|Targets||Polo-like Kinase (PLK)|
|Description||GSK-461364 is a Polo-like kinase 1 inhibitor, is also a small molecule Polo-like kinase 1 (PLK1) inhibitor with potential antineoplastic activity. Polo-like kinase 1 inhibitor GSK461364 selectively inhibits Plk1, inducing selective G2/M arrest followed by apoptosis in a variety of tumor cells while causing reversible cell arrest at the G1 and G2 stage without apoptosis in normal cells. Plk1, named after the polo gene of Drosophila melanogaster, is a serine/threonine protein kinase involved in regulating mitotic spindle function in a non-ATP competitive manner.|
|Appearance||white solid powder|
TAK-960 is an orally available PLK1 inhibitor with potential antineoplastic activity. Polo-like kinase 1 inhibitor TAK-960 selectively inhibits PLK1, inducing ...
SBE13 is a cell-permeable highly potent polo-like kinase (Plk1) inhibitor that targets the inactive conformation of the kinase. Its IC50 value is 0.2 nM. It doe...
TC-S 7005 is a potent and selective polo-like kinase 2 (PLK2) inhibitor (IC50 = 4 nM) with selectivity over PLK3 and PLK1 (IC50 = 24 and 214 nM, respectively). ...
The hydrochloride salt form of TAK-960, a newly studied selective PLK1 inhibitor, might have potential effect in inhibiting proliferation of sorts of cancer cel...
ON1231320, also known as GBO-006, was found to be a specific Polo like kinase 2 (PLK2) inhibitor when profiled against a panel of 288 wild-type, 55 mutant and 1...
TAK-960 is an orally available, potent and selective PLK1 inhibitor that was in a phase I clinical trial in patients with advanced non-hematologic malignancies.
Ro5203280 is a small-molecular PLK1 inhibitor. Ro5203280 shows a high efficacy for suppressing nasopharyngeal carcinoma growth with low toxicity in mouse studie...
Rigosertib (ON-01910 sodium salt), a synthetic benzyl styryl sulfone analogue with potential antineoplastic activity, is a non-ATP-competitive inhibitor of PLK1...
LFM-A13 is a specific Bruton's tyrosine kinase (BTK) with IC50 of 2.5 μM, >100-fold selectivity over other protein kinases including JAK1, JAK2, HCK, EGFR,and I...
The fumarate salt form of CFI-400945, has been found to be a PLK4 inhibitor that could be probably useful in anticancer studies through influencing mitosis and ...
Rigosertib, a synthetic benzyl styryl sulfone, is a non-ATP-competitive inhibitor of PLK1 (IC50=9 nM).
BI 6727 (Volasertib) is a small highly potent Polo-like kinase inhibitor (Plk) with an IC50 of 0 .87 nM and EC50 of 11-37 nM on a panel of cancer cell lines, w...
SBE13 is a cell-permeable highly potent polo-like kinase (Plk1) inhibitor that targets the inactive conformation of the kinase. SBE13 does not effect the activi...
GSK-461364 is a Polo-like kinase 1 inhibitor, is also a small molecule Polo-like kinase 1 (PLK1) inhibitor with potential antineoplastic activity. Polo-like kin...
NMS1286937, also know as NMS-P937, is an orally bioavailable, small-molecule Polo-like kinase 1 (PLK1) inhibitor with potential antineoplastic activity. Polo-l...
MLN0905 is a potent, selective small-molecule PLK1 inhibitor. MLN0905 inhibits cell proliferation in a broad range of human tumor cells including DLBCL cell lin...
Centrinone, a pyrimidinamine derivative, has been found to be a high affinity and selective PLK4 inhibitor (Ki = 0.16 nM).
GSK 461364 analogue I
GSK 461364 analogue I is a potent polo-like kinase (PLK) inhibitor with selectivity for PLK1 (IC50: 2 nM) over PLK3 (IC50: 630 nM).
HMN-214 is an oral prodrug of HMN-176, a stilbene derivative that interferes with the subcellular spatial location of polo-like kinase-1, a serine/threonine kin...
GSK 461364 analogue II
GSK 461364 analogue II is a potent polo-like kinase (PLK) inhibitor with selectivity for PLK1 (IC50: 2 nM) over PLK3 (IC50: 270 nM).