OM-153

• Description:

  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].

• 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• Isoform:

  TNKS1/PARP5A; TNKS2/PARP5B

• CAS Number:

  [2406278-81-5]