr, Phosphatases, Cell, Cycle, Inhibitors, Microtubules, 7303, Tocris Bioscience
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