OM-153

Names

[ Name ]:
OM-153

Biological Activity

[Description]:

OM-153 is a potent tankyrase inhibitor with IC50s of 13 and 2 nM for tankyrase 1 and tankyrase 2, respectively. OM-153 shows inhibition of WNT/β-catenin signaling and proliferation in COLO 320DM[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> PARP

Signaling Pathways >> Cell Cycle/DNA Damage >> PARP

[Target]

TNKS1:13 nM (IC50)

TNKS2:2 nM (IC50)

[In Vitro]

OM-153 shows picomolar IC50 inhibition (0.63 nM) in a cellular (HEK293) WNT/β-catenin signaling reporter assay, no off-target liabilities, overall favorable absorption, distribution, metabolism, and excretion (ADME) properties, and an improved pharmacokinetic profile in mice[1].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₈H₂₄FN₇O₂

[ Molecular Weight ]:
509.53

OM-153

Names

Biological Activity

Chemical & Physical Properties

Related Compounds