NSC139021

NSC139021 (ERGi-USU) is a RIOK2 inhibitor with anticancer activity. RIOK2 can highly selectively inhibit the growth of ERG-positive cancer cells with IC50s of 30-400 nM against cell lines. RIOK2 also causes cell cycle arrest and apoptosis in glioblastoma via induction of Skp2 and Skp2-p27/p21-Cyclin E/CDK2-pRb signaling[1][2].

Product Specifications

CAS Number

[1147-56-4]

Product Name Alternative

ERGi-USU

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Ser/Thr Kinase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/NSC139021.html

Purity

99.86

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

OC1=C(/N=N/C2=NC=CS2)C3=CC=CC=C3C=C1

Molecular Formula

C13H9N3OS

Molecular Weight

255.30

Precautions

H302, H315, H319, H335

References & Citations

[1]Mohamed AA, et al. Identification of a small molecule that selectively inhibits ERG-positive cancer cell growth. Cancer Res. 2018 Apr 30. pii: canres.2949.2017.|[2]Yu M, et al. RIOK2 Inhibitor NSC139021 Exerts Anti-Tumor Effects on Glioblastoma via Inducing Skp2-Mediated Cell Cycle Arrest and Apoptosis. Biomedicines. 2021 Sep 17;9 (9) :1244.