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5.31294

Sigma-Aldrich

Perk Inhibitor III, LDN-0070977

Synonym(s):

Perk Inhibitor III, LDN-0070977, LDN 0070977, PKR-like ER kinase Inhibitor, LDN-0070977, LDN0070977

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About This Item

Empirical Formula (Hill Notation):
C12H8N2O
CAS Number:
Molecular Weight:
196.20
MDL number:
UNSPSC Code:
12352200

Assay

≥98% (HPLC)

Quality Level

form

powder

potency

7 μM IC50

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

off-white

solubility

DMSO: 50 mg/mL

storage temp.

2-8°C

SMILES string

O/N=C(C1=C2N=CC=C1)/C3=C2C=CC=C3

General description

A cell-permeable tricyclic heterocycle oxime that acts as a reversible and non ATP-competitive inhibitor of PERK (PKR-like ER kinase, IC50 = 7.04 µM) and blocks PERK-dependent phosphorylation of elF2a. Shown to reduce thapsigargin-induced elF2a phosphorylation in mouse embryonic fibroblasts over a wide range. Does not exhibit any cellular toxicity up to 50 µM levels.
A cell-permeable, reversible, and non ATP-competitive inhibitor of PERK (PKR-like ER kinase, IC₅₀ = 7.04 µM) and blocks PERK-dependent phosphorylation of elF2a.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
PERK

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Pytel, D., et al. 2014. J. Biomol. Screen.19, 1024.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

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