PERK-IN-5

PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor (IC50s of 2 and 9 nM for PERK and p-eIF2α, respectively) . PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model[1].

Product Specifications

CAS Number

[2616821-91-9]

UNSPSC

12352005

Target

PERK

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/perk-in-5.html

Concentration

10mM

Purity

99.40

Solubility

DMSO : 250 mg/mL (ultrasonic)

Smiles

CCC1=C(C2=CN=C(N)C(C(NC(C)C)=O)=C2)C=CC(NC([C@@H](C3=CC(F)=CC(F)=C3)O)=O)=C1

Molecular Formula

C25H26F2N4O3

Molecular Weight

468.50

References & Citations

[1]Calvo V, et al. Discovery of 2-amino-3-amido-5-aryl-pyridines as highly potent, orally bioavailable, and efficacious PERK kinase inhibitors. Bioorg Med Chem Lett. 2021;43:128058.