OM-153

OM-153 is a potent and orally active tankyrase inhibitor with IC50s of 13 nM and 2 nM for tankyrase 1 and tankyrase 2 (TNKS1/2), respectively. OM-153 inhibits luciferase-based Wnt/β-catenin signaling reporter activity with an IC50 value of 0.63 nM. OM-153 shows inhibition of Wnt/β-catenin signaling and proliferation in COLO 320DM[1][2].

Product Specifications

CAS Number

[2406278-81-5]

UNSPSC

12352005

Target

PARP; Wnt

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics; Stem Cell/Wnt

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/om-153.html

Concentration

10mM

Purity

99.30

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(C1=C2N=CC=NC2=CC=C1)N[C@H]3C[C@H](C4=NN=C(C5=NC=C(OCC)C=C5)[N@]4[C@]6=CC=CC=C6F)C3

Molecular Formula

C28H24FN7O2

Molecular Weight

509.53

References & Citations

[1]Leenders RGG, et al. Development of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II. J Med Chem. 2021;64 (24) :17936-17949. |[2]Shoshy A. Brinch, et al. The Tankyrase Inhibitor OM-153 Demonstrates Antitumor Efficacy and a Therapeutic Window in Mouse Models. Cancer Research Communications (2022) 2 (4) : 233-245.