iHAP1

Name: iHAP1
Brand: tocris
SKU: 7303

Catalog # 7303

Datasheet / COA / SDS

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Bio-Techne Corporation

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$35 to United States

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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

View Full Technical Details for 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

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
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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Reconstitution Calculator

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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