WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 206799
Description: ON1231320, also known as GBO-006, is a Polo-like kinase 2 (PLK2) inhibitor. In vitro testing revealed that ON1231320 is a selective inhibitor of PLK2 with no inhibitory activity against PLK1, PLK3 and PLK4. The cytotoxic effect of the drug is mediated by apoptosis as evidenced by the induction of Caspase 3/7 activity and by the cleavage of PARP in a dose dependent manner. ON1231320 affects cell cycle progression by blocking tumor cells in the G2/M phase however it does not affect normal human fibroblasts.
MedKoo Cat#: 206799
Chemical Formula: C22H15F2N5O3S
Exact Mass: 467.0864
Molecular Weight: 467.4508
Elemental Analysis: C, 56.53; H, 3.23; F, 8.13; N, 14.98; O, 10.27; S, 6.86
Synonym: ON1231320; ON-1231320; ON 1231320; GBO-006; GBO006; GBO 006.
IUPAC/Chemical Name: 2-((1H-indol-5-yl)amino)-6-((2,4-difluorophenyl)sulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one
InChi Key: ZEHBZHZMQSHZFI-UHFFFAOYSA-N
InChi Code: InChI=1S/C22H15F2N5O3S/c1-29-20-13(9-19(21(29)30)33(31,32)18-5-2-14(23)10-16(18)24)11-26-22(28-20)27-15-3-4-17-12(8-15)6-7-25-17/h2-11,25H,1H3,(H,26,27,28)
SMILES Code: C1=CC(F)=CC(F)=C1S(=O)(=O)C1=CC2=CN=C(NC3=CC=C4NC=CC4=C3)N=C2N(C)C1=O
The Polo like kinases play key roles in mitosis. While the upregulation of PLK1 in cancer is well documented and PLK3 has been demonstrated to be a tumor suppressor, little is known about the oncogenic significance of PLK2. PLK2 kinase activity is essential for centriolar duplication and is also believed to play a regulatory role in the survival pathway by physically stabilizing the TSC1/2 complex in tumor cells under hypoxic conditions. Protein tyrosine hyper-phosphorylation and the upregulation of serine/threonine kinases associated with cell cycle progression have been linked to the etiology of cancer.