PKN1/2-IN-1

PKN1/2-IN-1 is a potent cell permeabilizer and selective PKN1/2 inhibitor with IC50 values of 16 nM and 210 nM for PKN1 and PKN2, respectively, and Ki values of 8 nM and 108 nM, respectively. PKN1/2-IN-1 exhibits strong intracellular PKN2 binding capacity in NanoBRET assays (IC50 = 2.1 μM) . PKN1/2-IN-1 can be used to study physiological processes such as tumor cell migration[1].

Product Specifications

CAS Number

[942425-34-5]

UNSPSC

12352005

Target

PKC

Type

Reference compound

Related Pathways

Epigenetics; TGF-beta/Smad

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/pkn1-2-in-1.html

Concentration

10mM

Purity

99.92

Solubility

DMSO : 35.71 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

CCN1C(C2=CC=NC=C2)=CC3=C1CCNC3=O

Molecular Formula

C14H15N3O

Molecular Weight

241.29

References & Citations

[1]Scott F, et al. Development of dihydropyrrolopyridinone-based PKN2/PRK2 chemical tools to enable drug discovery. Bioorg Med Chem Lett. 2022;60:128588.