iHAP1

For research use only.

Catalog No.S9695

iHAP1 Chemical Structure

CAS No. 105925-39-1

iHAP1 is an activator of protein phosphatase 2A (PP2A) enzymes that activates PP2A-B56ε and potently kills malignant cells.

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Biological Activity

Description iHAP1 is an activator of protein phosphatase 2A (PP2A) enzymes that activates PP2A-B56ε and potently kills malignant cells.
Targets
PP2A [1]
()
In vitro

Phenothiazine analog iHAP1 activates PP2A-B56ε and potently kills malignant cells. iHAP1 does not inhibit dopamine signaling or cause prohibitive neurologic toxicity. The PP2A complex activated by iHAP1 dephosphorylates the MYBL2 transcription factor on Ser241, causing irreversible arrest of leukemia and other cancer cells in prometaphase.[1]

In vivo

In preclinical testing against T-ALL xenografts, iHAP1 emerges as a much more promising compound than PPZ, showing improved antitumor activity and lack of toxicity.[1]

Protocol

Cell Research:

[1]

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  • Cell lines: HEK293T cells
  • Concentrations: 0.5 μM
  • Incubation Time: 3 h
  • Method:

    Human dopamine receptor D2 (DRD2) and modified murine Gq5i cDNA are inserted into the pENTR1A dual selection vector, and CSII-EF-MCS-IRES2-Venus and CSII-EF-MCS-IRES2-hKO1 expression vectors. After verifying the PCR products by DNA sequencing, the DRD2 and the Gq5i cDNAs are lentivirally-transduced into HEK293T cells. After establishing HEK293T cells stably expressing both genes, we transfect them with the PathDetect pSRE-Luc Cis-Reporter plasmid. The Gq5i expression enables Gi/o-coupled receptor activity to be detected by using a serum response element (SRE)-luciferase-specific reporter gene. The cells are then starved in FCS free DMEM medium for 6 hours before being incubated with 2 μM dopamine hydrochloride, together with PPZ or iHAP1 at 0.5 μM for 3 hours. The reporter activity is measured with the Pierce Firefly Luciferase Glow Assay kit.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: 8-week-old female C57BL/6 mice, NSG (NOD/Scid/ IL2Rγnull) mice
  • Dosages: 2.5 mg/kg, 80 mg/kg
  • Administration: Oral gavage, IP
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 20 mg/mL (54.36 mM)
Water Insoluble
Ethanol ''5 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 367.85
Formula

C20H14ClNO2S

CAS No. 105925-39-1
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID