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Cat.No. 7303 - iHAP1 | C20H14ClNO2S | CAS No. 105925-39-1
Description: Allosteric activator of protein phosphatase 2A (PP2A)
Chemical Name: (2-Chloro-10H-phenothiazin-10-yl)(4-methoxyphenyl)methanone
Purity: ≥98% (HPLC)
Literature (1)

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.

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
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 Data for iHAP1

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 18.39 50

Preparing Stock Solutions for iHAP1

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.

Select a batch to recalculate based on the batch molecular weight:
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 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

If you know of a relevant reference for iHAP1, please let us know.

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