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MilliporeSigma

SML4427

ERK-MYD88 PPI inhibitor EI-52

≥98% (HPLC)

Synonym(s):

2-[4-(Dimethyl-amino)phenyl]-N-(6-methoxy-3-pyridinyl)-1H-benzimidazole-6-carboxamide hydrate, EI-52

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About This Item

Empirical Formula (Hill Notation):
C22H21N5O2 · xH2O
Molecular Weight:
387.43 (anhydrous basis)
UNSPSC Code:
12352200
Assay:
≥98% (HPLC)
Form:
powder
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Quality Segment

assay

≥98% (HPLC)

form

powder

color

gray to very dark black-purple

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

Biochem/physiol Actions

EI-52, a benzimidazole, is a potent and selective inhibitor of ERK-MYD88 interaction (IC50 = 3.1μM). EI-52 binds to the ERK D-recruitment site (DRS) without influence on ERK (ERK1 and ERK2) kinase activity and potently disrupts ERK-MYD88 interaction leading to immunogenic apoptosis specific to cancer cells. ERK-MYD88 PPI inhibitor EI-52 exhibits antitumor activity in mice models and in patient-derived tumor organoids. EI-52 induces an anti-tumor T cell response in mice in vivo.


Pictograms

Exclamation mark

Signal Word

Warning

Hazard Codes

Hazard Classifications

Acute Tox. 4 Oral - Skin Sens. 1B

Storage Class

11 - Combustible Solids

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable



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