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SML2937

Sigma-Aldrich

iHAP1

≥98% (HPLC)

Synonym(s):

(2-Chloro-10H-phenothiazin-10-yl)(4-methoxyphenyl)methanone, 2-Chloro-10-(4-methoxybenzoyl)-10H-phenothiazine

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$78.18
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5 MG
$78.18
25 MG
$333.00

About This Item

Empirical Formula (Hill Notation):
C20H14ClNO2S
CAS Number:
105925-39-1
Molecular Weight:
367.85
MDL number:
MFCD01245092
UNSPSC Code:
12352200
NACRES:
NA.77

$78.18

List Price$82.30Save 5%
Web-Only Promotion

Available to ship onApril 29, 2025Details

Request a Bulk Order

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

S1c2c(cc(cc2)Cl)N(c4c1cccc4)C(=O)c3ccc(cc3)OC

InChI key

CSWHYHPUEDNIQY-UHFFFAOYSA-N

Related Categories

Biochem/physiol Actions

iHAP1 is a potent activator of protein phosphatase 2A (PP2A) that allosterically facilitates assembly and activation of PP2A holoenzyme complex consisting PPP2R1A, PPP2R5E (B56ε, regulatory), and PPP2CA subunits. iHAP1 induces dephosphorylation of MYBL2 transcription factor on Ser241, causing irreversible cell cycle arrest of leukemia and other cancer cells in prometaphase. iHAP1 exhibits significant antitumor activity and lack of toxicity in T-ALL xenograft mice models. Normal CD34+ HSPCs are appears to be resistant to iHAP1. iHAP1 does not inhibit dopamine receptor D2.
potent allosteric activator of protein phosphatase 2A (PP2A) containing regulatory subunit PPP2R5E (B56ε)

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Ken Morita et al.
Cell, 181(3), 702-715 (2020-04-22)
Protein phosphatase 2A (PP2A) enzymes can suppress tumors, but they are often inactivated in human cancers overexpressing inhibitory proteins. Here, we identify a class of small-molecule iHAPs (improved heterocyclic activators of PP2A) that kill leukemia cells by allosterically assembling a

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