iHAP1

Biological Activity

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.

Technical Data

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.

Background References

1. N-benzoylated phenoxazines and phenothiazines: synthesis, antiproliferative activity, and inhibition of tubulin polymerization.
   Prinz et al.
   J.Med.Chem., 2011;54:4247
2. Protein phosphatase 2A as a potential target for treatment of adult T cell leukemia.
   Mori et al.
   Curr.Cancer Drug Targets., 2013;13:829
3. Allosteric activators of protein phosphatase 2A display broad antitumor activity mediated by dephosphorylation of MYBL2.
   Morita et al.
   Cell., 2020;181:702

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