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Merck
CN

SML2937

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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About This Item

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

Key Documents

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Product Name

iHAP1, ≥98% (HPLC)

SMILES string

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

InChI key

CSWHYHPUEDNIQY-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Quality Level

100

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

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000108514
0000108513
0000105556

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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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